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DB00001
|
Lepirudin
|
Lepirudin is a recombinant hirudin formed by 65 amino acids that acts as a highly specific and direct thrombin inhibitor.[L41539,L41569] Natural hirudin is an endogenous anticoagulant found in _Hirudo medicinalis_ leeches.[L41539] Lepirudin is produced in yeast cells and is identical to natural hirudin except for the absence of sulfate on the tyrosine residue at position 63 and the substitution of leucine for isoleucine at position 1 (N-terminal end).[A246609]
Lepirudin is used as an anticoagulant in patients with heparin-induced thrombocytopenia (HIT), an immune reaction associated with a high risk of thromboembolic complications.[A3, L41539] HIT is caused by the expression of immunoglobulin G (IgG) antibodies that bind to the complex formed by heparin and platelet factor 4. This activates endothelial cells and platelets and enhances the formation of thrombi.[A246609] Bayer ceased the production of lepirudin (Refludan) effective May 31, 2012.[L41574]
|
solid
|
Lepirudin is indicated for anticoagulation in adult patients with acute coronary syndromes (ACS) such as unstable angina and acute myocardial infarction without ST elevation. In patients with ACS, lepirudin is intended for use with [aspirin].[L41539] Lepirudin is also indicated for anticoagulation in patients with heparin-induced thrombocytopenia (HIT) and associated thromboembolic disease in order to prevent further thromboembolic complications.[L41539]
|
Lepirudin is a recombinant hirudin that acts as a highly specific thrombin inhibitor. Its activity is measured by anti-thrombin units (ATUs) that correspond to the amount of lepirudin required to neutralize a unit of the World Health Organization α-thrombin (89/588) standard. The activity of lepirudin is 16,000 ATU/mg.[L41539,L41569] A single molecule of lepirudin binds to a molecule of thrombin, blocking its thrombogenic activity. This drug increases activated partial thromboplastin time (aPTT) and PT (INR) values in a dose-dependent manner, and its mode of action is independent of antithrombin III.[L41539,L41569] Platelet factor 4 does not inhibit lepirudin.[L41539,L41569]
The pharmacodynamic effect of lepirudin was evaluated by measuring an increase in aPTT. No saturable effect was observed at the highest tested dose (0.5 mg/kg, IV bolus).[L41539] Thrombin time was considered an unsuitable routine test for lepirudin monitoring due to the high values detected (200 seconds) even at low doses.[L41539] The concomitant use of thrombolytic therapy and lepirudin is not recommended due to the high risk of bleeding that may be life-threatening. In patients with a risk of bleeding, a physician should weigh the risks of lepirudin administration against its benefits. There is also an especially high risk of bleeding in patients who weigh less than 50 kg, and a lower dosage is required. Patients with renal impairment have a higher risk of hemorrhagic adverse events.[L41539]
|
Lepirudin is a direct thrombin inhibitor used as an anticoagulant in patients for whom heparin is contraindicated.[L41539,A3] Thrombin is a serine protease that participates in the blood-clotting cascade, and it is formed by the cleavage of pro-thrombin. Active thrombin cleaves fibrinogen and generates fibrin monomers that polymerize to form fibrin clots.[A246624]
Lepirudin binds to the catalytic and substrate-binding sites of thrombin, forming a stable, irreversible and non-covalent complex.[A246609] This blocks the protease activity of thrombin and inhibits the coagulation process. Each molecule of lepirudin binds to a single molecule of thrombin,[L41539] and unlike [heparin], it is able to inhibit thrombin in both its clot-bound or free states.[A246609]
|
Lepirudin administered as a single intravenous bolus injection of 0.4 mg/kg in 9 healthy volunteers (male and female) resulted in a C<sub>max</sub> of 2924 ng/mL, a t<sub>max</sub> of 0.17 h and an AUC<sub>0-∞</sub> of 2500 ng•h/mL.[L41539] When 0.1, 0.15 and 0.2 mg/kg of lepirudin was administered as a single intravenous infusion over 6 hours in healthy male volunteers, lepirudin had a corresponding C<sub>max</sub> of 111, 203, and 2446 ng/mL and a corresponding AUC of 612, 1184, and 1446 ng•h/mL.[L41544] Bioavailability is 100% following injection. Also, it has been reported that following subcutaneous (sc) administration, the bioavailability of lepirudin is almost 100%.[A246609]
|
As a polypeptide, lepirudin is expected to be metabolized by the sequential cleavage of amino acids by kidney exoproteases, which have carboxypeptidase and dipeptidase-like activity.[L41539,L41544] The C-terminal cleavage of lepirudin aminoacids (aminoacids 1 to 65) produces four metabolites with anti-thrombotic activity: M1 (aminoacids 1 to 64), M2 (aminoacids 1 to 63), M3 (aminoacids 1 to 62), and M4 (aminoacids 1 to 61).[L41544]
|
The acute toxicity of intravenous lepirudin was evaluated in mice (0.1-1000 mg/kg), rats (1-1000 mg/kg), and monkeys (1-100 mg/kg), and toxicity was not detected at the doses investigated.[L41539] The acute toxicity of lepirudin administered subcutaneously was also evaluated in mice (1-1250 mg/kg) and rats (1-500 mg/kg), and no toxicity was detected.[L41539] One rat (100 mg/kg) died of rapid blood loss after the subcutaneous administration of lepirudin. Reactions to local injections such as hemorrhages, hematomas and/or nodules were detected in mice and rats given subcutaneous doses of lepirudin equal or higher than 500 mg/kg and 10 mg/kg, respectively.[L41539]
Chronic toxicity was evaluated in rats and monkeys given lepirudin for up to 3 months. Most of the effects observed were due to the antithrombotic action of lepirudin. After 3 months, hemosiderin deposits in the spleen and moderate sinus histiocytosis in the lymph node were observed in rats. In monkeys, external and internal hemorrhages and hematomas were detected.[L41539] Lepidurin was reported as not mutagenic.[L41539]
Relative overdose may occur in patients with renal impairment, therefore, bolus dose and rate of infusion must be reduced in case of known or suspected renal insufficiency.[L41539] Excessively high activated partial thromboplastin time (aPTT) values suggest an overdose and a risk of bleeding. Lepirudin has no known antidote. In case of life-threatening bleeding and if excessive plasma levels of lepirudin are suspected: 1)stop the administration of lepirudin immediately, 2) determine aPTT and coagulation parameters, 3) determine hemoglobin, and prepare for a transfusion, 4) follow the treatment guidelines for patients with shock.[L41539] Hemofiltration or hemodialysis may be useful in case of overdose, based in single case reports and animal data.[L41539]
|
Lepirudin has an initial half-life of approximately 10 minutes, and in young healthy volunteers, it has a terminal half-time of 1.3 hours.[L41539] Lepirudin has a first-order elimination kinetic; plasma concentration increases proportionally as the lepirudin intravenous dose is increased. Elimination half-life values of up to 2 days were detected in patients with marked renal insufficiency (creatinine clearance < 15 mL/min).[L41539]
|
In human plasma, the protein binding of lepirudin was approximately 3%.[L41539]
|
Lepirudin is mostly excreted through urine (48.3%). About 35% of lepirudin is excreted unchanged, while metabolites are found in a smaller proportion (2.5% of M1, 5.4% of M2, 3.9% of M3 and 1.6% of M4).[L41544]
|
The volume of distribution of lepirudin at steady state was 12.2 L in healthy young subjects (n=18, 18-60 years), 18.7 L in healthy elderly subjects (n=10, 65-80 years), 18.0 L in renally impaired subjects (n=16, creatinine clearance < 80 mL/min, and 32.1 L in heparin-induced thrombocytopenia patients (n=73).[L41539] The distribution of lepirudin is mainly restricted to extracellular fluids.[L41539]
|
The clearance of lepirudin is proportional to the glomerular filtration rate. On average, lepirudin clearance was 164 mL/min in healthy young subjects (n=18, 18-60 years) and 25% lower in women than in men. In healthy elderly subjects (n=10, 65-80 years), clearance was 139 mL/min, about 20% lower than in younger patients.[L41539] This is possibly due to the lower creatinine clearance in elderly patients. In renally impaired subjects (n=16, creatinine clearance < 80 mL/min), clearance was 61 mL/min, and in heparin-induced thrombocytopenia patients (n=73), it was 114 mL/min.[L41539]
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"withdrawn"
] |
[
"B01AE",
"B01A",
"B01",
"B"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "273.19",
"description": "Refludan 50 mg vial",
"unit": "vial"
}
] |
[
{
"approved": "1993-01-19",
"country": "United States",
"expires": "2010-01-19",
"number": "5180668"
}
] |
[Leu1, Thr2]-63-desulfohirudin | Desulfatohirudin | Hirudin variant-1 | Lepirudin | Lepirudin recombinant | R-hirudin | 3.4.21.5 | Coagulation factor II
|
[
"Refludan",
"Refludan",
"Refludan",
"Refludan",
"Refludan",
"Refludan"
] |
[] |
[] |
[
"P00734"
] |
[] |
[] |
[] |
DB01022
|
Phylloquinone
|
Vitamin K1, also called phylloquinone or phytonadione, is a fat soluble vitamin.[L33319,L33345] Phylloquinone is a cofactor of the enzyme γ-carboxylase, which modifies and activates precursors to coagulation factors II, VII, IX, and X.[A234264,A234195,A234259] It is indicated in the treatment of coagulation disorders due to faulty formation of coagulation factors II, VII, IX, and X caused by deficiency or interference in the activity of vitamin K.[L33319]
Phylloquinone has been synthesized since at least 1939,[A234384] and was approved by the FDA prior to 1955.[L33389]
|
liquid
|
Oral phylloquinone is indicated to treat prothrombin deficiency caused by coumarin or indanedione derivatives; and hypoprothrombinemia secondary to antibacterial therapy, salicylates, or obstructive jaundice or biliary fistulas with concomitant bile salt administration.[L33345]
Parenteral (intravenous, intramuscular, and subcutaneous) phylloquinone is indicated to treat coagulation disorders due to faulty formation of coagulation factors II, VII, IX, and X caused by vitamin K deficiency or some interference with vitamin K activity.[L33319] These indications include the above indications as well as hypoprothrombinemia secondary to sprue, ulcerative colitis, celiac disease, intestinal resection, pancreatic cystic fibrosis, or regional enteritis; or hypoprothrombinemia caused by interference with vitamin k metabolism.[L33319]
|
Phylloquinone is a vitamin K indicated in the treatment of coagulation disorders due to faulty formation of coagulation factors II, VII, IX, and X caused by deficiency or interference in the activity of vitamin K.[L33319] It has a long duration of action as vitamin K is cycled in the body,[A234259] and a wide therapeutic index as large doses can be tolerated.[A234284,L33345] Patients should have their prothrombin time monitored during therapy and healthcare professionals should be aware of the increased risk of hypersensitivity reactions with parenteral administration.[L33345]
|
Vitamin K is a cofactor of gamma-carboxylase.[A234264,A234195] Gamma carboxylase attaches carboxylic acid functional groups to glutamate, allowing precursors of factors II, VII, IX, and X to bind calcium ions.[A234259] Binding of calcium ions converts these clotting factors to their active form, which are then secreted from hepatocytes into the blood, restoring normal clotting function.[L33345]
Vitamin K may also carboxylate matrix proteins in chondrocytes, inhibiting calcification of joints, and may increase type II collagen.[A234304] The role of vitamin K in osteroarthritis,[A234304] bone density,[A234309] and vascular calcification[A234314] is currently under investigation.
|
A 4 µg oral dose of phylloquinone is 13% ± 9% bioavailable, with a T<sub>max</sub> of 4.7 ± 0.8 hours.[A234264] 1.5 ± 0.8 nmol is found in the plasma compartment, and 3.6 ± 3.4 nmol is found in the second compartment.[A234264]
A 10 mg intramuscular phylloquinone dose is 89.2% ± 25.4% bioavailable.[A234344] The same dose reaches a mean C<sub>max</sub> of 67 ± 30 ng/mL, with a mean T<sub>max</sub> of 9.2 ± 6.6 hours, and an AUC of 1700 ± 500 h\*ng/mL.[A234344]
A 10 mg intravenous phylloquinone dose has a mean AUC of 1950 ± 450 h\*ng/mL.[A234344]
|
Phylloquinone's phytyl side chain is omega hydroxylated by CYP4F2.[A137578] The side chain is then cleaved to 5 or 7 carbons long, and then glucuronidated prior to elimination.[A234104,A234109,A234114,A234119]
Vitamin Ks in general undergo a cycle of reduction to vitamin K hydroquinone by vitamin K epoxide reductase (VKOR), oxidation to vitamin K epoxide by gamma-glutamyl carboxylase, and converted back to vitamin K by VKOR.[A234259]
|
High doses of vitamin K1 are not associated with toxicity.[A234259] Intravenous administration has been associated with an increased risk of toxicity.[A234284] These patients should be treated with symptomatic and supportive measures.
The intravenous LD<sub>50</sub> in mice is 1170 mg/kg and the oral LD<sub>50</sub> is >24180 mg/kg.[L33345]
|
Intravenous phylloquinone has an initial half life of 22 minutes, followed by a half life of 125 minutes.[A234104]
| null |
Intravenous phylloquinone is 36% eliminated in the feces in 5 days and 22% recovered in urine in 3 days.[A234104,A234329]
|
The steady state volume of distribution of phylloquinone is 20 ± 6 L in subjects who are also taking phenprocoumon therapy.[A234374]
|
Intravenous phylloquinone is 90% cleared in 2 hours, and 99% cleared in 8 hours.[A234104,A234329] A 10 mg intravenous dose of phylloquinone has a mean clearance of 91 ± 24 mL/min.[A234344]
|
Organic compounds
|
Lipids and lipid-like molecules
|
Prenol lipids
|
Quinone and hydroquinone lipids
|
[
"approved",
"investigational"
] |
[
"B02BA",
"B02B",
"B02",
"B"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "2.76",
"description": "Vitamin K1 10 mg/ml",
"unit": "ml"
},
{
"cost": "4.79",
"description": "Vitamin K1 Pediatric 2 mg/ml",
"unit": "ml"
},
{
"cost": "5.95",
"description": "Mephyton 5 mg tablet",
"unit": "tablet"
},
{
"cost": "35.0",
"description": "Vitamin k1 liquid",
"unit": "g"
},
{
"cost": "66.0",
"description": "Phytonadione liquid",
"unit": "g"
},
{
"cost": "111.13",
"description": "Phytonadione crystal",
"unit": "g"
}
] |
[] |
2-Methyl-3-(3,7,11,15-tetramethyl-2-hexadecenyl)-1,4-naphthalenedione | 2-Methyl-3-[(2E)-3,7,11,15-tetramethyl-2-hexadecenyl]naphthoquinone | 2-Methyl-3-phytyl-1,4-naphthochinon | 2-Methyl-3-phytyl-1,4-naphthoquinone | 3-Phytylmenadione | alpha-Phylloquinone | Fitomenadiona | Phyllochinon | Phyllochinonum | Phylloquinone | Phythyl-menadion | Phytomenadione | Phytomenadionum | Phytonadione | Phytonadionum | Phytylmenadione | trans-Phylloquinone | Vitamin K | Vitamin K1 | α-phylloquinone | 4.1.1.90 | Gamma-glutamyl carboxylase | GC | Peptidyl-glutamate 4-carboxylase | Vitamin K gamma glutamyl carboxylase | BGP | Bone Gla protein | Gamma-carboxyglutamic acid-containing protein | 1.14.14.1 | 20-HETE synthase | 20-hydroxyeicosatetraenoic acid synthase | Arachidonic acid omega-hydroxylase | CYPIVF2 | Cytochrome P450-LTB-omega | Docosahexaenoic acid omega-hydroxylase | Leukotriene-B(4) 20-monooxygenase 1 | Leukotriene-B(4) omega-hydroxylase 1 | Phylloquinone omega-hydroxylase CYP4F2 | 2.5.1.- | 2.5.1.39 | TERE1 | Transitional epithelial response protein 1 | 1.17.4.4 | Vitamin K1 2,3-epoxide reductase subunit 1 | VKOR
|
[
"Adeks - Dps",
"Adeks Tablets",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"AquaMEPHYTON",
"AquaMEPHYTON",
"Decara K Vegicaps",
"Infuvite Adult",
"Infuvite Adult",
"Infuvite Pediatric",
"Infuvite Pediatric",
"M.V.I. Adult",
"M.V.I. Adult",
"M.V.I. Paediatric",
"M.V.I. Pediatric",
"Mephyton",
"Mephyton",
"Mephyton",
"Mephyton",
"Mephyton",
"Mephyton",
"Mephyton",
"Mephyton",
"Mephyton",
"Mephyton",
"Mephyton",
"Multi-12/k1 Pediatric",
"Mvc 9+4 Inj",
"Omega-3 Rx Complete",
"Pediatric Infuvite Multiple Vitamins",
"Pediatric Infuvite Multiple Vitamins",
"Pediatric Infuvite Multiple Vitamins",
"Pediatric Infuvite Multiple Vitamins",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione",
"Phytonadione Inj 2mg/ml",
"Phytonadione Phytonadione",
"Pro Hers Vanilla",
"Pro Pcos Citrus",
"Truemed Group LLC",
"Vitalipid N",
"Vitalipid N",
"Vitalipid N",
"Vitamin D2 and K1",
"Vitamin K1",
"Vitamin K1",
"Vitamin K1",
"Vitamin K1",
"Vitamin K1",
"Vitamin K1",
"Vitamin K1",
"Vitamin K1",
"Vitamin K1",
"Vitamin K1 - Phytonadione",
"Vitamin K1 Inj 10mg/ml",
"Vitamin K1 Inj 2mg/ml",
"Vitamin K1 Phytonadione"
] |
[
"Aqua-Mephyton",
"Konakion"
] |
[
"Omega-3 Rx Complete",
"M.V.I. Pediatric",
"Pro Pcos Citrus",
"Pro Hers Vanilla",
"M.V.I. Adult",
"M.V.I. Adult",
"Pediatric Infuvite Multiple Vitamins",
"Pediatric Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Pediatric Infuvite Multiple Vitamins",
"Pediatric Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Adult Infuvite Multiple Vitamins",
"Decara K Vegicaps",
"Mvc 9+4 Inj",
"M.V.I. Paediatric",
"Multi-12/k1 Pediatric",
"Adeks - Dps",
"Adeks Tablets",
"Vitamin D2 and K1",
"Vitalipid N",
"Vitalipid N",
"Vitalipid N",
"Infuvite Adult",
"Infuvite Adult",
"Infuvite Pediatric",
"Infuvite Pediatric"
] |
[
"P38435",
"P02818"
] |
[
"P78329",
"Q9Y5Z9",
"Q9BQB6"
] |
[] |
[] |
DB01373
|
Calcium
|
Calcium plays a vital role in the anatomy, physiology and biochemistry of organisms and of the cell, particularly in signal transduction pathways. The skeleton acts as a major mineral storage site for the element and releases Ca2+ ions into the bloodstream under controlled conditions. Circulating calcium is either in the free, ionized form or bound to blood proteins such as serum albumin. Although calcium flow to and from the bone is neutral, about 5 mmol is turned over a day. Bone serves as an important storage point for calcium, as it contains 99% of the total body calcium. Low calcium intake may also be a risk factor in the development of osteoporosis. The best-absorbed form of calcium from a pill is a calcium salt like carbonate or phosphate. Calcium gluconate and calcium lactate are absorbed well by pregnant women. Seniors absorb calcium lactate, gluconate and citrate better unless they take their calcium supplement with a full breakfast.
|
solid
|
Calcium plays a vital role in the anatomy, physiology and biochemistry of organisms and of the cell, particularly in signal transduction pathways. It is vital in cell signaling, muscular contractions, bone health, and signalling cascades.
|
Calcium (Ca2+) plays a pivotal role in the physiology and biochemistry of organisms and the cell. It plays an important role in signal transduction pathways, where it acts as a second messenger, in neurotransmitter release from neurons, contraction of all muscle cell types, and fertilization. Many enzymes require calcium ions as a cofactor, those of the blood-clotting cascade being notable examples. Extracellular calcium is also important for maintaining the potential difference across excitable cell membranes, as well as proper bone formation.
|
Calcium plays a vital role in the anatomy, physiology and biochemistry of organisms and of the cell, particularly in signal transduction pathways. More than 500 human proteins are known to bind or transport calcium. The skeleton acts as a major mineral storage site for the element and releases Ca2+ ions into the bloodstream under controlled conditions. Circulating calcium is either in the free, ionized form or bound to blood proteins such as serum albumin. Parathyroid hormone (secreted from the parathyroid gland) regulates the resorption of Ca2+ from bone. Calcitonin stimulates incorporation of calcium in bone, although this process is largely independent of calcitonin. Although calcium flow to and from the bone is neutral, about 5 mmol is turned over a day. Bone serves as an important storage point for calcium, as it contains 99% of the total body calcium. Low calcium intake may also be a risk factor in the development of osteoporosis. The best-absorbed form of calcium from a pill is a calcium salt like carbonate or phosphate. Calcium gluconate and calcium lactate are absorbed well by pregnant women. Seniors absorb calcium lactate, gluconate and citrate better unless they take their calcium supplement with a full breakfast. The currently recommended calcium intake is 1,500 milligrams per day for women not taking estrogen and 800 milligrams per day for women on estrogen. There is close to 300 milligrams of calcium in one cup of fluid milk. Calcium carbonate is currently the best and least expensive form of calcium supplement available.
| null | null | null | null | null |
The kidney excretes 250 mmol a day in urine, and resorbs 245 mmol, leading to a net loss in the urine of 5 mmol/d.
| null | null | null | null | null | null |
[
"nutraceutical"
] |
[
"M05BB",
"M05B",
"M05",
"M",
"A11AA",
"A11A",
"A11",
"A",
"M05BB",
"M05B",
"M05",
"M",
"A11GB",
"A11G",
"A11",
"A",
"M05BB",
"M05B",
"M05",
"M",
"M05BB",
"M05B",
"M05",
"M",
"M05BB",
"M05B",
"M05",
"M"
] |
[
"Humans and other mammals"
] |
[] |
[] |
Calcio | Calcium, elemental | Elemental calcium | Kalzium | CACH2 | CACN2 | CACNL1A1 | Calcium channel, L type, alpha-1 polypeptide, isoform 1, cardiac muscle | CCHL1A1 | Voltage-gated calcium channel subunit alpha Cav1.2 | 7.2.2.10 | ATP-dependent Ca(2+) pump PMR1 | ATPase 2C1 | Ca(2+)/Mn(2+)-ATPase 2C1 | KIAA1347 | PMR1L | Secretory pathway Ca(2+)-transporting ATPase type 1 | SPCA1 | TN-C | TNNC | Beta-II spectrin | Fodrin beta chain | Spectrin, non-erythroid beta chain 1 | SPTB2 | S-100 protein beta chain | S-100 protein subunit beta | S100 calcium-binding protein B | Calpain inhibitor | Sperm BS-17 component | COMP | Thrombospondin-5 | TSP5 | 1.4.3.22 | ABP | ABP1 | Amiloride-binding protein | Amiloride-binding protein 1 | Amine oxidase copper domain-containing protein 1 | DAO | Diamine oxidase | Histaminase | KAO | KDAO | Kidney amine oxidase | S100 calcium-binding protein A13 | 3.1.3.1 | Alkaline phosphatase Regan isozyme | Placental alkaline phosphatase 1 | PLAP | PLAP-1 | CAGA | Calgranulin-A | Calprotectin L1L subunit | CFAG | Cystic fibrosis antigen | Leukocyte L1 complex light chain | Migration inhibitory factor-related protein 8 | MRP-8 | MRP8 | p8 | S100 calcium-binding protein A8 | Urinary stone protein band A | CAGB | Calgranulin-B | Calprotectin L1H subunit | CFAG | Leukocyte L1 complex heavy chain | Migration inhibitory factor-related protein 14 | MRP-14 | MRP14 | p14 | S100 calcium-binding protein A9 | CAN19 | Protein S-100L | S100 calcium-binding protein A2 | S100L | Cuproxidase ceruloplasmin | Ferroxidase ceruloplasmin | Glutathione peroxidase ceruloplasmin | Glutathione-dependent peroxiredoxin ceruloplasmin | BMP-2B | BMP-4 | BMP2B | Bone morphogenetic protein 2B | DVR4 | Cell growth-inhibiting gene 36 protein | MGLAP | MGP | KIAA1313 | ALG-2 | ALG2 | Apoptosis-linked gene 2 protein homolog | CALM | CAM | CAM1 | CAM2 | CAMB | CALML2 | CAM3 | CAMC | CAMIII
|
[
"24 Multivitamins + Minerals",
"50 Plus Multiple Vitamins & Minerals",
"7030 Calcium Gold",
"7030 Calcium Gold",
"7030 Calcium Premium",
"7030 Calcium Premium",
"7030 Calcium Premium",
"A D Calcium Tab",
"A-D Calcium Cap",
"A.R.T.H. Away Formula",
"A/o-26 - Caplet",
"Acti-cal/mag 2:1 + Zinc and D Caplet",
"Actical Plus Calcium-magnesium-vitamin D3-silicon Chewable",
"Active Calcium Plus Magnesium, Vitamin D and Silicon",
"Ad & Calcium Cap",
"Ad Calcium Cap",
"Adult Formula 50+",
"Advanced B & T Formula",
"Ag-X",
"Ag-X",
"Alkadrenergy Tablets",
"Anaplex Tab",
"Astral C Tab",
"Avon Vitadvance Multi-kids Complete",
"B & J Formula Dietary Supplement",
"B-Nexa",
"B-Nexa",
"Biocalth Calcium Powder",
"Biocalth Calcium Supplement",
"Body Rox",
"Bseltzer",
"C P Re",
"C. Vit-min Formula",
"C.H.V. Formula",
"Cal & Mag Hvp Chel Plus C Potass & Zinc Tab",
"Cal Gel Cap 45mg",
"Cal Mag Drink With Vitamin C",
"Cal Mag Plus - Tab",
"Cal-mag Citrate Zinc & Vitamin D Tablets",
"Cal-mag With Zinc & Vitamin D",
"Cal/mag 1:1 With Zinc and Vitamin D - Tablet",
"Cal/mag 2:1 With D",
"Cal/mag+d",
"Calci A and D Tab",
"Calcimag Tab",
"Calcitol",
"Calcium",
"Calcium & Magnesium Citrate Plus D With Manganese, Potassium & Zinc",
"Calcium & Magnesium Citrate Plus D With Manganese, Potassium & Zinc",
"Calcium & Magnesium Plus Potassium & Zinc",
"Calcium & Magnesium Plus Potassium & Zinc",
"Calcium & Magnesium Plus Potassium & Zinc",
"Calcium & Magnesium Plus Potassium, Zinc, & Manganese",
"Calcium & Magnesium With Potassium & Zinc",
"Calcium & Magnesium With Potassium, Zinc, Manganese & Vitamin D",
"Calcium 400 With Magnesium - Pwr",
"Calcium 650mg Tab",
"Calcium A D",
"Calcium and Magnesium 1:1 Plus Tablets",
"Calcium Capsules With Magnesium and Vitamin D",
"Calcium Chelate Plus Vit D",
"Calcium Citramate",
"Calcium Complex High Grade",
"Calcium Et Magnesium Plus Vitamine D/fe/zn",
"Calcium Et Magnesium Tab",
"Calcium Liquid",
"Calcium Liquid Syrup",
"Calcium Magnesium 1000/500 - Tab",
"Calcium Magnesium Avec Vitamine D Et Zinc",
"Calcium Magnesium Sulfur Silicon - Tab",
"Calcium Phosphorus & Vitamin D",
"Calcium Sandoz Syr 110mg/5ml",
"Calcium Syrup 110mg/5ml",
"Calcium With Mg Zn Mn Cu CR Si and Vit. C & D",
"Calcium With Vitamin D 200 Mg/160 Iu",
"Calcium/magnesium Drink",
"Calcor",
"Calplus",
"Card-floe II Tab",
"Cavan One",
"Cavan-EC SOD DHA",
"Cell-wise",
"Cell-wise Natural Source",
"Central-vite 18 Essential",
"Century Complete",
"Chela Calmag-100 Plus Zinc D3",
"Chela Calmag-300 Plus Zinc D3",
"Chelamins Plus Tab",
"Chelated Cal-mag(2:1)with Zn Vit.c and D",
"Chelated Cal/mag/zn With Vitamins",
"Chelated Calcium and Magnesium Tab",
"Chelated Calcium Supplement - 150mg Tab",
"Chelazome Calcium 125mg",
"Chewable Adult Multivitamins With Minerals",
"Chewable Cal-mag Chocolate Flavour",
"Chewable Calcium & Magnesium 2:1 Tablet",
"Chewable Calcium Plus Magnesium and Minerals",
"Chewable Children's Complete Multivitamins With Essential Minerals",
"Children's Chewable Multi-vitamin Complete With Minerals",
"Children's Chewable Multivitamin Complete With Minerals",
"Children's Chewable Multivitamins and Minerals",
"Children's Chewable Multivitamins With Minerals",
"Classic Swiss One 10 Multivitamin and Mineral Tab",
"Complete Multivitamins and Minerals Tablets Timed Release",
"Complete One A Day Tab",
"Complete One-A-day - Tab",
"D T B T",
"Doctor's Choice Brand for Men",
"ENA Actimineral A",
"Envirocomplex",
"Enviroflex - Tab",
"Essential Vitamins and Minerals",
"Extra Once A Day",
"Fem Time Tab",
"Ferrous Sulfate",
"Focalgin B",
"Folcaps Omega-3",
"Folgard",
"For-2",
"Formula A.R.-th Dietary Supplement",
"Formula Inf",
"Formula Int",
"Formula O-care Vitamin and Mineral Supplement",
"Formula Osg",
"Fusion Activator Formula Tab",
"Fusion PM Formula Tab",
"Gellucal Cap 45mg",
"Global Vigen Recare Calcium",
"Grand Master Formula Tab",
"Great Calcium",
"Great Calcium",
"H.W. Children's Chewable Multi Vit & Mineral",
"HANTAI 8030 Ca-D3 GOLD",
"HANTAI 8030 Ca-D3 GOLD",
"HANTAI 8030 Ca-D3 Premium",
"HANTAI 8030 Ca-D3 Premium",
"HANTAI 8030 Ca-D3 Premium",
"Hemarexin Tab",
"Hi Potency Multi Tab",
"Hsn Formula",
"Hvp Chelated Cal/mag With Zinc and Vitamins C and D",
"Hypo Vites Tab",
"Innersource Tab",
"Isotonix Calcium Plus Formula",
"K.L. Vitamin-mineral",
"Kanga-V Multivitamins & Minerals",
"Korea Calcium King",
"Korea Calcium King",
"Korea Calcium King",
"L.G.I.T.",
"Leonas Calcium Plus Vitamin D3",
"Liquid Calcium and Magnesium With Vit.d",
"Liquid Calcium Mg Phosphorus and Vit.d-3",
"Liquid Calcium With Vitamin D",
"Liquid Opti-minplex +d",
"Luna Vitamin and Mineral Bar for Women",
"M-Natal Plus",
"M-Natal Plus",
"M-Natal Plus",
"M-Natal Plus",
"Mag/cal 1:1 Capsules W Vitamin D",
"Magnacal",
"Magnesium Chloride",
"Maintain Multiple Vitamin & Minerals",
"Maximum Once A Day",
"Maxine Vitamin and Mineral Supplement",
"Maxum Multi-vite",
"Mega Capsules",
"Mega Multiple Minerals",
"Mega Plex III - Pck",
"Mega Plex III - Pck",
"Mega Plex IV - Pck",
"Mega Plex IV - Pck",
"Mega-vim 75 With Beta-carotene - Tablets",
"Mega-vim 75 With Beta-carotene - Tablets",
"Men's",
"Men's 50+",
"Men's Biomultiple Vitamin and Mineral Supplement",
"Milltrium Senior Vitamin and Mineral Supplement",
"Mineral Support",
"Mnps Formula Supplement",
"Mor-vites Tab",
"Multi #2",
"Multi Cal Mag Liquid",
"Multi Flow Tablets",
"Multi II IV Vi Tab",
"Multi Mega Minerals With Vitamin D",
"Multi Plex I - Tab",
"Multi Plex II - Tab",
"Multi Rol",
"Multi Spectrum - Tablet",
"Multi Tabs",
"Multi Vitamin & Minerals",
"Multi Vitamins & Minerals",
"Multi-actin",
"Multi-mins Minerals",
"Multi-vitamins With Minerals",
"Multicaps",
"Multimineral Chelates",
"Multimineral Tablets",
"Multiminerals",
"Multipack II",
"Multiple Mineral Liquid",
"Multiple Minerals",
"Multiple Vitamin Plus Minerals Tab",
"Multiple Vitamins and Minerals Tab",
"Multiple Vitamins W Minerals Tab",
"Multiple Vitamins With Minerals Tablets",
"Multitabs",
"Multivitamin & Minerals (iron Free)",
"Multivitamin & Multimineral",
"Multivitamines Et Mineraux Reguliers / Regular Multivitamins and Minerals",
"Multivitamins and Minerals - Complete",
"Multivitamins and Minerals for Men",
"Multivitamins and Minerals for Women",
"Multivitamins and Minerals Tablets",
"Multivitamins and Minerals With Betacarotene Tablets",
"Multivitamins and Multiminerals Formula Regular Tablet",
"Multra Plex",
"Multra With Iron",
"Nata Komplete",
"Natelle One",
"Natural Liquid Mineral Supplement",
"Natural Source Spectrum With Beta Carotene",
"Neonatal Plus Vitamin",
"Neonatal Vitamin",
"NESTABS ABC Prenatal Multi-vitamin/Mineral Supplement with DHA/EPA",
"Nexa Plus",
"Nexa Plus",
"Nexa Select Rx Prenatal Vitamin with Plant-Based DHA",
"Nitro Vites - Tab",
"Nutra Boost",
"Nutra-clear",
"Nutri-chem Cal Mag",
"Nutri-chem Calcium Magnesium With D and Zinc",
"Nutrifer Plus Tablets",
"Nutrilite Double X",
"Nutrilite Double X",
"Nutrilite Double X",
"O-Cal FA multivitamin",
"O-Cal Prenatal Vitamin",
"Olympian Multi Vit Plus Minerals Tab",
"Omega-3 Rx Complete",
"One A Day Advance Adults",
"One A Day Advance Adults 50+",
"One A Day Multiple Vit W Minerals",
"One A Day Tab",
"One Daily Vitamin and Mineral Dietary Supplement",
"Only One - Tablet",
"OnlyCal",
"Opti-cal Chewable +d Caplet",
"Osteo Factors",
"Osteo Formula",
"Osteo Formula",
"Osteo Formula",
"Osteo Formula",
"Osteo Formula Tab",
"Osteo Regime",
"Osteo Tablets",
"Osteo-force",
"Osteo-life",
"Osteoligo",
"Osteoshield",
"Oyster Shell Calcium with Vitamin D",
"Oyster Shell Calcium with Vitamin D",
"P D All",
"P D All M",
"P D M",
"Paramettes Adults",
"Phytofortis + Calcium A-D",
"Pnv-dha",
"Pnv-dha",
"Port A Mins Super Cal-mag 300/150 With Vitamin D3",
"Port A Mins Super Cal-mag 600/300",
"Port A Mins Super Calcium 375 With Vitamin D3",
"Port A Mins Super Calcium 750 With Vitamin D3",
"PreFol-DHA",
"Premel",
"Premium Prenatal",
"Premium Prenatal - Tablets",
"Prenara",
"Prenatal",
"Prenatal Formula Tab",
"Prenatal Vi-min",
"Prenatal Vitamin and Mineral Supplement",
"Prenatal Vitamin No 53 Iron Fum Folic Acid Docusate CA DHA",
"PreNatal Vitamins Plus",
"PreNatal Vitamins Plus",
"Prenatvite",
"Prenatvite Complete",
"Prenatvite Plus",
"Preplus",
"Preplus",
"Prevencal 300 + D A Croquer",
"Protect Plus SO 60",
"Pure Calcium calcium",
"Resto L",
"Restoration Treatment",
"Revitex Ampoules Et Comprimes",
"Revival 1 Tab",
"Right Choice P.M. Multi Formula - Caplet",
"Rocky Mountain Multiple Vit and Min Mega Tab",
"Senior Multi One",
"Spd Tab",
"Spectrum 2 Cap",
"Spectrum Performa Multivitamins and Minerals Tablets",
"Sub small molecule disinfectant",
"Super Cal Mag Plus",
"Super Kids Chewable Multivitamin Multimineral (chewable Tablets)",
"Super Multi",
"Super Vita Vim Multivitamins and Minerals",
"Super Vita-vim With Beta-carotene - Tab",
"Supplements De Vitamines Et Mineraux",
"Swical D-M - Tab",
"Swical Extra-fort",
"Swical-energy 3e Age",
"Swical-multi",
"Swiss One",
"Swiss One Multi Vit & Chel Min Tab",
"Swiss One Multivitamin and Mineral Caplet",
"Swiss Total One",
"T-PA Cap",
"Tall G U",
"Tianshi Calcium With Natural Source Vitamin D Tablets",
"Tianshi Vital Powder I",
"Tianshi Vital Powder II",
"Tianshi Vital Powder III",
"Timed Release and Esterified Vitamin C-500",
"Timed Release Vita-vim Srt",
"Total Living Concepts Formula One - Tab",
"Total Living Concepts Formula One - Tab",
"Tri-mins - Cap",
"Tropicana Calcium & Vitamin C Supplement",
"Tropicana Calcium and Vitamin C Supplement",
"Tropicana Calcium Supplement 344 mg",
"Tropicana Calcium Supplement 393 mg",
"Tropicana Calcium Supplement 604 mg",
"Twin G.F. Powder",
"Twin G.F. Powder",
"Twin G.F. Powder Vanilla Flavor",
"Twin Opti Pwr",
"Ultimate Tab",
"UltimateCare ONE NF",
"Usana Calmag Plus Tablets - Tab",
"Usana Multimineral Tablets",
"Usana Multimineral Tablets - Tab",
"Usana Optimizer Actical Plus Calcium-magnesium-vitamin D3-silicon Tablets",
"V & M Vitamin and Mineral Supplement",
"Vc II",
"Vege 1 Daily Tab",
"Vege Swiss One Multivitamin W Chel Mins Tab",
"VIL-Rx",
"Vimeral Tab",
"Vimeral Tab",
"Vita Balance 2000",
"Vita Plex Tab",
"Vita Vim Multivitamins and Minerals Tab",
"Vita-vim - Tab",
"Vitaflex Dietary Suplement",
"Vitafol Caplet",
"Vitafol OB Caplet",
"Vitafol-OB Plus DHA Prenatal Supplement Plus DHA",
"Vitalife - Capsule",
"Vitality Brand Calcium Plus Tab",
"Vitamin & Mineral Formula 1 Dietary Supplement",
"Vitamin C W Chelates Tab",
"Vitaplex",
"Vyo Cylate - Pwr",
"Women's Biomultiple Vitamin and Mineral Supplement",
"Women's Change Formula",
"Zingiber"
] |
[] |
[
"Pure Calcium calcium",
"Oyster Shell Calcium with Vitamin D",
"O-Cal Prenatal Vitamin",
"Cavan One",
"Zingiber",
"PreNatal Vitamins Plus",
"Prenatal Vitamin No 53 Iron Fum Folic Acid Docusate CA DHA",
"Vitafol Caplet",
"Ferrous Sulfate",
"PreFol-DHA",
"Focalgin B",
"Nata Komplete",
"PreNatal Vitamins Plus",
"Cavan-EC SOD DHA",
"Nexa Plus",
"Nexa Select Rx Prenatal Vitamin with Plant-Based DHA",
"UltimateCare ONE NF",
"Folcaps Omega-3",
"B-Nexa",
"B-Nexa",
"Pnv-dha",
"Pnv-dha",
"Neonatal Plus Vitamin",
"Omega-3 Rx Complete",
"Natural Liquid Mineral Supplement",
"Preplus",
"Prenatal",
"Magnesium Chloride",
"Neonatal Vitamin",
"Leonas Calcium Plus Vitamin D3",
"Preplus",
"Vitafol OB Caplet",
"Oyster Shell Calcium with Vitamin D",
"Prenatvite",
"Prenatvite Plus",
"Prenatvite Complete",
"M-Natal Plus",
"Prenara",
"Sub small molecule disinfectant",
"Revival 1 Tab",
"Nutrifer Plus Tablets",
"Prenatal Vitamin and Mineral Supplement",
"Vita Plex Tab",
"Premium Prenatal - Tablets",
"Vyo Cylate - Pwr",
"Multiple Vitamins W Minerals Tab",
"Hypo Vites Tab",
"Multiple Vitamin Plus Minerals Tab",
"Vc II",
"One A Day Tab",
"Olympian Multi Vit Plus Minerals Tab",
"Vitaplex",
"Hemarexin Tab",
"One Daily Vitamin and Mineral Dietary Supplement",
"One A Day Multiple Vit W Minerals",
"Premium Prenatal",
"Right Choice P.M. Multi Formula - Caplet",
"Multiple Vitamins and Minerals Tab",
"Swical-energy 3e Age",
"Milltrium Senior Vitamin and Mineral Supplement",
"C. Vit-min Formula",
"Natelle One",
"NESTABS ABC Prenatal Multi-vitamin/Mineral Supplement with DHA/EPA",
"O-Cal FA multivitamin",
"VIL-Rx",
"Folgard",
"Nexa Plus",
"M-Natal Plus",
"Vitafol-OB Plus DHA Prenatal Supplement Plus DHA",
"Cal/mag+d",
"Hi Potency Multi Tab",
"Maxine Vitamin and Mineral Supplement",
"Mag/cal 1:1 Capsules W Vitamin D",
"Calcium Magnesium Avec Vitamine D Et Zinc",
"Swiss One Multivitamin and Mineral Caplet",
"Vege Swiss One Multivitamin W Chel Mins Tab",
"Liquid Opti-minplex +d",
"Acti-cal/mag 2:1 + Zinc and D Caplet",
"Mor-vites Tab",
"Rocky Mountain Multiple Vit and Min Mega Tab",
"Extra Once A Day",
"Opti-cal Chewable +d Caplet",
"Ultimate Tab",
"A-D Calcium Cap",
"Multiminerals",
"T-PA Cap",
"Multi-mins Minerals",
"Calcium Et Magnesium Plus Vitamine D/fe/zn",
"Multi Flow Tablets",
"Fusion Activator Formula Tab",
"Fusion PM Formula Tab",
"Calcium With Mg Zn Mn Cu CR Si and Vit. C & D",
"Paramettes Adults",
"Maximum Once A Day",
"Liquid Calcium Mg Phosphorus and Vit.d-3",
"Osteo Formula Tab",
"Innersource Tab",
"Prenatal Formula Tab",
"Timed Release Vita-vim Srt",
"Astral C Tab",
"Card-floe II Tab",
"Avon Vitadvance Multi-kids Complete",
"Liquid Calcium and Magnesium With Vit.d",
"Super Vita Vim Multivitamins and Minerals",
"Natural Source Spectrum With Beta Carotene",
"Chelated Cal-mag(2:1)with Zn Vit.c and D",
"Vitality Brand Calcium Plus Tab",
"Osteo Tablets",
"Calcium Magnesium 1000/500 - Tab",
"Calcium Magnesium Sulfur Silicon - Tab",
"Calcium A D",
"Total Living Concepts Formula One - Tab",
"Total Living Concepts Formula One - Tab",
"Twin Opti Pwr",
"Cal Mag Plus - Tab",
"Twin G.F. Powder",
"Twin G.F. Powder Vanilla Flavor",
"Twin G.F. Powder",
"Only One - Tablet",
"Vita Vim Multivitamins and Minerals Tab",
"Mega-vim 75 With Beta-carotene - Tablets",
"Mega-vim 75 With Beta-carotene - Tablets",
"Swical D-M - Tab",
"Prenatal Vi-min",
"Multiple Minerals",
"Anaplex Tab",
"Grand Master Formula Tab",
"Ad & Calcium Cap",
"Multiple Mineral Liquid",
"Ad Calcium Cap",
"A D Calcium Tab",
"Mega Capsules",
"Vitalife - Capsule",
"Multi Spectrum - Tablet",
"24 Multivitamins + Minerals",
"Calcitol",
"Vitamin C W Chelates Tab",
"H.W. Children's Chewable Multi Vit & Mineral",
"Cal/mag 1:1 With Zinc and Vitamin D - Tablet",
"Calcium 400 With Magnesium - Pwr",
"Tri-mins - Cap",
"Vimeral Tab",
"Vimeral Tab",
"Complete One-A-day - Tab",
"A/o-26 - Caplet",
"Usana Multimineral Tablets - Tab",
"Usana Calmag Plus Tablets - Tab",
"Multi Rol",
"Phytofortis + Calcium A-D",
"Calcium Chelate Plus Vit D",
"Calcium Et Magnesium Tab",
"Calci A and D Tab",
"Women's Change Formula",
"For-2",
"Maxum Multi-vite",
"Usana Multimineral Tablets",
"Vita-vim - Tab",
"Super Vita-vim With Beta-carotene - Tab",
"Enviroflex - Tab",
"Chewable Cal-mag Chocolate Flavour",
"Timed Release and Esterified Vitamin C-500",
"Envirocomplex",
"Swical-multi",
"Doctor's Choice Brand for Men",
"Osteoligo",
"Usana Optimizer Actical Plus Calcium-magnesium-vitamin D3-silicon Tablets",
"Cal/mag 2:1 With D",
"Multi #2",
"Port A Mins Super Cal-mag 300/150 With Vitamin D3",
"Port A Mins Super Calcium 375 With Vitamin D3",
"Port A Mins Super Calcium 750 With Vitamin D3",
"Port A Mins Super Cal-mag 600/300",
"Century Complete",
"Central-vite 18 Essential",
"Swiss One",
"Formula Osg",
"Multi Cal Mag Liquid",
"Formula A.R.-th Dietary Supplement",
"Mega Multiple Minerals",
"Chewable Calcium Plus Magnesium and Minerals",
"Children's Chewable Multivitamins and Minerals",
"Osteo-force",
"Cell-wise",
"Multivitamines Et Mineraux Reguliers / Regular Multivitamins and Minerals",
"Isotonix Calcium Plus Formula",
"Calplus",
"Nutri-chem Cal Mag",
"Calcium and Magnesium 1:1 Plus Tablets",
"Calcimag Tab",
"Cell-wise Natural Source",
"Complete Multivitamins and Minerals Tablets Timed Release",
"Calcium Phosphorus & Vitamin D",
"Tropicana Calcium and Vitamin C Supplement",
"Mineral Support",
"Calcium & Magnesium Citrate Plus D With Manganese, Potassium & Zinc",
"Calcium & Magnesium Plus Potassium & Zinc",
"Vitamin & Mineral Formula 1 Dietary Supplement",
"Osteo-life",
"L.G.I.T.",
"A.R.T.H. Away Formula",
"Calcium/magnesium Drink",
"Osteo Formula",
"Multiple Vitamins With Minerals Tablets",
"Super Kids Chewable Multivitamin Multimineral (chewable Tablets)",
"Actical Plus Calcium-magnesium-vitamin D3-silicon Chewable",
"Supplements De Vitamines Et Mineraux",
"Chelated Cal/mag/zn With Vitamins",
"C.H.V. Formula",
"Multivitamins and Minerals - Complete",
"Children's Chewable Multi-vitamin Complete With Minerals",
"Multi Vitamins & Minerals",
"Formula Inf",
"Formula Int",
"Classic Swiss One 10 Multivitamin and Mineral Tab",
"Calcium & Magnesium Plus Potassium, Zinc, & Manganese",
"Calcium & Magnesium Citrate Plus D With Manganese, Potassium & Zinc",
"Multi-vitamins With Minerals",
"Multra Plex",
"Formula O-care Vitamin and Mineral Supplement",
"Luna Vitamin and Mineral Bar for Women",
"Chewable Calcium & Magnesium 2:1 Tablet",
"Calcium & Magnesium With Potassium & Zinc",
"Calcium & Magnesium With Potassium, Zinc, Manganese & Vitamin D",
"Cal-mag With Zinc & Vitamin D",
"Osteo Formula",
"Tropicana Calcium & Vitamin C Supplement",
"Multivitamins and Minerals for Men",
"Multivitamins and Minerals for Women",
"Osteo Factors",
"Calcium & Magnesium Plus Potassium & Zinc",
"Multra With Iron",
"Senior Multi One",
"Multitabs",
"Multipack II",
"Multimineral Chelates",
"Chewable Adult Multivitamins With Minerals",
"Multicaps",
"Children's Chewable Multivitamins With Minerals",
"Men's",
"Men's 50+",
"Multimineral Tablets",
"Multivitamins and Multiminerals Formula Regular Tablet",
"One A Day Advance Adults 50+",
"Bseltzer",
"Nutri-chem Calcium Magnesium With D and Zinc",
"Osteo Formula",
"Children's Chewable Multivitamin Complete With Minerals",
"Multivitamins and Minerals With Betacarotene Tablets",
"One A Day Advance Adults",
"Multi Vitamin & Minerals",
"Essential Vitamins and Minerals",
"Super Multi",
"Adult Formula 50+",
"Calcium With Vitamin D 200 Mg/160 Iu",
"Super Cal Mag Plus",
"Active Calcium Plus Magnesium, Vitamin D and Silicon",
"Multi Tabs",
"Magnacal",
"Premel",
"Hsn Formula",
"Multivitamin & Minerals (iron Free)",
"Cal Mag Drink With Vitamin C",
"Multivitamin & Multimineral",
"Osteo Regime",
"Nutrilite Double X",
"Nutrilite Double X",
"Nutrilite Double X",
"50 Plus Multiple Vitamins & Minerals",
"Chewable Children's Complete Multivitamins With Essential Minerals",
"Calcium Capsules With Magnesium and Vitamin D",
"Spectrum Performa Multivitamins and Minerals Tablets",
"Multi Mega Minerals With Vitamin D",
"Body Rox",
"Swiss Total One",
"Multivitamins and Minerals Tablets",
"Calcium & Magnesium Plus Potassium & Zinc",
"Chela Calmag-300 Plus Zinc D3",
"Swiss One Multi Vit & Chel Min Tab",
"Chela Calmag-100 Plus Zinc D3",
"Vege 1 Daily Tab",
"Prevencal 300 + D A Croquer",
"Chelated Calcium and Magnesium Tab",
"Fem Time Tab",
"Chelamins Plus Tab",
"Maintain Multiple Vitamin & Minerals",
"Revitex Ampoules Et Comprimes",
"Multi II IV Vi Tab",
"Spectrum 2 Cap",
"Spd Tab",
"Cal & Mag Hvp Chel Plus C Potass & Zinc Tab",
"Men's Biomultiple Vitamin and Mineral Supplement",
"Women's Biomultiple Vitamin and Mineral Supplement",
"Complete One A Day Tab",
"Nitro Vites - Tab",
"Multi Plex I - Tab",
"Multi Plex II - Tab",
"Mega Plex III - Pck",
"Mega Plex III - Pck",
"Mega Plex IV - Pck",
"Mega Plex IV - Pck",
"K.L. Vitamin-mineral",
"Nutra-clear",
"Swical Extra-fort",
"Nutra Boost",
"Cal-mag Citrate Zinc & Vitamin D Tablets",
"Hvp Chelated Cal/mag With Zinc and Vitamins C and D",
"Osteoshield",
"Multi-actin",
"Calcor",
"Alkadrenergy Tablets",
"Calcium Complex High Grade",
"Vita Balance 2000",
"Vitaflex Dietary Suplement",
"B & J Formula Dietary Supplement",
"Mnps Formula Supplement",
"V & M Vitamin and Mineral Supplement",
"Osteo Formula",
"Liquid Calcium With Vitamin D",
"Tianshi Vital Powder III",
"Tianshi Vital Powder II",
"Tianshi Vital Powder I",
"Tianshi Calcium With Natural Source Vitamin D Tablets",
"Advanced B & T Formula",
"Kanga-V Multivitamins & Minerals",
"Global Vigen Recare Calcium",
"Protect Plus SO 60",
"M-Natal Plus",
"M-Natal Plus"
] |
[
"Q13936",
"P98194",
"P02585",
"P63316",
"Q01082",
"P04271",
"P20810",
"P49747",
"P19801",
"Q99584",
"P05187",
"P05109",
"P06702",
"P29034",
"P00450",
"P12644",
"P08493",
"Q8TAB3",
"O75340",
"P0DP23",
"P0DP24",
"P0DP25"
] |
[] |
[] |
[] |
DB00002
|
Cetuximab
|
Cetuximab is a recombinant chimeric human/mouse IgG1 monoclonal antibody that competitively binds to epidermal growth factor receptor (EGFR) and competitively inhibits the binding of epidermal growth factor (EGF).[A227973] EGFR is a member of the ErbB family of receptor tyrosine kinases found in both normal and tumour cells; it is responsible for regulating epithelial tissue development and homeostasis.[A228083] EGFR has been implicated in various types of cancer, as it is often overexpressed in malignant cells [A227973] and EGFR overexpression has been linked to more advanced disease and poor prognosis.[A227963] EGFR is often mutated in certain types of cancer and serves as a driver of tumorigenesis.[A228083] _In vitro_, cetuximab was shown to mediate anti-tumour effects in numerous cancer cell lines and human tumour xenografts.[A227963]
Approved by the FDA in February 2004 under the brand name ERBITUX, cetuximab is used for the treatment of head and neck cancer and metastatic, KRAS wild-type colorectal cancer, and metastatic colorectal cancer with a BRAF V600E mutation.[A227963,L39045] It has also been investigated in advanced colorectal cancer, EGFR-expressing non-small cell lung cancer (NSCLC), and unresectable squamous cell skin cancer.[L31418] Cetuximab is administered via intravenous infusion and is used as monotherapy or in combination with other chemotherapies, including platinum agents, radiation therapy, [leucovorin], [fluorouracil], and [irinotecan].[L30448]
|
liquid
|
Cetuximab indicated for the treatment of locally or regionally advanced squamous cell carcinoma of the head and neck in combination with radiation therapy. It is indicated for treating a recurrent locoregional disease or metastatic squamous cell carcinoma of the head and neck in combination with platinum-based therapy with fluorouracil. It is indicated for recurrent or metastatic squamous cell carcinoma of the head and neck progressing after platinum-based therapy.[L30448]
Cetuximab is also indicated for K-Ras wild-type, EGFR-expressing, metastatic colorectal cancer as determined by an FDA-approved test in combination with FOLFIRI, a chemotherapy combination that includes [leucovorin], [fluorouracil], and [irinotecan]; in combination with irinotecan in patients who are refractory to irinotecan-based chemotherapy; or as monotherapy in patients who have failed oxaliplatin- and irinotecan-based chemotherapy or who are intolerant to irinotecan.[L30448]
Additionally, cetuximab is also indicated for metastatic colorectal cancer that is BRAF V600E mutation-positive (as determined by an FDA-approved test) in combination with [encorafenib] but only after prior therapy.[L39045]
Cetuximab is not indicated for the treatment of Ras-mutant colorectal cancer or when the results of the Ras mutation tests are unknown.[L30448]
|
Cetuximab is an anticancer agent that works by inhibiting the growth and survival of epidermal growth factor receptor (EGFR)-expressing tumour cells with high specificity and higher affinity than epidermal growth factor (EGF) and transforming growth factor-alpha (TGF-α), which are natural ligands of EGFR.[L31418] Cetuximab works by inhibiting the growth and survival of EGFR-positive tumours.[A227963] _In vitro_, it promotes antibody-dependent cellular cytotoxicity (ADCC) against certain human tumour types. On the contrary, cetuximab does not exert its anti-tumour effects on human tumour xenografts lacking EGFR expression.[A227963, L30448]
Cetuximab potentiates the cytotoxic effects of chemotherapeutics and radiation therapy when used in combination.[L30448] In human tumour xenograft models in mice, cetuximab and irinotecan synergistically inhibited the growth of orthotopic anaplastic thyroid carcinoma xenografts _in vitro_ and _in vivo_. Cetuximab potentiated the _in vitro_ anti-proliferative and pro-apoptotic effect of irinotecan and achieved 93% _in vivo_ inhibition of tumour growth when combined with irinotecan, compared to 77% and 79% inhibition when cetuximab and irinotecan were used alone, respectively.[A227978]
|
The epidermal growth factor receptor (EGFR) is a transmembrane glycoprotein and a type I receptor tyrosine kinase expressed on both normal and malignant cells. It has been investigated as a therapeutic target for anticancer treatment, as it is often upregulated in cancer types, including head and neck, colon, and rectal cancers.[L30448] When activated by its ligand, EGFR undergoes a conformational change and dimerization to form homodimers or heterodimers with another member of the ErbB family of receptors. Dimerization of EGFR activates the intracellular tyrosine kinase region of EGFR and promotes autophosphorylation, initiating a series of downstream signalling cascades, including cell differentiation, proliferation, migration, angiogenesis, and apoptosis. This EGFR signalling pathway is often dysregulated in cancer cells, leading to aberrant cell growth and enhanced cell survival.[L31418]
Cetuximab is a monoclonal antibody that binds specifically to the EGFR on both normal and tumour cells to competitively inhibit the binding of epidermal growth factor (EGF) and other ligands that are produced by normal and tumour tissue epithelial cells.[A11, L30448] Upon binding to domain III of EGFR - which is the binding site for its growth factor ligands - cetuximab prevents the receptor from adopting an extended conformation and thereby inhibits EGFR activation, as well as phosphorylation and activation of receptor-associated kinases (MAPK, PI3K/Akt, Jak/Stat).[A11, A228078] Inhibition of the EGFR signalling pathway ultimately leads to inhibition of cell cycle progression, cell survival pathways, and tumour cell motility and invasion.[A227963] Cetuximab also induces cell apoptosis and decreases matrix metalloproteinase and vascular endothelial growth factor (VEGF) production.[A228078, L30448] _In vitro_, cetuximab was shown to inhibit tumour angiogenesis.[A227978] Binding of cetuximab to EGFR also results in internalization of the antibody-receptor complex, leading to an overall downregulation of EGFR expression.[A227973]
K-ras is a small G-protein downstream of EGFR that plays an important role in promoting the EGFR signalling cascade: in some malignant cells, K-ras can acquire activating mutations in exon 2 [L31418] and thus be continuously active regardless of EGFR regulation.[L30448] Since mutant Ras proteins can isolate the pathway from the effect of EGFR, K-Ras mutations can render EGFR inhibitors like cetuximab ineffective in exerting anti-tumour effects.[L30448, L31418] Cetuximab is thus only limited in its use for K-Ras wild-type, EGFR-expressing cancers.[L30448]
|
After administration of a 400 mg/m<sup>2</sup> initial dose followed by a 250 mg/m<sup>2</sup> weekly dose, the steady-state levels of cetuximab was reached by the third weekly infusion with mean peak and trough concentrations across studies ranging from 168 µg/mL to 235 µg/mL and 41 µg/mL to 85 µg/mL, respectively.[L30448] T<sub>max</sub> is about 3 hours.[A227963]
|
Like other monoclonal antibodies, cetuximab is expected to undergo lysosomal degradation by the reticuloendothelial system and protein catabolism by a target‐mediated disposition pathway.[A40006]
|
The intravenous LD<sub>50</sub> is > 300 mg/kg in mice and > 200 mg/kg in rats.[L31408] There is limited information on the overdose from cetuximab.
In clinical trials, cetuximab was associated with serious and fatal infusion reactions, cardiopulmonary arrest or sudden death, and serious dermatologic toxicities. Pulmonary toxicities, such as interstitial lung disease, interstitial pneumonitis with non-cardiogenic pulmonary edema, and exacerbation of pre-existing fibrotic lung disease have been reported.[L30448]
|
After administration of a 400 mg/m<sup>2</sup> initial dose followed by a 250 mg/m<sup>2</sup> weekly dose, the mean half-life for cetuximab was approximately 112 hours, with a range of 63 to 230 hours.[L30448]
|
There is no information available.
|
There is limited information available.
|
The volume of the distribution is about 2-3 L/m<sup>2</sup> and is independent of dose.[L30448]
|
In patients with recurrent and/or metastatic squamous cell carcinoma of the head and neck, the estimated clearance rate was 0.103 L/h.[A228003] At doses ranging from 200 to 400 mg/m<sup>2</sup>, complete saturation of systemic clearance was observed. In a population pharmacokinetic study, female patients had a 25% lower intrinsic cetuximab clearance than male patients, although there was no evidence of the need for dose modification based on sex.[A227963]
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved"
] |
[
"L01FE",
"L01F",
"L01",
"L"
] |
[
"Humans and other mammals"
] |
[] |
[
{
"approved": "1999-03-02",
"country": "Canada",
"expires": "2016-03-02",
"number": "1340417"
}
] |
Cetuximab | Cétuximab | Cetuximabum | 2.7.10.1 | ERBB | ERBB1 | HER1 | Proto-oncogene c-ErbB-1 | Receptor tyrosine-protein kinase erbB-1 | CD16-I | CD16B | Fc-gamma RIII | Fc-gamma RIII-beta | Fc-gamma RIIIb | FCG3 | FCGR3 | FcR-10 | FcRIII | FcRIIIb | IGFR3 | IgG Fc receptor III-1 | C1QG | CD16-II | CD16A | CD16a antigen | Fc-gamma RIII | Fc-gamma RIII-alpha | Fc-gamma RIIIa | FCG3 | FcgammaRIIIA | FCGR3 | FcR-10 | FcRIII | FcRIIIa | IGFR3 | IgG Fc receptor III-2 | IgG Fc receptor III-A | Fc-gamma RI | Fc-gamma RIA | FCG1 | FcgammaRIa | FCGR1 | FcRI | IGFR1 | IgG Fc receptor I | CD32 | CDw32 | Fc-gamma RII-a | Fc-gamma-RIIa | FCG2 | FCGR2A1 | FcRII-a | IGFR2 | IgG Fc receptor II-a
|
[
"Erbitux",
"Erbitux",
"Erbitux",
"Erbitux",
"Erbitux"
] |
[] |
[] |
[
"P00533",
"O75015",
"P02745",
"P02746",
"P02747",
"P08637",
"P12314",
"P12318"
] |
[] |
[] |
[] |
DB00003
|
Dornase alfa
|
Dornase alfa is a biosynthetic form of human deoxyribunuclease I (DNase I) enzyme. It is produced in genetically modified Chinese hamster ovary (CHO) cells using recombinant DNA technology. The 260-amino acid sequence of dornase alfa is identical to the endogenous human enzyme. Dornase alfa cleaves extracellular DNA to 5´-phosphodinucleotide and 5´-phosphooligonucleotide end products without affecting intracellular DNA. In individuals with cystic fibrosis, extracellular DNA, which is an extremely viscous anion, is released by degenerating leukocytes that accumulate during inflammatory responses to infections. Enzymatic breakdown of this extracellular DNA appears to reduce sputum viscosity and viscoelasticity.
|
liquid
|
Used as adjunct therapy in the treatment of cystic fibrosis.
|
Cystic fibrosis (CF) is a disease characterized by the retention of viscous purulent secretions in the airways. These thick secretions contribute both to reduced pulmonary function and to frequent pulmonary infection. Purulent pulmonary secretions of individuals with cystic fibrosis contain very high concentrations of extracellular DNA released by degenerating leukocytes that accumulate in response to these infections. Dornase alfa hydrolyzes the DNA in sputum of CF patients and reduces sputum viscosity and viscoelasticity. The enzyme does not appear to affect sputum in the absence of an inflammatory response to infection, nor does it affect the sputum of healthy individuals.
|
Dornase alfa is a biosynthetic form of human DNase I. The enzyme is involved in endonucleolytic cleavage of extracellular DNA to 5´-phosphodinucleotide and 5´-phosphooligonucleotide end products. It has no effect on intracellular DNA. Optimal activity is dependent on the presence of divalent cations such as calcium and magnesium. Extracellular DNA is a viscous anionic polymer and its breakdown appears to improve the viscosity and viscoelasticity of purulent sputum of individuals with CF, thus reducing airflow obstruction. Dornase alfa does not seem to have any effect on non-purulent sputum.
|
Studies in rats and monkeys after inhalation of dornase alfa shows very little systemic absorption (less than 15% for rats and less than 2% for monkeys). The results were also witnessed in patients. Dornase alfa is also associated with very low accumulation with no serum concentration greater than 10ng/mL observed no matter the dose administered. Bioavailability: mean sputum concentrations of dornase alfa can be measured after 15 minutes. Onset is achieved within 3 to 7 days. Peak concentrations are achieved after 9 days.
|
While no conclusive studies have yet been published, dornase alfa is expected to be metabolized by proteases in biofluids.
|
Adverse reactions occur at a frequency of < 1/1000 and are usually mild and transient in nature. Reported adverse effects include chest pain (pleuritic/non-cardiac), fever, dyspepsia, voice alteration (hoarseness), pharyngitis, dyspnea, laryngitis, rhinitis, decreased lung function, rash, urticaria, and conjunctivitis. There is no evidence of carcinogenic or mutagenic properties. The safety of dornase alfa has not been studied in pregnant women, nursing women and children under the age of 5 years old.
| null | null | null |
In studies in rats and monkeys, the initial volume of distribution is similar to the serum volume. Concentrations in sputum decline rapidly after inhalation.
|
Studies in rats indicate that, following aerosol administration, the disappearance half-life of dornase alfa from the lungs is 11 hours. In humans, sputum DNase levels declined below half of those detected immediately post-administration within 2 hours but effects on sputum rheology persisted beyond 12 hours.
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved"
] |
[
"R05CB",
"R05C",
"R05",
"R"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "3.21",
"description": "Lufyllin 200 mg tablet",
"unit": "tablet"
},
{
"cost": "3.84",
"description": "Lufyllin-gg tablet",
"unit": "tablet"
},
{
"cost": "3.99",
"description": "Lufyllin-GG 200-200 mg tablet",
"unit": "tablet"
},
{
"cost": "4.62",
"description": "Lufyllin-400 tablet",
"unit": "tablet"
},
{
"cost": "4.81",
"description": "Lufyllin 400 mg tablet",
"unit": "tablet"
},
{
"cost": "37.05",
"description": "Pulmozyme 1 mg/ml ampul",
"unit": "ml"
},
{
"cost": "77.06",
"description": "Pulmozyme 1 mg/ml Solution 2.5ml Plastic Container",
"unit": "plastic"
},
{
"cost": "0.6",
"description": "Lufyllin-GG 100-100 mg/15ml Elixir",
"unit": "ml"
}
] |
[
{
"approved": "2005-02-22",
"country": "Canada",
"expires": "2015-02-28",
"number": "2184581"
},
{
"approved": "2004-10-26",
"country": "Canada",
"expires": "2013-05-28",
"number": "2137237"
}
] |
Deoxyribonuclease (human clone 18-1 protein moiety) | Dornasa alfa | Dornase alfa | Dornase alfa, recombinant | Dornase alpha | Recombinant deoxyribonuclease (DNAse) | 3.1.21.1 | Deoxyribonuclease I | DNase I | DNL1 | DRNI
|
[
"Pulmozyme",
"Pulmozyme"
] |
[
"Viscozyme"
] |
[] |
[
"P24855"
] |
[] |
[] |
[] |
DB00004
|
Denileukin diftitox
|
Denileukin diftitox is an IL2-receptor-directed cytotoxin, is a recombinant DNA-derived fusion protein composed of the amino acid sequences for diphtheria toxin fragments A and B (Met<sub>1</sub>-Thr<sub>387</sub>)-His and the sequence for human interleukin-2 (IL-2; Ala<sub>1</sub>-Thr<sub>133</sub>).[L51254] It is designed to deliver diphtheria toxin into IL-2 receptor-expressing cancer cells to cause cell death.[A264349, L51254]
Denileukin diftitox was originally approved by the FDA in 1999 for the treatment of cutaneous T-cell lymphoma (CTCL),[A264339, L51264] making it the first fusion protein cytotoxin approved to treat a human disease in the US.[A264344] In 2014, it was withdrawn voluntarily from the market due to manufacturing issues; however, the biologics license application (BLA) for denileukin diftitox was resubmitted, and it was approved on August 8, 2024.[L51264]
|
liquid
|
Denileukin diftitox was previously indicated for the treatment of adult patients with persistent or recurrent cutaneous T-cell lymphoma (CTCL) whose malignant cells express the CD25 component of the IL-2 receptor.[L26381] It is also indicated for the treatment of adult patients with relapsed or refractory Stage I-III CTCL after at least one prior systemic therapy.[L51254]
|
Denileukin diftitox is an anticancer drug with cytocidal actions on cancer cells.[L51254] Denileukin diftitox demonstrated the ability to deplete immunosuppressive regulatory T lymphocytes (T<sub>regs</sub>) and antitumor activity through direct cytocidal action on IL-2R-expressing tumours.[L51254]
|
Denileukin diftitox is a fusion protein composed of truncated diphtheria toxin (DT), which is a cytocidal moiety, and the full-length sequence of interleukin-2 (IL-2), which acts as a ligand for the IL-2 receptor.[A264344] Denileukin diftitox is reported to bind to a high- or intermediate-affinity receptor.[A264344] Once the drug molecule binds to the IL-2 receptor, denileukin diftitox is internalized via receptor-mediated endocytosis in an acidified vesicle.[A15, A264344] After uptake into the cell, denileukin diftitox is proteolytically cleaved within the endosomes to release the enzymatically active portion of the DT. DT is translocated across the endosomal membrane into the cytosol to inhibit protein synthesis via ADP-ribosylation of elongation factor-2, ultimately resulting in cell death.
The fragment of DT is translocated across the endosomal membrane into the cytosol where it inhibits protein synthesis via ADP-ribosylation of elongation factor-2, resulting in cell death.[A264344, L51254]
|
Following a single dose of denileukin diftitox 9 mcg/kg via one-hour infusion in patients with CTCL, the geometric mean (coefficient of variation [CV]%) maximum serum concentration (C<sub>max</sub>) was 94.4 ng/mL (77%) and area under the concentration over time curve (AUC<sub>0-inf</sub>) was 20700 ng x min/L (60%) on the first day of the first administration cycle. There is no accumulation after repeated daily dosing.[L51254]
|
Denileukin diftitox is expected to be metabolized into small peptides by catabolic pathways.[L51254]
|
There is limited information regarding the acute toxicity (LD<sub>50</sub>) and overdose of denileukin diftitox.
|
The arithmetic mean (CV%) denileukin diftitox terminal half-life is 112 minutes (31%) on the first day of the first cycle.[L51254]
| null | null |
The geometric mean (CV%) volume of distribution of denileukin diftitox is 5.0 L (43%) on the first day of the first administration cycle.[L51254]
|
The geometric mean (CV%) clearance is 36.5 mL/min (73%) after the first dose of denileukin diftitox at the recommended dose level.[L51254]
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[
"L01XX",
"L01X",
"L01",
"L"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "878.4",
"description": "Ontak 150 mcg/ml vial",
"unit": "ml"
}
] |
[] |
DAB(SUB 389)IL2 | Denileukin | Denileukin diftitox | Interleukin-2/diptheria toxin fusion protein | N-L-METHIONYL-387-L-HISTIDINE-388-L-ALANINE-1-388-TOXIN (CORYNEBACTERIUM DIPHTHERIAE STRAIN C7) (388->2') PROTEIN WITH 2-133-INTERLEUKIN 2 (HUMAN CLONE PTIL2-21A) | N-MET-187-HIS-388-ALA-1-388-TOXIN (CORYNEBACTERIUM DIPHTHERIAE C7) WITH 1-133-INTERLEUKIN 2 | IL-2 receptor subunit alpha | IL-2-RA | IL-2R subunit alpha | IL2-RA | p55 | TAC antigen | High affinity IL-2 receptor subunit beta | IL-2 receptor subunit beta | IL-2R subunit beta | IL-2RB | IL15RB | Interleukin-15 receptor subunit beta | p70-75 | p75
|
[
"Ontak"
] |
[] |
[] |
[
"P01589",
"P14784"
] |
[] |
[] |
[] |
DB00005
|
Etanercept
|
Dimeric fusion protein consisting of the extracellular ligand-binding portion of the human 75 kilodalton (p75) tumor necrosis factor receptor (TNFR) linked to the Fc portion of human IgG1.[L14862,A216522] The Fc component of etanercept contains the CH2 domain, the CH3 domain and hinge region, but not the CH1 domain of IgG1. Etanercept is produced by recombinant DNA technology in a Chinese hamster ovary (CHO) mammalian cell expression system. It consists of 934 amino acids. It is used to treat or manage a variety of inflammatory conditions including rheumatoid arthritis (RA), ankylosing spondylitis (AS), and juvenile idiopathic poly-articular arthritis (JIA).
|
liquid
|
Etanercept is indicated for the treatment of moderately to severely active rheumatoid arthritis in adults and in chronic moderate to severe plaque psoriasis in patients 4 years of age and older.[L14862,L45523] It is also used to manage signs and symptoms of polyarticular idiopathic arthritis and Juvenile Psoriatic Arthritis in those aged 2 years and older. Etanercept is also used to manage the symptoms of psoriatic arthritis and ankylosing spondylitis.[L48526]
|
Etanercept binds specifically to tumor necrosis factor (TNF) and thereby modulates biological processes that are induced or regulated by TNF.[L14862,A216522] Such processes or molecules affected include the level of adhesion molecules expressed, as well as serum levels of cytokines and matrix metalloproteinases.
|
There are two distinct receptors for TNF (TNFRs), a 55 kilodalton protein (p55) and a 75 kilodalton protein (p75). The biological activity of TNF is dependent upon binding to either cell surface receptor (p75 or p55).[A216522] Etanercept is a dimeric soluble form of the p75 TNF receptor that can bind to two TNF molecules, thereby effectively removing them from circulation. Notably, etancerpt is only capable of binding to the active trimeric form of TNF as its binding site is located in the cleft between subunits.[A77626]TNF is a naturally occurring cytokine that is involved in normal inflammatory and immune responses.[A216522] Increased levels of TNF are found in tissues and fluids of those with rheumatoid arthritis, psoriatic arthritis, ankylosing spondylitis, and plaque psoriasis.
|
Population pharmacokinetic modeling in adults with RA, AS, or who were healthy showed a subcutaneous bioavailability of 56.9% with a Ka of 0.0223/h.[A215352] Another model in pediatric JIA patients showed an increased Ka of 0.05/h with a high mean interindividual variability of 215%.[A215357] Cmax after a single 25 mg subcutaneous dose of Enbrel is reported as 1.1 mcg/L with a Tmax of 69 h.[L14862] Cmax after repeated dosing is reported as 2.4 mcg/L in adult RA patients with a dosage of 25 mg twice weekly and 2.1 mcg in pediatric JIA patients with a dosage of 0.4 mg/kg twice weekly.
|
As etanercept is a fusion protein antibody, it is assumed to be metabolized via proteinases similarly to endogenous proteins.
| null |
Etanercept has a mean half-life of elimination of 102 hours in RA patients.[L14862] Population models have shown a mean half-life of 68 hours in healthy adults and 70.7-94.8 hours in pediatric JIA patients.[A215657,A215357]
|
No significant protein binding has been identified.
| null |
Population pharmacokinetic modeling predicts a total Vd of 5.49 L with a peripheral compartment of 1.24 L in adults with RA and an apparent Vd with subcutaneous administration in pediatric JIA patients of 7.88 L.[A215352,A215357]
|
Etanercept has a mean apparent clearance of 160 mL/h in RA patients.[L14862] Population models predict a mean apparent clearance of 132 mL/h in healthy adults and 0.0576 L/h in pediatric JIA patients.[A215657,A215357]
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[
"L04AB",
"L04A",
"L04",
"L"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "250.37",
"description": "Enbrel 25 mg kit",
"unit": "each"
},
{
"cost": "488.74",
"description": "Enbrel 50 mg/ml sureclick syr",
"unit": "syringe"
},
{
"cost": "1016.57",
"description": "Enbrel 4 25 mg Kit (1 Box = 1 Kit = Four 25 mg Vials)",
"unit": "box"
},
{
"cost": "2033.14",
"description": "Enbrel (1 Box = 1 Kit = Four 50 mg Syringes) 3.92ml Box",
"unit": "box"
},
{
"cost": "2033.14",
"description": "Enbrel SureClick (1 Box Contains Four 50 mg Prefilled Autoinjectors)",
"unit": "box"
}
] |
[
{
"approved": "2009-06-16",
"country": "Canada",
"expires": "2023-02-27",
"number": "2476934"
},
{
"approved": "2000-03-14",
"country": "Canada",
"expires": "2013-09-14",
"number": "2123593"
},
{
"approved": "2007-10-02",
"country": "United States",
"expires": "2024-07-29",
"number": "7276477"
}
] |
Etanercept | etanercept-szzs | etanercept-ykro | Recombinant human TNF | rhu TNFR:Fc | rhu-TNFR:Fc | TNFR-Immunoadhesin | Cachectin | TNF-a | TNF-alpha | TNFA | TNFSF2 | Tumor necrosis factor ligand superfamily member 2 | LT-alpha | TNF-beta | TNFB | TNFSF1 | Tumor necrosis factor ligand superfamily member 1 | Fc-gamma RI | Fc-gamma RIA | FCG1 | FcgammaRIa | FCGR1 | FcRI | IGFR1 | IgG Fc receptor I | CD32 | CDw32 | Fc-gamma RII-a | Fc-gamma-RIIa | FCG2 | FCGR2A1 | FcRII-a | IGFR2 | IgG Fc receptor II-a | CD32 | CDw32 | Fc-gamma RII-b | Fc-gamma-RIIb | FCG2 | FcRII-b | IGFR2 | IgG Fc receptor II-b | CD32 | CDw32 | Fc-gamma RII-c | Fc-gamma-RIIc | FCG2 | FcRII-c | IGFR2 | IgG Fc receptor II-c | CD16-II | CD16A | CD16a antigen | Fc-gamma RIII | Fc-gamma RIII-alpha | Fc-gamma RIIIa | FCG3 | FcgammaRIIIA | FCGR3 | FcR-10 | FcRIII | FcRIIIa | IGFR3 | IgG Fc receptor III-2 | IgG Fc receptor III-A | CD16-I | CD16B | Fc-gamma RIII | Fc-gamma RIII-beta | Fc-gamma RIIIb | FCG3 | FCGR3 | FcR-10 | FcRIII | FcRIIIb | IGFR3 | IgG Fc receptor III-1 | C1QG
|
[
"Benepali",
"Benepali",
"Benepali",
"Benepali",
"Benepali",
"Benepali",
"Benepali",
"Brenzys",
"Brenzys",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Enbrel",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Erelzi",
"Eticovo",
"Eticovo",
"Nepexto",
"Nepexto",
"Nepexto",
"Nepexto",
"Nepexto",
"Nepexto",
"Nepexto",
"Nepexto",
"Rymti",
"Rymti",
"Rymti",
"Truemed Group LLC"
] |
[
"Davictrel",
"Tunex"
] |
[
"Enbrel",
"Enbrel"
] |
[
"P01375",
"P01374",
"P12314",
"P12318",
"P31994",
"P31995",
"P08637",
"O75015",
"P02745",
"P02746",
"P02747"
] |
[] |
[] |
[] |
DB00006
|
Bivalirudin
|
Bivalirudin is a synthetic 20 residue peptide (thrombin inhibitor) which reversibly inhibits thrombin. Once bound to the active site, thrombin cannot activate fibrinogen into fibrin, the crucial step in the formation of thrombus. It is administered intravenously. Because it can cause blood stagnation, it is important to monitor changes in hematocrit, activated partial thromboplastin time, international normalized ratio and blood pressure.
|
solid
|
For treatment of heparin-induced thrombocytopenia and for the prevention of thrombosis. Bivalirudin is indicated for use in patients undergoing percutaneous coronary intervention (PCI), in patients at moderate to high risk acute coronary syndromes due to unstable angina or non-ST segment elevation in whom a PCI is planned.
|
Bivalirudin mediates an inhibitory action on thrombin by directly and specifically binding to both the catalytic site and anion-binding exosite of circulating and clot-bound thrombin. The action of bivalirudin is reversible because thrombin will slowly cleave the thrombin-bivalirudin bond which recovers the active site of thrombin.
|
Inhibits the action of thrombin by binding both to its catalytic site and to its anion-binding exosite. Thrombin is a serine proteinase that plays a central role in the thrombotic process, acting to cleave fibrinogen into fibrin monomers and to activate Factor XIII to Factor XIIIa, allowing fibrin to develop a covalently cross-linked framework which stabilizes the thrombus; thrombin also activates Factors V and VIII, promoting further thrombin generation, and activates platelets, stimulating aggregation and granule release.
|
Following intravenous administration, bivalirudin exhibits linear pharmacokinetics. The mean steady state concentration is 12.3 +/- 1.7mcg/mL after administration of an intravenous bolus of 1mg/kg followd by a 2.5mg/kg/hr intravenous infusion given over 4 hours.
|
80% proteolytic cleavage
|
Based on a study by Gleason et al., the no-observed-adverse-effect level (NOAEL) for bivalirudin, administered to rats via intravenous infusion over a 24-hour period, was 2000 mg/kg/24 h.
|
* Normal renal function: 25 min (in normal conditions)
* Creatinine clearance 10-29mL/min: 57min
* Dialysis-dependant patients: 3.5h
|
Other than thrombin and red blood cells, bivalirudin does not bind to plasma proteins.
|
Bivalirudin is cleared from plasma by a combination of renal mechanisms (20%) and proteolytic cleavage.
|
0.2L/kg
|
* 3.4 mL/min/kg [Normal renal function]
* 3.4 mL/min/kg [mild renal function]
* 2.7 mL/min/kg [moderate renal function]
* 2.8 mL/min/kg [severe renal function]
* 1 mL/min/kg [Dialysis-dependent patients]
|
Organic compounds
|
Organic Polymers
|
Polypeptides
| null |
[
"approved",
"investigational"
] |
[
"B01AE",
"B01A",
"B01",
"B"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "780.0",
"description": "Angiomax 250 mg vial",
"unit": "vial"
}
] |
[
{
"approved": "1993-03-23",
"country": "United States",
"expires": "2010-05-23",
"number": "5196404"
},
{
"approved": "1999-12-14",
"country": "Canada",
"expires": "2010-08-17",
"number": "2065150"
},
{
"approved": "2009-10-06",
"country": "United States",
"expires": "2029-01-27",
"number": "7598343"
},
{
"approved": "2009-09-01",
"country": "United States",
"expires": "2029-01-27",
"number": "7582727"
},
{
"approved": "2019-05-20",
"country": "United States",
"expires": "2039-05-20",
"number": "11903993"
},
{
"approved": "2019-05-20",
"country": "United States",
"expires": "2039-05-20",
"number": "11918622"
},
{
"approved": "2019-05-20",
"country": "United States",
"expires": "2039-05-20",
"number": "11992514"
}
] |
Bivalirudin | Bivalirudina | Bivalirudinum | 3.4.21.5 | Coagulation factor II | 1.11.2.2 | MPO
|
[
"Angiomax",
"Angiomax",
"Angiomax",
"Angiomax",
"Angiomax RTU",
"Angiox",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin",
"Bivalirudin for Injection",
"Bivalirudin for Injection",
"Bivalirudin for Injection",
"Bivalirudin for Injection",
"Bivalirudin in 0.9% Sodium Chloride",
"Bivalirudin in 0.9% Sodium Chloride",
"Bivalirudin Injection",
"Bivalirudin RTU"
] |
[
"Angiox",
"Hirulog"
] |
[] |
[
"P00734"
] |
[
"P05164"
] |
[] |
[] |
DB00007
|
Leuprolide
|
Leuprolide is a synthetic 9-residue peptide analogue of gonadotropin-releasing hormone (GnRH). Unlike the endogenous decapeptide GnRH, leuprolide contains a single D-amino acid (D-leucyl) residue, which helps to increase its circulating half-life from three to four minutes to approximately three hours.[A203222] As a GnRH mimic, leuprolide is capable of binding to the GnRH receptor (GnRHR) and inducing downstream modulation of both gonadotropin hormone and sex steroid levels. Prolonged activation of GnRHR results in significant downregulation of sex steroid levels, which is primarily responsible for the clinical efficacy of leuprolide in diverse conditions, including advanced prostate cancer, endometriosis, and central precocious puberty.[A203126, A203132]
Leuprolide was first approved in 1985 as a daily subcutaneous injection under the tradename Lupron™ by Abbvie Endocrine Inc.[L13850] Since this initial approval, various long-acting intramuscular and subcutaneous products have been developed such that patients can be dosed once every six months.[L13781, L13790] Leuprolide remains frontline therapy in all conditions for which it is indicated for use.
|
solid
|
Leuprolide is indicated for the treatment of advanced prostate cancer [L13781, L34415] and as palliative treatment of advanced prostate cancer.[L13790]
It is also used for the treatment of pediatric patients with central precocious puberty (CPP).[L13784, L13787]
In combination with oral [norethisterone] (also known as norethindrone), leuprolide is also indicated for the initial treatment of the symptoms of endometriosis.[L10310] Finally, in combination with iron supplementation, leuprolide is indicated for the preoperative hematological improvement of anemic patients with uterine leiomyomata (uterine fibroids).[L13814]
|
Leuprolide is a gonadotropin-releasing hormone (GnRH) analogue that functions as a GnRH receptor superagonist.[A203132, A203222] After an initial spike in GnRH-mediated steroidal production, including testosterone and estradiol, prolonged use results in a significant drop in circulating steroid levels, in line with those produced through other forms of androgen-deprivation therapy (ADT).[A203126, A203129, A203132] The corresponding hormonal/steroidal changes produce specific adverse effects in different patient populations.
In women undergoing treatment for endometriosis or uterine leiomyomata, careful consideration regarding pregnancy status is advised. The initial increase in estradiol levels may worsen symptoms such as pain and bleeding. Long-term use of leuprolide is associated with loss of bone mineral density. Patients co-administered with [norethisterone] may experience sudden vision loss, proptosis, diplopia, migraine, thrombophlebitis, and pulmonary embolism and may also be at higher risk of cardiovascular disease. Patients with a history of depression may experience severe recurrence of depressive symptoms.[L10310, L13814]
In men undergoing palliative treatment for advanced/metastatic prostate cancer, short-term spikes in testosterone levels may cause tumour flare and associated symptoms such as bone pain, hematuria, neuropathy, bladder and/or ureteral obstruction, and spinal cord compression. In addition, patients are at increased risk of developing hyperglycemia, diabetes, and cardiovascular disease, which may manifest through myocardial infarction, stroke, cardiac death, or prolonged QT/QTc interval. In addition, Leuprolide may cause convulsions and embryo-fetal toxicity.[L13781, L13790]
In pediatric patients undergoing treatment for central precocious puberty (CPP), the initial steroidal spike may be associated with increased clinical signs of puberty within 2-4 weeks of treatment initiation. In addition, leuprolide may cause convulsions and psychiatric symptoms, including irritability, impatience, aggression, anger, and crying.[L13784, L13787]
|
Gonadotropin-releasing hormone (GnRH) is a naturally occurring decapeptide that modulates the hypothalamic-pituitary-gonadal (HPG) axis. GnRH binds to corresponding receptors (GnRHRs) on the anterior pituitary gonadotropes, which in turn release luteinizing hormone (LH) and follicle-stimulating hormone (FSH); these, in turn, affect the downstream synthesis and release of the sex hormones testosterone, dihydrotestosterone, estrone, and estradiol.[A203126, A203132]
Despite the variety of conditions indicated for treatment with leuprolide, the mechanism of action underlying efficacy is the same in all cases. As a GnRHR agonist, leuprolide binds to and initially activates downstream LH and FSH release; this initial spike in gonadotropin levels is responsible for some of the adverse effects associated with treatment. After 2-4 weeks of treatment, continuous stimulation of GnRHR results in feedback inhibition and significant downregulation of LH, FSH, and their corresponding downstream effects, producing a therapeutic benefit. These effects are reversible upon treatment discontinuation.[A203126, A203129, A203132, A203222, L10310, L13781, L13784, L13787, L13790, L13814]
|
Leuprolide is typically administered as a single-dose long-acting formulation employing either microsphere or biodegradable solid depot technologies.[A203126] Regardless of the exact formulation and initial dose strength, the C<sub>max</sub> is typically achieved by 4-5 hours post-injection and displays large variability in the range of 4.6 - 212 ng/mL. Eventual steady-state kinetics are typically achieved by four weeks, with a narrower range of 0.1 - 2 ng/mL. No studies on the effects of food on absorption have been carried out.[L10310, L13781, L13784, L13787, L13790, L13814, L34415]
|
Radiolabeling studies suggest that leuprolide is primarily metabolized to inactive penta-, tri-, and dipeptide entities, which are likely further metabolized. It is expected that various peptidases encountered throughout systemic circulation are responsible for leuprolide metabolism.[L10310, L13781, L13784, L13787, L13790, L13814, L34415]
|
Leuprolide is considered extremely safe, with low dose-related toxicity and comparatively mild adverse effects.[A203126] Prostate cancer patients treated with leuprolide at doses as high as 20 mg/day for two years showed no additional adverse effects compared to those receiving 1 mg/day.[L13814]
|
Leuprolide has a terminal elimination half-life of approximately three hours.[L10310, L13781, L13784, L13787, L13790, L13814, L34415]
|
Leuprolide displays _in vitro_ binding to human plasma proteins between 43% and 49%.[L10310, L13781, L13784, L13787, L13790, L13814, L34415]
|
Following administration of 3.75 mg leuprolide depot suspension to three patients, less than 5% of the initial dose was recovered as unchanged or pentapeptide metabolite in the urine.[L10310, L13781, L13784, L13814]
|
Leuprolide has an apparent steady-state volume of distribution of 27 L following intravenous bolus administration to healthy males. The volume of distribution for indicated routes of subcutaneous or intramuscular injection has not been reported.[L10310, L13781, L13784, L13787, L13790, L13814, L34415]
|
Leuprolide administered as a 1 mg intravenous bolus in healthy males has a mean systemic clearance between 7.6 and 8.3 L/h.[L10310, L13781, L13784, L13787, L13790, L13814, L34415]
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[
"L02AE",
"L02A",
"L02",
"L",
"L02AE",
"L02A",
"L02",
"L"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "385.33",
"description": "Leuprolide 2wk 1 mg/0.2 ml kit",
"unit": "kit"
},
{
"cost": "400.74",
"description": "Leuprolide Acetate 1 mg/0.2ml Kit 2.8ml 2-Week Kit",
"unit": "box"
},
{
"cost": "493.2",
"description": "Eligard 7.5 mg syringe",
"unit": "syringe"
},
{
"cost": "594.37",
"description": "Lupron 2-wk 1 mg/0.2 ml kit",
"unit": "kit"
},
{
"cost": "1479.6",
"description": "Eligard 22.5 mg syringe",
"unit": "syringe"
},
{
"cost": "1972.8",
"description": "Eligard 30 mg syringe",
"unit": "syringe"
},
{
"cost": "2959.2",
"description": "Eligard 45 mg syringe",
"unit": "syringe"
}
] |
[
{
"approved": "2000-03-14",
"country": "United States",
"expires": "2016-12-13",
"number": "6036976"
},
{
"approved": "2014-12-30",
"country": "United States",
"expires": "2031-02-05",
"number": "8921326"
},
{
"approved": "2008-09-30",
"country": "United States",
"expires": "2019-01-13",
"number": "7429559"
},
{
"approved": "2014-08-26",
"country": "United States",
"expires": "2022-06-28",
"number": "8815801"
},
{
"approved": "1998-03-17",
"country": "United States",
"expires": "2017-01-30",
"number": "5728396"
},
{
"approved": "2000-12-05",
"country": "United States",
"expires": "2017-01-30",
"number": "6156331"
},
{
"approved": "2002-04-23",
"country": "United States",
"expires": "2018-12-17",
"number": "6375978"
},
{
"approved": "2001-05-22",
"country": "United States",
"expires": "2017-06-13",
"number": "6235712"
},
{
"approved": "2000-09-05",
"country": "United States",
"expires": "2018-07-24",
"number": "6113938"
},
{
"approved": "2000-09-26",
"country": "United States",
"expires": "2017-06-13",
"number": "6124261"
},
{
"approved": "2002-05-28",
"country": "United States",
"expires": "2017-01-30",
"number": "6395292"
},
{
"approved": "2000-10-17",
"country": "United States",
"expires": "2017-01-30",
"number": "6132420"
},
{
"approved": "1999-11-16",
"country": "United States",
"expires": "2017-01-30",
"number": "5985305"
},
{
"approved": "1999-08-03",
"country": "United States",
"expires": "2017-06-13",
"number": "5932547"
},
{
"approved": "2003-05-20",
"country": "United States",
"expires": "2018-10-28",
"number": "6565874"
},
{
"approved": "2004-08-10",
"country": "United States",
"expires": "2018-10-28",
"number": "6773714"
},
{
"approved": "2003-09-30",
"country": "United States",
"expires": "2020-03-27",
"number": "6626870"
},
{
"approved": "2016-03-15",
"country": "United States",
"expires": "2018-10-28",
"number": "9283282"
},
{
"approved": "2016-02-09",
"country": "United States",
"expires": "2018-10-28",
"number": "9254307"
},
{
"approved": "2013-07-16",
"country": "United States",
"expires": "2018-10-28",
"number": "8486455"
},
{
"approved": "2014-09-23",
"country": "United States",
"expires": "2020-11-13",
"number": "8840916"
},
{
"approved": "2013-06-25",
"country": "United States",
"expires": "2023-10-15",
"number": "8470359"
},
{
"approved": "2017-01-10",
"country": "United States",
"expires": "2020-11-13",
"number": "9539333"
},
{
"approved": "2018-03-13",
"country": "United States",
"expires": "2020-11-13",
"number": "9914802"
},
{
"approved": "2020-05-12",
"country": "United States",
"expires": "2027-01-16",
"number": "10646572"
},
{
"approved": "2017-02-21",
"country": "United States",
"expires": "2027-01-16",
"number": "9572857"
},
{
"approved": "2017-08-29",
"country": "United States",
"expires": "2027-01-16",
"number": "9744207"
},
{
"approved": "2017-10-17",
"country": "United States",
"expires": "2020-12-15",
"number": "9789064"
},
{
"approved": "2017-04-11",
"country": "United States",
"expires": "2028-03-22",
"number": "9617303"
},
{
"approved": "2019-01-01",
"country": "United States",
"expires": "2039-01-01",
"number": "11717555"
},
{
"approved": "2021-12-22",
"country": "United States",
"expires": "2041-12-22",
"number": "11771841"
},
{
"approved": "2021-12-22",
"country": "United States",
"expires": "2041-12-22",
"number": "11931559"
}
] |
Leuprorelin | Leuprorelina | Leuproreline | Leuprorelinum | GnRH receptor | GnRH-R | GRHR | GNRH | GRH | LHRH | Progonadoliberin I
|
[
"Camcevi",
"Camcevi",
"Camcevi",
"Camcevi",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Eligard",
"Fensolvi",
"Fensolvi",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate Depot",
"Leuprolide Acetate Injection",
"Lupaneta Pack",
"Lupaneta Pack",
"Lupron",
"Lupron",
"Lupron",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot",
"Lupron Depot Ped",
"Lupron Depot Ped",
"Lupron Depot Ped",
"Lupron Depot-PED",
"Lupron Depot-PED",
"Lupron Depot-PED",
"Lupron Depot-PED",
"Lupron Depot-PED",
"Lupron Depot-PED",
"Lupron Depot-PED",
"Viadur",
"Zeulide Depot",
"Zeulide Depot"
] |
[
"Camcevi",
"Leuplin",
"LeuProMaxx",
"Memryte",
"Prostap 3",
"Prostap SR"
] |
[
"Viadur",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Lupron Depot",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Lupaneta Pack",
"Lupaneta Pack",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate",
"Leuprolide Acetate"
] |
[
"P30968",
"P01148"
] |
[] |
[] |
[] |
DB00008
|
Peginterferon alfa-2a
|
Peginterferon alfa-2a is a form of recombinant interferon used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients [L852]. Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) resulting in less use of Peginterferon alfa-2a. Peginterferon alfa-2a is derived from the alfa-2a moeity of recombinant human interferon and acts by binding to human type 1 interferon receptors. Activation and dimerization of this receptor induces the body's innate antiviral response by activating the janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway. Use of Peginterferon alfa-2a is associated with a wide range of severe adverse effects including the aggravation and development of endocrine and autoimmune disorders, retinopathies, cardiovascular and neuropsychiatric complications, and increased risk of hepatic decompensation in patients with cirrhosis. The use of Peginterferon alfa-2a has largely declined since newer interferon-free antiviral therapies have been developed.
In a joint recommendation published in 2016, the American Association for the Study of Liver Diseases (AASLD) and the Infectious Diseases Society of America (IDSA) no longer recommend Peginterferon alfa-2a for the treatment of Hepatitis C [A19593]. Peginterferon alfa-2a was used alongside [DB00811] with the intent to cure, or achieve a sustained virologic response (SVR), after 48 weeks of therapy. SVR and eradication of HCV infection is associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of Hepatocellular Carcinoma, and reduced all-cause mortality [A19626].
Peginterferon alfa-2a is available as a fixed dose injector (tradename Pegasys) used for the treatment of chronic Hepatitis C. Approved in 2002 by the FDA, Pegasys is indicated for the treatment of HCV with [DB00811] or other antiviral drugs [FDA Label]. When combined together, Peginterferon alfa-2a and [DB00811] have been shown to achieve a SVR between 36% for genotype 1 and 59% for genotypes 2-6 after 48 weeks of treatment.
|
liquid
|
Peginterferon alfa-2a is indicated for the treatment of HCV in combination with other antiviral drugs in patients over 5 years of age with compensated liver disease [FDA Label]. May be used as a monotherapy in patients with contraindications to or significant intolerance to other anti-viral therapies.
Peginterferon alfa-2a is also indicated as a monotherapy for adult patients with HBeAg positive and HBeAg negative chronic hepatitis B infection who have compensated liver disease and evidence of viral replication and liver inflammation [FDA Label].
|
Peginterferon alfa-2a induces the body's innate antiviral response [FDA Label].
|
Peginterferon alfa-2a is derived from recombinant human interferon's alfa-2a moeity [FDA Label]. It binds to and activates human type 1 interferon receptors causing them to dimerize. This activates the JAK/STAT pathway. Activation of the JAK/STAT pathway increases expression of multiple genes in multiple tissues involved in the innate antiviral response.
|
Peginterferon alfa-2a reaches peak plasma concentration 72-96 hours after subcutaneous administration [FDA Label]. Trough concentrations at week 48 are approximately 2 fold higher than week 1. The peak to trough ratio at week 48 is 2.
| null |
Peginterferon alfa-2a may manifest neuropsychiatric complications include suicide, suicidal ideation, homicidal ideation, depression, relapse of drug addiction, and drug overdose [FDA Label]. Hypertension, supraventricular arrhythmias, chest pain, and myocardial infarction have been observed in patients using Peginterferon alfa-2a. Peginterferon alfa-2a may produce myelosuppression as well as the development or aggravation of autoimmune disorders including myositis, hepatitis, thrombotic thrombocytopenic purpura, idiopathic thrombocytopenic purpura, psoriasis, rheumatoid arthritis, interstitial nephritis, thyroiditis, and systemic lupus erythematosus. Peginterferon alfa-2a causes or aggravates hypothyroidism and hyperthyroidism. Hyperglycemia, hypoglycemia, and diabetes mellitus have been observed to develop in patients treated with Peginterferon alfa-2a. Peginterferon alfa-2a may decrease or produce loss of vision, retinopathy including macular edema, retinal artery or vein thrombosis, retinal hemorrhages and cotton wool spots, optic neuritis, papilledema and serous retinal detachment. Peginterferon mayy be related to increased ischemic and hemorrhagic cerebrovascular events. Patients with cirrhosis on Peginterferon alfa-2a are at risk of hepatic decompensation. Dyspnea, pulmonary infiltrates, pneumonia, bronchiolitis obliterans, interstitial pneumonitis, pulmonary hypertension and sarcoidosis may be induced or aggravated by Peginterferon alfa-2a. Serious and severe infections (bacterial, viral, or fungal) have been reported during treatment with Peginterferon alfa-2a. Ulcerative and hemorrhagic/ischemic colitis have been observed within 12 weeks of starting Peginterferon alfa-2a treatment. Pancreatitis and peripheral nephropathy have also been reported. Peginterferon alfa-2a is associated with growth inhibition in pediatric patients. Use of Peginterferon alfa-2a while pregant may result in delopmental abnormalities or death of the fetus.
|
The mean terminal half-life of peginterferon alfa-2a is 164 in a range of 84-353 hours [FDA Label].
| null | null | null |
The mean systemic clearance of peginterferon alfa-2a is 94 milliliters per hour [FDA Label].
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[
"L03AB",
"L03A",
"L03",
"L",
"L03AB",
"L03A",
"L03",
"L"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "642.64",
"description": "Pegasys 180 mcg/ml vial",
"unit": "ml"
},
{
"cost": "2533.2",
"description": "Pegasys 180 mcg/0.5 ml conv.pk",
"unit": "each"
},
{
"cost": "2634.53",
"description": "Pegasys (1 Kit = Four 180 mcg/ml Vials Prefilled Syringes) Box",
"unit": "box"
}
] |
[
{
"approved": "2009-06-30",
"country": "Canada",
"expires": "2017-04-23",
"number": "2203480"
},
{
"approved": "2000-10-03",
"country": "Canada",
"expires": "2016-03-26",
"number": "2172664"
}
] |
PEG-IFN alfa-2A | PEG-Interferon alfa-2A | Peginterferon alfa-2a | Pegylated Interfeaon alfa-2A | Pegylated interferon alfa-2a | Pegylated interferon alpha-2a | Pegylated-interferon alfa 2a | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | Interferon alpha binding protein | Type I interferon receptor 2 | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member 1 | IFN-alpha/beta receptor 1 | IFN-R-1 | IFNAR | Type I interferon receptor 1 | 1.14.14.1 | Cholesterol 25-hydroxylase | CYPIA2 | Cytochrome P(3)450 | Cytochrome P450 4 | Cytochrome P450-P3 | Hydroperoxy icosatetraenoate dehydratase
|
[
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys",
"Pegasys Rbv",
"Pegasys Rbv"
] |
[] |
[
"Pegasys Rbv",
"Pegasys Rbv"
] |
[
"P48551",
"P17181"
] |
[
"P05177"
] |
[] |
[] |
DB00009
|
Alteplase
|
Alteplase is a recombinant tissue plasminogen activator (rt-PA) used as a thrombolytic agent.[L43125] It cleaves plasminogen to form plasmin, an enzyme involved in the degradation of fibrin clots. In the absence of fibrin, the alteplase-mediated conversion of plasminogen is limited, thanks to the high affinity between alteplase and fibrin.[A252330,L43125] Alteplase is a purified glycoprotein of 527 amino acids expressed in Chinese hamster ovary (CHO) cells.[A252345,L43125] It was first approved by the FDA in 1987 for the management of thromboembolic disease, including acute myocardial infarction (AMI).[A252270] The use of alteplase to manage AMI has decreased thanks to the availability of safer treatments such as angioplasty and stenting. However, its use for the treatment of acute ischemic stroke (AIS) has increased over the years.[A252340] New thrombolytic agents derived from tissue plasminogen activator, such as [desmoteplase], [tenecteplase] and [reteplase], have also been developed.[A252270,A252345] Alteplase is also available as Cathflo Activase (intracatheter instillation) for the restoration of function to central venous access devices.[L34864]
|
liquid
|
Alteplase is indicated for the treatment of acute ischemic stroke (AIS) and for use in acute myocardial infarction (AMI) for the reduction of mortality and incidence of heart failure. Alteplase is also indicated for the lysis of acute massive pulmonary embolism, defined as acute pulmonary emboli obstructing blood flow to a lobe or multiple lung segments, and acute pulmonary emboli accompanied by unstable hemodynamics.[L43125]
|
Alteplase binds to fibrin and plasminogen. Alteplase specificity for fibrin is achieved thanks to its high affinity for lysine residues. Also, it can bind plasminogen via loop structures called kringles, stabilized by three disulphide linkages similar to the ones in plasminogen. The specificity of alteplase for plasminogen bound to fibrin allows this drug to act in a clot- or fibrin-specific manner, leading to low concentrations of circulating plasmin and a lower risk of hemorrhagic transformation.[A252270,A252330]
In patients with acute myocardial infarction, alteplase reduces fibrinogen levels 3 to 6 hours after treatment. In patients with acute ischemic stroke, patients treated with alteplase have a significantly higher resolution of hyperdense artery sign, a marker of clot formation in the proximal middle cerebral artery, compared to those treated with placebo.[A252330] The use of alteplase increases the risk of bleeding and thromboembolic events. Rare cases of cholesterol embolism have also been reported.[L43125]
|
Alteplase is a recombinant tissue plasminogen activator (rt-PA) that converts plasminogen to plasmin in a fibrin-dependent process. In the absence of fibrin, alteplase converts a limited amount of plasminogen. However, in the presence of fibrin clots, alteplase binds to fibrin and cleaves the arginine-valine bond at positions 560 and 561 of plasminogen, converting it into its active form, plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus and promotes clot dissolution.[A252270] Alteplase initiates local fibrinolysis with limited systemic proteolysis.[L43125]
|
Healthy volunteers with a baseline endogenous tissue plasminogen activator (t-PA) of 3.3 ng/ml had a 290-fold increase in baseline concentrations after receiving alteplase at an infusion rate of 0.25 mg/kg for 30 min; with an infusion rate of 0.5 mg/kg, a 550-fold increase was observed.[A252270] Acute myocardial infarction patients (n=12) given 10 mg of alteplase in a 2-minute infusion reached a peak plasma concentration of 3310 ng/ml. This was followed by 50 mg of alteplase in 1 h and 30 mg in 1.5 h, resulting in steady-state plasma levels of 2210 ng/ml and 930 ng/ml, respectively.[A252285]
|
Alteplase is mainly metabolized by the liver. The carbohydrate and polypeptide domains of alteplase interact with hepatic glycoprotein receptors, leading to receptor-mediated endocytosis.[A252270] _In vivo_ studies suggest that alteplase follows zero-order kinetics, meaning that its metabolism is saturable at higher plasma concentrations.[A252270]
|
Toxicity information regarding alteplase is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as risk of bleeding and thromboembolic events.[L43125] Symptomatic and supportive measures are recommended. The carcinogenic potential of alteplase or its effect on fertility have not been evaluated. _In vivo_ studies evaluating tumorigenicity and _in vitro_ studies evaluating mutagenicity were negative.[L43125] It has been estimated that the acute oral and dermal toxicity of alteplase is above 5,000 mg/kg.[L43175]
|
Alteplase has an initial half-life of less than 5 minutes in patients with acute myocardial infarction (AMI). The dominant initial plasma half-life of the 3-hour and the accelerated regimens for AMI are similar.[L43125]
|
Not available.
|
In healthy volunteers, more than 80% of alteplase is eliminated through urine 18 hours after administration.[A252270]
|
The initial volume of distribution approximates plasma volume.[L43125] The average volume of distribution of the central compartment goes from 3.9 to 4.3 L, and the volume of distribution at steady state goes from 7.2 to 12 L.[A252270]
|
Alteplase has a plasma clearance between 380 and 570 mL/min.[L43125]
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[
"B01AD",
"B01A",
"B01",
"B",
"S01XA",
"S01X",
"S01",
"S"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "106.33",
"description": "Cathflo activase 2 mg vial",
"unit": "vial"
},
{
"cost": "2389.85",
"description": "Activase 50 mg vial",
"unit": "vial"
},
{
"cost": "4779.71",
"description": "Activase 100 mg vial",
"unit": "vial"
}
] |
[] |
Alteplasa | Alteplase | Alteplase (genetical recombination) | Alteplase, recombinant | Alteplase,recombinant | Plasminogen activator (human tissue-type protein moiety) | rt-PA | t-PA | t-plasminogen activator | Tissue plasminogen activator | Tissue plasminogen activator alteplase | Tissue plasminogen activator, recombinant | tPA | 3.4.21.7 | Endothelial plasminogen activator inhibitor | PAI | PAI-1 | PAI1 | PLANH1 | Serpin E1
|
[
"Activase",
"Activase",
"Activase RT-PA",
"Activase RT-PA",
"Activase RT-PA Inj",
"Activase RT-PA Inj",
"Activase RT-PA Inj",
"Cathflo",
"Cathflo Activase",
"Lysatec RT - Pa"
] |
[] |
[
"Lysatec RT - Pa",
"Activase RT-PA",
"Activase RT-PA"
] |
[
"P00747",
"P02671",
"P02679",
"P05121"
] |
[] |
[] |
[] |
DB00010
|
Sermorelin
|
Sermorelin acetate is the acetate salt of an amidated synthetic 29-amino acid peptide (GRF 1-29 NH 2 ) that corresponds to the amino-terminal segment of the naturally occurring human growth hormone-releasing hormone (GHRH or GRF) consisting of 44 amino acid residues
|
liquid
|
For the treatment of dwarfism, prevention of HIV-induced weight loss
|
Sermorelin is used in the treatment of children with growth hormone deficiency or growth failure. Geref increases plasma growth hormone (GH) concentration by stimulating the pituitary gland to release GH. Geref is similar to the full-length native hormone (44 residues) in its ability to stimulate GH secretion in humans.
|
Sermorelin binds to the growth hormone releasing hormone receptor and mimics native GRF in its ability to stimulate growth hormone secretion.
| null | null | null |
11-12 min
| null | null | null | null |
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"withdrawn"
] |
[
"V04CD",
"V04C",
"V04",
"V",
"H01AC",
"H01A",
"H01",
"H"
] |
[
"Humans and other mammals"
] |
[] |
[] |
Sermorelin | GHRH receptor | GRF receptor | GRFR | Growth hormone-releasing factor receptor
|
[] |
[
"Geref"
] |
[] |
[
"Q02643"
] |
[] |
[] |
[] |
DB00011
|
Interferon alfa-n1
|
Interferon alfa-n1 consists of purified, natural (n is for natural) alpha interferon subtypes, at least two of which are glycosylated. This differs from recombinant alpha interferons, which are individual non-glycosylated proteins produced from individual alpha interferon genes.
|
liquid
|
For the treatment of venereal or genital warts caused by the Human Papiloma Virus.
|
Upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also induce the synthesis of several key antiviral mediators, including 2'-5' oligoadenylate synthetase (2'-5' A synthetase) and protein kinase R.
|
Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers and activators of transcription)which dimerize and activate multiple (~100) immunomodulatory and antiviral proteins. Interferon alpha binds less stably to type I interferon receptors than interferon beta.
| null | null | null |
1.2 hours (mammalian reticulocytes, in vitro); >20 hours (yeast, in vivo); >10 hours (Escherichia coli, in vivo).
| null | null | null | null |
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[
"L03AB",
"L03A",
"L03",
"L"
] |
[
"Humans and other mammals"
] |
[] |
[] |
Interferon alfa-n1 | Interferon alpha-n1 (INS) | WELL-FERON | WELLFERON | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member 1 | IFN-alpha/beta receptor 1 | IFN-R-1 | IFNAR | Type I interferon receptor 1 | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | Interferon alpha binding protein | Type I interferon receptor 2 | 1.14.14.1 | Cholesterol 25-hydroxylase | CYPIA2 | Cytochrome P(3)450 | Cytochrome P450 4 | Cytochrome P450-P3 | Hydroperoxy icosatetraenoate dehydratase
|
[
"Wellferon Inj 10 000 000unit/ml",
"Wellferon Inj 3000000unit/ml"
] |
[
"Wellferon"
] |
[] |
[
"P17181",
"P48551"
] |
[
"P05177"
] |
[] |
[] |
DB00012
|
Darbepoetin alfa
|
Human erythropoietin with 2 aa substitutions to enhance glycosylation (5 N-linked chains), 165 residues (MW=37 kD). Produced in Chinese hamster ovary (CHO) cells by recombinant DNA technology.
|
liquid
|
For the treatment of anemia (from renal transplants or certain HIV treatment)
|
Darbepoetin alfa is used in the treatment of anemia. It is involved in the regulation of erythrocyte differentiation and the maintenance of a physiological level of circulating erythrocyte mass.
|
Darbepoetin alfa stimulates erythropoiesis by the same mechanism as endogenous erythropoietin. Erythropoietin interacts with
progenitor stem cells to increase red cell production. Binding of erythropoietin to the erythropoietin receptor leads to receptor dimerization, which facilitates activation of JAK-STAT signaling pathways within the cytosol. Activated STAT (signal transducers and activators of transcription) proteins are then translocated to the nucleus where they serve as transcription factors which regulate the activation of specific genes involved in cell division or differentiation.
| null | null | null | null | null | null | null | null |
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[
"B03XA",
"B03X",
"B03",
"B"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "156.36",
"description": "Aranesp 25 mcg/ml vial",
"unit": "ml"
},
{
"cost": "162.61",
"description": "Aranesp (Albumin Free) 25 mcg/ml vial",
"unit": "vial"
},
{
"cost": "250.2",
"description": "Aranesp 40 mcg/ml vial",
"unit": "ml"
},
{
"cost": "375.3",
"description": "Aranesp 60 mcg/ml vial",
"unit": "ml"
},
{
"cost": "390.31",
"description": "Aranesp (Albumin Free) 60 mcg/ml vial",
"unit": "vial"
},
{
"cost": "625.44",
"description": "Aranesp 100 mcg/ml vial",
"unit": "ml"
},
{
"cost": "1250.88",
"description": "Aranesp 200 mcg/ml vial",
"unit": "ml"
},
{
"cost": "1876.32",
"description": "Aranesp 300 mcg/ml vial",
"unit": "ml"
},
{
"cost": "1951.37",
"description": "Aranesp (Albumin Free) 300 mcg/ml vial",
"unit": "vial"
},
{
"cost": "2601.83",
"description": "Aranesp (Albumin Free) 100 mcg/0.5ml Solution (1 Box = Four 0.5ml Syringes)",
"unit": "box"
},
{
"cost": "2601.83",
"description": "Aranesp (Albumin Free) 100 mcg/ml Solution Four 1ml Vials Per Box",
"unit": "box"
},
{
"cost": "3902.75",
"description": "Aranesp (Albumin Free) 150 mcg/0.75ml Solution (1 Box = Four 0.75ml Vials)",
"unit": "box"
}
] |
[
{
"approved": "2003-03-18",
"country": "Canada",
"expires": "2010-10-15",
"number": "2165694"
},
{
"approved": "2002-11-05",
"country": "Canada",
"expires": "2014-08-16",
"number": "2147124"
}
] |
Darbepoetin | Darbepoetin alfa | Darbepoetin alfa,recombinant | Darbepoetina alfa | EPO-R
|
[
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp",
"Aranesp -(hsa-free)",
"Aranesp -(hsa-free)",
"Aranesp -(hsa-free)",
"Aranesp -(hsa-free)",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo",
"Nespo"
] |
[] |
[] |
[
"P19235"
] |
[] |
[] |
[] |
DB00013
|
Urokinase
|
Urokinase is an endogenous peptide that is cleaved in the presence of plasmin between lysine 158 and isoleucine 159 to yield active urokinase.[A191943] Urokinase remains connected between these 2 chains by a sulfhydryl bond.[A191943]
Urokinase was granted FDA approval on 16 January 1978.[L12138]
|
liquid
|
In Canada, urokinase is indicated for lysis of acute massive pulmonary emboli, acute thrombi obstructing coronary arteries, occlusive thromboemboli in peripheral arteries and grafts, and restoration of patency to intravenous catheters.[L12141]
|
Urokinase is a serine protease that activates plasminogen to an active fibrinolytic protease.[A191928] The duration of action is short due to the short half life.[L12138] Patients should be counselled regarding the risk of bleeding, anaphylaxis, infusion reactions, and cholesterol embolization.[L12138
|
Urokinase is a serine protease.[A191928] It cleaves plasminogen to form the active fibrinolytic protease, plasmin.[A191928]
|
Urokinase is delivered intravenously, so the bioavailability is high.
|
Because urokinase is a protein, it is expected to be metabolized by proteases to smaller proteins and amino acids.
|
Patients experiencing an overdose may present with bleeding.[L12141] Treat patients with symptomatic and supportive measures which may include application of local pressure, administration of whole blood or plasma, and administration of aminocaproic acid.[L12141]
|
Urokinase has a half life of 12.6±6.2 minutes.[L12138]
|
Data regarding the protein binding of urokinase in plasma is not readily available.
|
Urokinase is eliminated in the bile and urine.[L12138]
|
The volume of distribution of urokinase is 11.5L.[L12138]
|
Data regarding the clearance of urokinase is not readily available.
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational",
"withdrawn"
] |
[
"B01AD",
"B01A",
"B01",
"B"
] |
[
"Humans and other mammals"
] |
[] |
[] |
Kinase (enzyme-activating), uro-urokinase | TCUK | Tissue culture urokinase | Two-chain urokinase | Urochinasi | Urokinase | Urokinasum | Uroquinasa | 3.4.21.7 | MO3 | Monocyte activation antigen Mo3 | U-PAR | UPAR | Endothelial plasminogen activator inhibitor | PAI | PAI-1 | PAI1 | PLANH1 | Serpin E1 | Monocyte Arg-serpin | PAI-2 | PAI2 | Placental plasminogen activator inhibitor | PLANH2 | Serpin B2 | Urokinase inhibitor | Acrosomal serine protease inhibitor | PAI-3 | PAI3 | PCI | PLANH3 | Plasminogen activator inhibitor 3 | PROCI | Protein C inhibitor | Serpin A5 | Glycoprotein 330 | gp330 | LRP-2 | Megalin | 3.4.21.109 | Matriptase | Membrane-type serine protease 1 | MT-SP1 | Prostamin | PRSS14 | Serine protease 14 | Serine protease TADG-15 | SNC19 | TADG15 | Tumor-associated differentially-expressed gene 15 protein | Entactin | NID | NID-1 | 3.4.24.65 | HME | Macrophage elastase | Matrix metalloproteinase-12 | ME | MME | MMP-12
|
[
"Kinlytic",
"Kinlytic (urokinase for Injection)",
"Kinlytic Open-cath"
] |
[
"Abbokinase"
] |
[] |
[
"P00747",
"Q03405",
"P05121",
"P05120",
"P05154",
"P98164",
"Q9Y5Y6",
"P14543"
] |
[
"P39900"
] |
[] |
[] |
DB00014
|
Goserelin
|
Goserelin is a synthetic hormone. In men, it stops the production of the hormone testosterone, which may stimulate the growth of cancer cells. In women, goserelin decreases the production of the hormone estradiol (which may stimulate the growth of cancer cells) to levels similar to a postmenopausal state. When the medication is stopped, hormone levels return to normal.
|
solid
|
Goserelin is indicated for:
- Use in combination with flutamide for the management of locally confined carcinoma of the prostate
- Palliative treatment of advanced carcinoma of the prostate
- The management of endometriosis
- Use as an endometrial-thinning agent prior to endometrial ablation for dysfunctional uterine bleeding
- Use in the palliative treatment of advanced breast cancer in pre- and perimenopausal women
|
The pharmacokinetics of goserelin have been determined in both male and female healthy volunteers and patients. In these studies, goserelin was administered as a single 250µg (aqueous solution) dose and as a single or multiple 3.6 mg depot dose by subcutaneous route.
|
Goserelin is a synthetic decapeptide analogue of LHRH. Goserelin acts as a potent inhibitor of pituitary gonadotropin secretion when administered in the biodegradable formulation. The result is sustained suppression of LH and serum testosterone levels.
|
Inactive orally, rapidly absorbed following subcutaneous administration.
|
Hepatic
|
No experience of overdosage from clinical trials.
|
4-5 hours
|
27.3%
|
Clearance of goserelin following subcutaneous administration of a radiolabeled solution of goserelin was very rapid and occurred via a combination of hepatic and urinary excretion. More than 90% of a subcutaneous radiolabeled solution formulation dose of goserelin was excreted in urine.
|
* 44.1 ± 13.6 L [subcutaneous administration of 250 mcg]
|
* 121 +/- 42.4 mL/min [prostate cancer with 10.8 mg depot]
|
Organic compounds
|
Organic acids and derivatives
|
Carboxylic acids and derivatives
|
Amino acids, peptides, and analogues
|
[
"approved"
] |
[
"L02AE",
"L02A",
"L02",
"L"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "451.19",
"description": "Zoladex 3.6 mg implant syringe",
"unit": "syringe"
},
{
"cost": "1380.65",
"description": "Zoladex 10.8 mg implant syringe",
"unit": "syringe"
}
] |
[
{
"approved": "2006-10-10",
"country": "United States",
"expires": "2022-04-13",
"number": "7118552"
},
{
"approved": "2007-05-22",
"country": "United States",
"expires": "2022-04-09",
"number": "7220247"
},
{
"approved": "2009-03-10",
"country": "United States",
"expires": "2021-02-26",
"number": "7500964"
}
] |
Goserelin | Goserelina | LCGR | LGR2 | LH/CG-R | LHR | LHRHR | LSH-R | Luteinizing hormone receptor | GNRH | GRH | LHRH | Progonadoliberin I | GnRH receptor | GnRH-R | GRHR
|
[
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex",
"Zoladex LA"
] |
[] |
[] |
[
"P22888",
"P01148",
"P30968"
] |
[] |
[] |
[] |
DB00015
|
Reteplase
|
Human tissue plasminogen activator, purified, glycosylated, 355 residues purified from CHO cells. Retavase is considered a "third-generation" thrombolytic agent, genetically engineered to retain and delete certain portions of human tPA. Retavase is a deletion mutein of human tPA formed by deleting various amino acids present in endogenous human tPA. Retavase contains 355 of the 527 amino acids of native human tPA (amino acids 1-3 and 176-527), and retains the activity-related kringle-2 and serine protease domains of human tPA. Three domains are deleted from retavase - kringle-1, finger, and epidermal growth factor (EGF).
|
liquid
|
For lysis of acute pulmonary emboli, intracoronary emboli, and management of myocardial infarction.
|
Reteplase cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action. This helps eliminate blood clots or arterial blockages that cause myocardial infarction.
|
Reteplase binds to fibrin rich clots via the fibronectin finger-like domain and the Kringle 2 domain. The protease domain then cleaves the Arg/Val bond in plasminogen to form plasmin. Plasmin in turn degrades the fibrin matrix of the thrombus, thereby exerting its thrombolytic action.
| null | null | null | null | null | null | null | null |
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[
"B01AD",
"B01A",
"B01",
"B"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "2605.93",
"description": "Retavase vial half-kit",
"unit": "vial"
}
] |
[
{
"approved": "2007-12-18",
"country": "Canada",
"expires": "2012-04-15",
"number": "2107476"
}
] |
Human t-PA (residues 1-3 and 176-527) | Reteplasa | Reteplase | Reteplase, recombinant | Reteplase,recombinant | 3.4.21.7 | Endothelial plasminogen activator inhibitor | PAI | PAI-1 | PAI1 | PLANH1 | Serpin E1
|
[
"Rapilysin",
"Retavase",
"Retavase",
"Retavase",
"Retavase",
"Retavase"
] |
[] |
[] |
[
"P00747",
"P02671",
"P05121"
] |
[] |
[] |
[] |
DB00016
|
Erythropoietin
|
Erythropoietin (EPO) is a growth factor produced in the kidneys that stimulates the production of red blood cells. It works by promoting the division and differentiation of committed erythroid progenitors in the bone marrow [FDA Label]. Epoetin alfa (Epoge) was developed by Amgen Inc. in 1983 as the first rhEPO commercialized in the United States, followed by other alfa and beta formulations. Epoetin alfa is a 165-amino acid erythropoiesis-stimulating glycoprotein produced in cell culture using recombinant DNA technology and is used for the treatment of patients with anemia associated with various clinical conditions, such as chronic renal failure, antiviral drug therapy, chemotherapy, or a high risk for perioperative blood loss from surgical procedures [FDA Label]. It has a molecular weight of approximately 30,400 daltons and is produced by mammalian cells into which the human erythropoietin gene has been introduced. The product contains the identical amino acid sequence of isolated natural erythropoietin and has the same biological activity as the endogenous erythropoietin. Epoetin alfa biosimilar, such as Retacrit (epoetin alfa-epbx or epoetin zeta), has been formulated to allow more access to treatment options for patients in the market [L2784]. The biosimilar is approved by the FDA and EMA as a safe, effective and affordable biological product and displays equivalent clinical efficacy, potency, and purity to the reference product [A7504]. Epoetin alfa formulations can be administered intravenously or subcutaneously.
|
liquid
|
Indicated in adult and paediatric patients for the:
- treatment of anemia due to Chronic Kidney Disease (CKD) in patients on dialysis and not on dialysis.
- treatment of anemia due to zidovudine in patients with HIV-infection.
- treatment of anemia due to the effects of concomitant myelosuppressive chemotherapy, and upon initiation, there is a minimum of two additional months of planned chemotherapy.
- reduction of allogeneic RBC transfusions in patients undergoing elective, noncardiac, nonvascular surgery.
|
Erythropoietin and epoetin alfa are involved in the regulation of erythrocyte differentiation and the maintenance of a physiological level of circulating erythrocyte mass. It is reported to increase the reticulocyte count within 10 days of initiation, followed by increases in the RBC count, hemoglobin, and hematocrit, usually within 2 to 6 weeks [F85]. Depending on the dose administered, the rate of hemoglobin increase may vary. In patients receiving hemodialysis, a greater biologic response is not observed at doses exceeding 300 Units/kg 3 times weekly [F85].
Epoetin alfa serves to restore erythropoietin deficiency in pathological and other clinical conditions where normal production of erythropoietin is impaired or compromised. In anemic patients with chronic renal failure (CRF), administration with epoetin alfa stimulated erythropoiesis by increasing the reticulocyte count within 10 days, followed by increases in the red cell count, hemoglobin, and hematocrit, usually within 2 to 6 weeks [FDA Label]. Epoetin alfa was shown to be effective in increasing hematocrit in zidovudine-treated HIV-infected patients and anemic cancer patients undergoing chemotherapy [FDA Label].
|
Erythropoietin or exogenous epoetin alfa binds to the erythropoietin receptor (EPO-R) and activates intracellular signal transduction pathways [A33079]. The affinity (Kd) of EPO for its receptor on human cells is ∼100 to 200 pM [A33080]. Upon binding to EPO-R on the surface of erythroid progenitor cells, a conformational change is induced which brings EPO-R-associated Janus family tyrosine protein kinase 2 (JAK2) molecules into close proximity. JAK2 molecules are subsequently activated via phosphorylation, then phosphorylate tyrosine residues in the cytoplasmic domain of the EPO-R that serve as docking sites for Src homology 2-domain-containing intracellular signaling proteins [A33079]. The signalling proteins include STAT5 that once phosphorylated by JAK2, dissociates from the EPO-R, dimerizes, and translocates to the nucleus where they serve as transcription factors to activate target genes involved in cell division or differentiation, including the apoptosis inhibitor Bcl-x [A33079]. The inhibition of apoptosis by the EPO-activated JAK2/STAT5/Bcl-x pathway is critical in erythroid differentiation. Via JAK2-mediated tyrosine phosphorylation, erythropoietin and epoetin alfa also activates other intracellular proteins involved in erythroid cell proliferation and survival, such as Shc , phosphatidylinositol 3-kinase (PI3K), and phospholipase C-γ1 [A33079].
|
The time to reach peak concentration is slower via the subcutaneous route than the intravenous route which ranges from 20 to 25 hours, and the peak is always well below the peak achieved using the intravenous route (5–10% of those seen with IV administration).[A33080] The bioavailability of subcutaneous injectable erythropoietin is much lower than that of the intravenously administered product and is approximately 20-40%.[A33080]
**Adult and paediatric patients with CRF:** Following subcutaneous administration, the peak plasma levels are achieved within 5 to 24 hours [FDA Label].
**Cancer patients receiving cyclic chemotherapy:** The average time to reach peak plasma concentration was approximately 13.3 ± 12.4 hours after 150 Units/kg three times per week (TIW) subcutaneous (SC) dosing. The Cmax is expected be 3- to 7- fold higher and the Tmax is expected to be 2- to 3-fold longer in patients receiving a 40,000 Units SC weekly dosing regimen [FDA Label].
|
Binding of erythropoietin and epoetin alfa to EPO-R leads to cellular internalization, which involves the degradation of the ligand. Erythropoietin and epoetin alfa may also be degraded by the reticuloendothelial scavenging pathway or lymphatic system [A33080].
|
Overdose from epoetin alfa include signs and symptoms associated with an excessive and/or rapid increase in hemoglobin concentration, including cardiovascular events. Patients with suspected or known overdose should be monitored closely for cardiovascular events and hematologic abnormalities. Polycythemia should be managed acutely with phlebotomy, as clinically indicated. Following resolution of the overdose, reintroduction of epoetin alfa therapy should be accompanied by close monitoring for evidence of rapid increases in hemoglobin concentration (>1 gm/dL per 14 days). In patients with an excessive hematopoietic response, reduce the dose in accordance with the recommendations described in the drug label [FDA Label].
|
**Healthy volunteers:** The half life is approximately 4 hours in healthy volunteers receiving an intravenous injection [F85]. A half-life of approximately 6 hours has been reported in children [F85].
**Adult and paediatric patients with CRF:** The elimination half life following intravenous administration ranges from 4 to 13 hours, which is about 20% longer in CRF patients than that in healthy subjects. The half life is reported to be similar between adult patients receiving or not receiving dialysis [FDA Label].
**Cancer patients receiving cyclic chemotherapy:** Following subcutaneous administration, the average half life is 40 hours with range of 16 to 67 hours [FDA Label].
|
No information of serum protein binding available.
|
Erythropoietin and epoetin alfa are cleared via uptake and degradation via the EPO-R-expressing cells, and may also involve other cellular pathways in the interstitium, probably via cells in the reticuloendothelial scavenging pathway or lymphatic system [A33080]. Only a small amount of unchanged epoetin alfa is found in the urine [F86].
|
In healthy volunteers, the volume of distribution of intravenous epoetin alfa was generally similar to the plasma volume (range of 40–63.80 mL/kg), indicating limited extravascular distribution [A33080, A33076].
|
**Healthy volunteers: ** In male volunteers receiving intravenous epoetin alfa, the total body clearance was approximately 8.12 ± 1.00 mL/h/kg [A33076].
**Cancer patients receiving cyclic chemotherapy:** The average clearance was approximately 20.2 ± 15.9 mL/h/kg after 150 Units/kg three times per week (TIW) subcutaneous (SC) dosing [FDA Label]. The patients receiving a 40,000 Units SC weekly dosing regimen display a lower clearance (9.2 ± 4.7 mL/h/kg) [FDA Label].
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved"
] |
[
"B03XA",
"B03X",
"B03",
"B"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "34.14",
"description": "Epogen 2000 unit/ml vial",
"unit": "vial"
},
{
"cost": "37.09",
"description": "Procrit 2000 unit/ml vial",
"unit": "vial"
},
{
"cost": "47.53",
"description": "Epogen 3000 unit/ml vial",
"unit": "vial"
},
{
"cost": "55.63",
"description": "Procrit 3000 unit/ml vial",
"unit": "vial"
},
{
"cost": "61.34",
"description": "Epogen 4000 unit/ml vial",
"unit": "vial"
},
{
"cost": "74.17",
"description": "Procrit 4000 unit/ml vial",
"unit": "vial"
},
{
"cost": "151.8",
"description": "Epogen 10000 unit/ml vial",
"unit": "ml"
},
{
"cost": "303.6",
"description": "Epogen 20000 unit/ml vial",
"unit": "ml"
},
{
"cost": "315.74",
"description": "Epogen 10000 unit/ml Solution 2ml Vial",
"unit": "vial"
},
{
"cost": "358.02",
"description": "Procrit 10000 unit/ml Solution 2ml Vial",
"unit": "vial"
},
{
"cost": "378.14",
"description": "Procrit 20000 unit/ml Solution",
"unit": "ml"
},
{
"cost": "388.97",
"description": "Procrit 20000 unit/ml vial",
"unit": "ml"
},
{
"cost": "640.37",
"description": "Epogen 40000 unit/ml vial",
"unit": "ml"
},
{
"cost": "710.87",
"description": "Procrit 10000 unit/ml vial",
"unit": "vial"
},
{
"cost": "767.03",
"description": "Procrit 40000 unit/ml vial",
"unit": "vial"
},
{
"cost": "1578.72",
"description": "Epogen 10000 unit/ml Solution 1 Box Contains Ten 1ml Vials",
"unit": "box"
},
{
"cost": "3157.44",
"description": "Epogen 20000 unit/ml Solution 1 Box Contains Ten 1ml Vials",
"unit": "box"
},
{
"cost": "6852.3",
"description": "Epogen 40000 unit/ml Solution 1 Box Contains Ten 1ml Vials",
"unit": "box"
}
] |
[
{
"approved": "1997-05-27",
"country": "Canada",
"expires": "2014-05-27",
"number": "1339047"
}
] |
1-165-Erythropoietin (human clone λHEPOFL13 protein moiety), glycoform α | E.P.O. | EPOETIN | Epoetin alfa | Epoetin alfa rDNA | Epoetin alfa-epbx | Epoetin alfa, recombinant | Epoetin epsilon | Epoetin gamma | Epoetin gamma rDNA | Epoetin kappa | Epoetin omega | Epoetin theta | Epoetin zeta | Epoetina alfa | Epoetina dseta | Epoetina zeta | Epoétine zêta | Epoetinum zeta | Erythropoiesis stimulating factor | Erythropoietin (human, recombinant) | Erythropoietin (recombinant human) | ESF | RECOMBINANT HUMAN ERYTHROPOIETIN ALFA | SH-polypeptide-72 | EPO-R
|
[
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Abseamed",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Binocrit",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Biopoin",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epoetin Alfa Hexal",
"Epogen",
"Epogen",
"Epogen",
"Epogen",
"Epogen",
"Epogen",
"Epogen",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eporatio",
"Eprex Sterile Solution",
"Eprex Sterile Solution",
"Eprex Sterile Solution 10000iu/1.0ml",
"Eprex Sterile Solution 10000iu/ml",
"Eprex Sterile Solution 1000iu/0.5ml",
"Eprex Sterile Solution 20000iu/ml",
"Eprex Sterile Solution 2000iu/0.5ml",
"Eprex Sterile Solution 2000iu/ml",
"Eprex Sterile Solution 3000iu/0.3ml",
"Eprex Sterile Solution 40000iu/ml",
"Eprex Sterile Solution 4000iu/0.4ml",
"Eprex Sterile Solution 4000iu/ml",
"Eprex Sterile Solution 5000iu/0.5ml",
"Eprex Sterile Solution 6000 Iu/0.6 Ml",
"Eprex Sterile Solution 8000 Iu/0.8 Ml",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon",
"Neorecormon Guard",
"Neorecormon Guard",
"Procrit",
"Procrit",
"Procrit",
"Procrit",
"Procrit",
"Procrit",
"Procrit",
"Procrit",
"Procrit",
"Procrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Retacrit",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo",
"Silapo"
] |
[
"Epobel",
"Epocept",
"Epofit",
"Epogin",
"Eqralys",
"Nanokine"
] |
[] |
[
"P19235"
] |
[] |
[] |
[] |
DB00017
|
Salmon calcitonin
|
Synthetic peptide, 32 residues long formulated as a nasal spray.
|
liquid
|
Used in the treatment of symptomatic Paget's disease for patients unresponsive to alternate treatments or intolerant to such treatments. In addition, it is used in emergency situations when serum calcium levels must be decreased quickly until the underlying condition is identified. It can also be added to existing therapeutic regimens for hypercalcemia such as intravenous fluids and furosemide, oral phosphate or corticosteroids, or other agents. Calcitonin can be used in patients with azotemia and cases where intravenous fluids would be contraindicated due to limited cardiac reserves. Also for the treatment of post-menopausal osteoporosis in women more than 5 years post-menopause.
|
Calcitonin inhibits bone resorption by osteoclasts (bone remodeling cells) and promotes bone formation by osteoblasts. This leads to a net increase in bone mass and a reduction in plasma calcium levels. It also promotes the renal excretion of ions such as calcium, phosphate, sodium, magnesium, and potassium by decreasing tubular reabsorption. In consequence, there is an increase in the jejunal secretion of water, sodium, potassium, and chloride.
|
Calcitonin binds to the calcitonin receptor (found primarily in osteoclasts) which then enhances the production of vitamin D producing enzymes (25-hydroxyvitamine D-24-hydroxylase), leading to greater calcium retention and enhanced bone density. Binding of calcitonin to its receptor also activates adenylyl cyclase and the phosphatidyl-inositol-calcium pathway.
|
Salmon calcitonin is rapidly absorbed with bioavailability of 71% following subcutaneous injection and 66% following intramuscular injection in humans. Via the nasal route, the bioavailability varies between 3 to 5% relative to IM.
|
Salmon calcitonin primarily undergoes degradation in the kidneys to form pharmacologically inactive metabolites. It is also metabolized in the blood and the peripheral tissue.
|
Salmon calcitonin was shown to inhibit lactation in animals and is not recommend in nursing mothers. While research in animals have shown a decrease in fetal weight, no studies have yet shown similar results in humans. It is recommended however to proceed carefully when administering salmon calcitonin to pregnant women and consider if the benefits outweigh the risks. Because of its protein nature, salmon calcitonin may provoke an allergy reaction (bronchospams and swelling of the tongue/throat) that can turn into a full-blown anaphylactic response. The manufacturer also reports an increase in the risk of malignancies from oral route (0.7%) to intranasal route (2.4%) compared to placebo. The same may apply to IV, IM and SC routes since the systemic exposure is higher in those cases.
Nausea is noticeable in some patients but tends to decrease with continued administration. Rhinitis, headaches and back pain have also been reported among others.
|
Half-life elimination (terminal): I.M. 58 minutes; SubQ 59 to 64 minutes; Nasal: ~18 to 23 minutes
|
Protein binding is about 30 to 40%.
|
Urine. Studies with injectable calcitonin show increases in the excretion of filtered phosphate, calcium, and sodium by decreasing their tubular reabsorption in the kidney.
|
0.15 to 0.3 L/kg
| null |
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[
"H05BA",
"H05B",
"H05",
"H"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "8.81",
"description": "Caltine 100 (100 Iu/Ml) 100 iu/ml",
"unit": "ml"
},
{
"cost": "29.94",
"description": "Calcimar 200 iu/ml",
"unit": "ml"
},
{
"cost": "30.73",
"description": "Miacalcin 200 unit/ml vial",
"unit": "ml"
},
{
"cost": "34.3",
"description": "Fortical 200 unit nasal spray",
"unit": "ml"
},
{
"cost": "39.51",
"description": "Calcitonin-salmon 200 unit sp",
"unit": "ml"
},
{
"cost": "44.68",
"description": "Miacalcin 200 unit nasal spray",
"unit": "ml"
},
{
"cost": "63.59",
"description": "Miacalcin For Inj, 2 unit = 1 Box 2ml Vial",
"unit": "vial"
},
{
"cost": "123.28",
"description": "Calcitonin (Salmon) 200 unit/act Solution 3.7ml Bottle",
"unit": "bottle"
},
{
"cost": "139.39",
"description": "Miacalcin 200 unit/act Solution 3.7ml Bottle",
"unit": "bottle"
}
] |
[
{
"approved": "1998-03-31",
"country": "United States",
"expires": "2015-03-31",
"number": "5733569"
},
{
"approved": "2002-08-27",
"country": "United States",
"expires": "2021-02-02",
"number": "6440392"
},
{
"approved": "2012-08-14",
"country": "United States",
"expires": "2021-02-02",
"number": "RE43580"
},
{
"approved": "2009-06-30",
"country": "United States",
"expires": "2021-02-02",
"number": "RE40812"
}
] |
Calcitonin (Salmon Synthetic) | Calcitonin salmon | Calcitonin salmon recombinant | Calcitonin-salmon | Calcitonin, salmon | Calcitonina salmón sintética | Recombinant salmon calcitonin | Salmon calcitonin | CT-R
|
[
"Apo-calcitonin Injectable",
"Apo-calcitonin Nasal Spray",
"Calcimar",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon",
"Calcitonin Salmon Injection USP",
"Caltine Inj 100 Unit/ml (1ml Amp)",
"Caltine Inj 100unit/ml (0.5ml Amp)",
"Forcaltonin",
"Fortical",
"Fortical",
"Miacalcin",
"Miacalcin",
"Miacalcin",
"Miacalcin",
"Miacalcin",
"Miacalcin",
"Miacalcin",
"Miacalcin Injection 200iu/ml",
"Miacalcin Nasal Spray 200 Iu",
"Pro-calcitonin - 200",
"Sandoz-calcitonin NS"
] |
[
"Calcimar"
] |
[] |
[
"P30988"
] |
[] |
[] |
[] |
DB00018
|
Interferon alfa-n3
|
Purified, natural (n is for natural) human interferon alpha proteins (consists of 3 forms or polymorphisms including 2a, 2b and 2c). 166 residues, some are glycosylated (MW range from 16 kD to 27 kD).
|
liquid
|
For the intralesional treatment of refractory or recurring external condylomata acuminata.
|
Interferon alfa-n3 upregulates the expression of MHC I proteins, allowing for increased presentation of peptides derived from viral antigens. This enhances the activation of CD8+ T cells that are the precursors for cytotoxic T lymphocytes (CTLs) and makes the macrophage a better target for CTL-mediated killing. Interferon alpha also induce the synthesis of several key antiviral mediators, including 2'-5' oligoadenylate synthetase (2'-5' A synthetase), beta-2 microglobulin, neopterin and protein kinase R.
|
Interferon alpha binds to type I interferon receptors (IFNAR1 and IFNAR2c) which, upon dimerization, activate two Jak (Janus kinase) tyrosine kinases (Jak1 and Tyk2). These transphosphorylate themselves and phosphorylate the receptors. The phosphorylated INFAR receptors then bind to Stat1 and Stat2 (signal transducers and activators of transcription) which dimerize and activate multiple (~100) immunomodulatory and antiviral proteins. Interferon alpha binds less stably to type I interferon receptors than interferon beta.
| null | null | null | null | null | null | null | null |
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[] |
[
"Humans and other mammals"
] |
[
{
"cost": "412.87",
"description": "Alferon n 5 million unit vial",
"unit": "ml"
}
] |
[] |
Interferon alfa-n3 | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member 1 | IFN-alpha/beta receptor 1 | IFN-R-1 | IFNAR | Type I interferon receptor 1 | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | Interferon alpha binding protein | Type I interferon receptor 2 | 1.14.14.1 | Cholesterol 25-hydroxylase | CYPIA2 | Cytochrome P(3)450 | Cytochrome P450 4 | Cytochrome P450-P3 | Hydroperoxy icosatetraenoate dehydratase
|
[
"Alferon"
] |
[
"Alferon",
"Alferon N"
] |
[] |
[
"P17181",
"P48551"
] |
[
"P05177"
] |
[] |
[] |
DB00019
|
Pegfilgrastim
|
Pegfilgrastim is a PEGylated form of the recombinant human granulocyte colony-stimulating factor (G-CSF) analogue, [filgrastim].[A187601] The drug is approved for use to decrease the incidence of infection, as manifested by febrile neutropenia, in susceptible patients with with non-myeloid cancer receiving myelosuppressive anti-cancer treatment.[L9746] Although the risk of developing febrile neutropenia is less than 20% in many readily used chemotherapy regimens,[A248855] infections pose risks of hospitalization and mortalities.[A187631] Due to the relatively short circulating half-life of filgrastim, a 20 kDa PEG moiety was covalently conjugated to the N-terminus of filgrastim (at the methionine residue) to develop longer-acting pegfilgrastim.[A29,A187607] Due to a longer half-life and slower elimination rate than filgrastim, pegfilgrastim requires less frequent dosing than filgrastim; however, pegfilgrastim has a comparable pharmacological activity to filgrastim and binds to the G-CSF receptor to stimulate the proliferation, differentiation, and activation of neutrophils.[A187607]
First developed by Amgen, pegfilgrastim was initially approved by the FDA in 2002 and marketed as Neulasta. It is typically administered via a subcutaneous injection. There are several pegfilgrastim biosimilars (Fulphila, Pelgraz or Lapelga, Pelmeg, Udenyca, Ziextenzo, Grasustek, Fylnetra, Stimufend) by Health Canada, European Union (EU), and FDA that are approved to reduce infection risk.[L9779,L9785,L43050] These biosimilars are highly similar to the reference product, Neulasta, in terms of pharmacological and pharmacokinetic profile and conditions of use.[L9974]
|
liquid
|
Pegfilgrastim is indicated to decrease the incidence of infection, as manifested by febrile neutropenia, in patients with non myeloid malignancies receiving myelosuppressive anti-cancer drugs associated with a clinically significant incidence of febrile neutropenia.[L44221]
It is also indicated to increase survival in patients acutely exposed to myelosuppressive doses of radiation (Hematopoietic Subsyndrome of Acute Radiation Syndrome).[L44221]
|
Pegfilgrastim is a recombinant human granulocyte colony-stimulating factor (G-CSF) that promotes the production, proliferation, and maturation of neutrophils, which are white blood cells involved in both innate and adaptive immune responses.[A187631,A248855] The safety and efficacy of pegfilgrastim in reducing the risk of febrile neutropenia and infections have been demonstrated in various tumor types and settings.[A187631]
During chemotherapy-induced neutropenia, the clearance of pegfilgrastim is significantly reduced and the concentration of pegfilgrastim is sustained until the onset of neutrophil recovery.[A29] Serum concentrations of pegfilgrastim decline as the neutrophil count increases as neutrophil and neutrophil precursors are involved in cell-mediated clearance of the drug.[A187601] Due the addition of polyethylene glycol group to its structure, Pegfilgrastim is a long-acting form of filgrastim with an extended serum half-life and reduced renal clearance.[A187607] Although it is more slowly absorbed than filgrastim, self-regulation of pegfilgrastim is more efficient and the drug effects are maintained during one chemotherapy cycle (2-3 weeks).[A29]
|
Neutrophils are short-lived immune cells that are highly susceptible to cell death following myelosuppressive chemotherapy. This marked reduction in neutrophil numbers during chemotherapy increases the risk of hospitalization, infection, and infection-related mortality. It also directly impacts the clinical outcome of patients if cases of febrile neutropenia requires dose reductions or schedule delay of chemotherapy, thus reducing the clinical efficacy of chemotherapy and patient benefit from receiving appropriate treatment.[A187631]
G-CSF is an endogenous haematopoietic growth factor that stimulates granulopoietic cells of the neutrophil lineage. Pegfilgrastim mimics its biological actions and binds to the same G-CSF receptor expressed on cells of myeloid lineage, such as granulocytic precursors and mature neutrophils.[A29] Upon binding of the ligand, G-CSF receptor undergoes a conformational change and activates several downstream signalling pathways including JAK/STAT, PI3K/AKT and MAPK/ERK.[A187868] These pathways work to increase proliferation and differentiation of granulocyte progenitor cells, induce maturation of the progenitor cells, and enhance survival and function of mature neutrophils.[A29]
|
Pegfilgrastim has a lower absolute bioavailability than filgrastim following subcutaneous administration. The absorption of pegfilgrastim is largely dependent on the lymphatic system due to the attached PEG group contributing to the large size of the drug. It is slowly absorbed following subcutaneous administration with a time to peak concentration (T<sub>max</sub>) of about one to two days.[A29]
|
It is not know whether pegfilgrastim is metabolized into major metabolites.[L10022] Once it binds to the therapeutic target, pegfilgrastim is internalized by the neutrophil and undergoes nonspecific degradation.[A29]
|
The maximum safe dose of pegfilgrastim has not been established; however, the highest dose used in clinical trials was 300 mcg/kg.[A248855] Overdosage of pegfilgrastim may result in leukocytosis and bone pain. Events of edema, dyspnea, and pleural effusion have been reported in a single patient who self-administered pegfilgrastim on 8 consecutive days in error. In the event of overdose, the patient should be monitored for signs and symptoms of toxicity and responded with appropriate general supportive care.[L9746,A248855]
|
The serum half-life of Pegfilgrastim is highly variable depending on the absolute neutrophil count, with the range of 15 to 80 hours following subcutaneous administration. The median serum half-life of 42 hours.[A187607,L9746]
|
The plasma protein binding of pegfilgrastim is unlikely.[L10022]
|
The polyethylene glycol moiety limits the renal clearance by glomerular filtration of pegfilgrastim, making neutrophil-mediated clearance as the predominant route of elimination.[A187607] This elimination pathway is initiated by the binding of pegfilgrastim to the G-CSF receptor on the neutrophil cell surface, leading to the internalization of the pegfilgrastim-receptor complex via endocytosis and subsequent degradation inside the cell. While hepatic clearance has not been well characterized for pegfilgrastim, its non-PEGylated precursor filgrastim is known to be unaffected by changes in hepatic clearance.[A29]
|
Pegfilgrastim appears to have a volume of distribution of approximately 170 L.[A33290]
|
Pegfilgrastim has a self-regulating clearance that involves neutrophil-induced clearance.[A29,A187631] The clearance is dependent on the number of neutrophils and body weight of the patient: the clearance increases with increasing number of granulocytes and lower body weights.[L9746] Pegfilgrastim is not eliminated from the circulation until neutrophils start to recover following chemotherapy-induced neutropenia and its clearance is increased as neutrophil counts also increase.[A187631] The apparent serum clearance is 14 mL/h/kg.[L10022]
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved"
] |
[
"L03AA",
"L03A",
"L03",
"L"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "4026.05",
"description": "Neulasta 6 mg/0.6ml Solution 0.6ml Syringe",
"unit": "syringe"
},
{
"cost": "4102.37",
"description": "Neulasta 6 mg/0.6 ml syringe",
"unit": "syringe"
}
] |
[
{
"approved": "2007-07-31",
"country": "Canada",
"expires": "2024-07-31",
"number": "1341537"
},
{
"approved": "1997-07-29",
"country": "Canada",
"expires": "2014-07-29",
"number": "1339071"
}
] |
Granulocyte colony-stimulating factor pegfilgrastim | peg-filgrastim | Pegfilgrastim | pegfilgrastim-apgf | pegfilgrastim-bmez | pegfilgrastim-cbqv | pegfilgrastim-jmdb | G-CSF receptor | G-CSF-R | GCSFR | 3.4.21.37 | Bone marrow serine protease | ELA2 | Elastase-2 | HLE | Human leukocyte elastase | Medullasin | PMN elastase
|
[
"Armlupeg",
"Cegfila",
"Fulphila",
"Fulphila",
"Fulphila",
"Fulphila",
"Fulphila",
"Fylnetra",
"Grasustek",
"Lapelga",
"Lapelga",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neulasta",
"Neupopeg",
"Neupopeg",
"Neupopeg",
"Niopeg",
"Nyvepria",
"Nyvepria",
"Nyvepria",
"Pelgraz",
"Pelgraz",
"Pelmeg",
"Ristempa",
"Ristempa",
"Ristempa",
"Stimufend",
"Stimufend",
"Udenyca",
"Udenyca",
"Udenyca",
"Udenyca",
"Ziextenzo",
"Ziextenzo",
"Ziextenzo"
] |
[] |
[] |
[
"Q99062"
] |
[
"P08246"
] |
[] |
[] |
DB00020
|
Sargramostim
|
Sargramostim is a human recombinant granulocyte macrophage colony-stimulating factor (GM-CSF) expressed in yeast. It is a glycoprotein that is 127 residues. Substitution of Leu23 leads to a difference from native protein.
|
liquid
|
For the treatment of cancer and bone marrow transplant
|
Sargramostim is used in the treatment of bone marrow transplant recipients or those exposed to chemotherapy an recovering from acut myelogenous leukemia, Leukine or GM-CSF is a hematopoietic growth factor which stimulates the survival, clonal expansion (proliferation) and differentiation of hematopoietic progenitor cells. GM-CSF is also capable of activating mature granulocytes and macrophages. After a bone marrow transplant or chemotherapy, patients have a reduced capacity to produce red and white blood cells. Supplementing them with external sources of GM-CSF helps bring the level of neutrophils back to normal so that they can better fight infections.
|
Sargramostim binds to the Granulocyte-macrophage colony stimulating factor receptor (GM-CSF-R-alpha or CSF2R) which stimulates a JAK2 STAT1/STAT3 signal transduction pathway. This leads to the production of hemopoietic cells and neutrophils
| null | null | null | null | null | null | null |
* 420 mL/min/m2 [Normal people with liquid LEUKINE (IV)]
* 431 mL/min/m2 [Normal people with lyophilized LEUKINE (IV)]
* 549 mL/min/m2 [Normal people with liquid LEUKINE (SC)]
* 529 mL/min/m2 [Normal people with lyophilized LEUKINE (SC)]
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[
"L03AA",
"L03A",
"L03",
"L"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "204.79",
"description": "Leukine 250 mcg vial",
"unit": "vial"
},
{
"cost": "0.42",
"description": "Bio-immunex capsule",
"unit": "capsule"
}
] |
[
{
"approved": "2000-12-05",
"country": "Canada",
"expires": "2017-12-05",
"number": "1341150"
}
] |
Recombinant human granulocyte-macrophage colony stimulating factor | rGM-CSF | rHu GM-CSF | Sargramostim | CDw116 | CSF2R | CSF2RY | GM-CSF-R-alpha | GMCSFR-alpha | GMR-alpha | IL-3 receptor subunit alpha | IL-3R subunit alpha | IL-3R-alpha | IL-3RA | IL3R | CDw131 | GM-CSF/IL-3/IL-5 receptor common beta subunit | IL3RB | IL5RB | Fibroglycan | Heparan sulfate proteoglycan core protein | HSPG | HSPG1 | SYND2 | BMPG | MBP | Proteoglycan 2
|
[
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine",
"Leukine"
] |
[
"Leucomax"
] |
[] |
[
"P15509",
"P26951",
"P32927",
"P34741",
"P13727"
] |
[] |
[] |
[] |
DB00022
|
Peginterferon alfa-2b
|
Peginterferon alfa-2b is a form of recombinant interferon used as part of combination therapy to treat chronic Hepatitis C, an infectious liver disease caused by infection with Hepatitis C Virus (HCV). HCV is a single-stranded RNA virus that is categorized into nine distinct genotypes, with genotype 1 being the most common in the United States, and affecting 72% of all chronic HCV patients [L852]. Treatment options for chronic Hepatitis C have advanced significantly since 2011, with the development of Direct Acting Antivirals (DAAs) resulting in less use of Peginterferon alfa-2b. Peginterferon alfa-2b is derived from the alfa-2b moeity of recombinant human interferon and acts by binding to human type 1 interferon receptors. Activation and dimerization of this receptor induces the body's innate antiviral response by activating the janus kinase/signal transducer and activator of transcription (JAK/STAT) pathway. Use of Peginterferon alfa-2b is associated with a wide range of severe adverse effects including the aggravation and development of endocrine and autoimmune disorders, retinopathies, cardiovascular and neuropsychiatric complications, and increased risk of hepatic decompensation in patients with cirrhosis. The use of Peginterferon alfa-2b has largely declined since newer interferon-free antiviral therapies have been developed.
In a joint recommendation published in 2016, the American Association for the Study of Liver Diseases (AASLD) and the Infectious Diseases Society of America (IDSA) no longer recommend Peginterferon alfa-2b for the treatment of Hepatitis C [A19593]. Peginterferon alfa-2b was used alongside [DB00811] with the intent to cure, or achieve a sustained virologic response (SVR), after 48 weeks of therapy. SVR and eradication of HCV infection is associated with significant long-term health benefits including reduced liver-related damage, improved quality of life, reduced incidence of Hepatocellular Carcinoma, and reduced all-cause mortality [A19626].
Peginterferon alfa-2b is available as a variable dose injectable product (tradename Pegintron) used for the treatment of chronic Hepatitis C. Approved in 2001 by the FDA, Pegintron is indicated for the treatment of HCV with [Ribavirin] or other antiviral drugs [FDA Label]. When combined together, Peginterferon alfa-2b and [Ribavirin] have been shown to achieve a SVR between 41% for genotype 1 and 75% for genotypes 2-6 after 48 weeks of treatment.
|
liquid
|
Peginterferon alfa-2b is indicated for the treatment of HCV in combination with [DB00811] and a NS3/4A protease inhibitor for genotype 1 or without a NS3/4A protease inhibitor for genotypes 2-6 [FDA Label]. May be used as a monotherapy in patients with contraindications to or significant intolerance to other anti-viral therapies.
It is also indicated for the adjuvant treatment of melanoma with microscopic or gross nodal involvement within 84 days of definitive surgical resection, including complete lymphadenectomy.[L45334]
|
Peginterferon alfa-2b inhibits viral replication in infected cells, suppresses cell proliferation, induces apoptosis, and exerts an anti-angiogenic effect [FDA Label]. Exerts immunomodulatory effects such as enhancement of the phagocytic activity of macrophages, activation of NK cells, stimulation of cytotoxic T-lymphocytes, and the upregulation of the Th1 T-helper cell subset. Also increases concentrations of effector proteins such as serum neopterin and 2'5' oligoadenylate synthetase, raises body temperature, and causes reversible decreases in leukocyte and platelet counts.
|
Peginterferon alfa-2b is derived from recombinant human interferon's alfa-2b moeity [FDA Label]. It binds to and activates human type 1 interferon receptors causing them to dimerize. This activates the JAK/STAT pathway. Activation of the JAK/STAT pathway increases expression of multiple genes in multiple tissues involved in the innate antiviral response. Peginterferon alfa-2b may also acitvate the nuclear factor κB pathway.
|
Peginterferon alfa-2b reaches peak plasma concentration 15-44 hours after subcutaneous administration [FDA Label]. The mean absorption half-life is 4.6 hours. After multiple doses the bioavailability of Peginterferon alfa-2b increases with trough concentrations at week 48 3-fold higher than those at week 4.
| null |
Peginterferon alfa-2b may manifest neuropsychiatric complications include suicide, suicidal ideation, homicidal ideation, depression, relapse of drug addiction, and drug overdose [FDA Label]. Hypertension, supraventricular arrhythmias, chest pain, and myocardial infarction have been observed in patients using Peginterferon alfa-2b. Peginterferon alfa-2b may produce myelosuppression as well as the development or aggravation of autoimmune disorders including myositis, hepatitis, thrombotic thrombocytopenic purpura, idiopathic thrombocytopenic purpura, psoriasis, rheumatoid arthritis, interstitial nephritis, thyroiditis, and systemic lupus erythematosus. Peginterferon alfa-2b causes or aggravates hypothyroidism and hyperthyroidism. Hyperglycemia, hypoglycemia, and diabetes mellitus have been observed to develop in patients treated with Peginterferon alfa-2b. Peginterferon alfa-2b may decrease or produce loss of vision, retinopathy including macular edema, retinal artery or vein thrombosis, retinal hemorrhages and cotton wool spots, optic neuritis, papilledema and serous retinal detachment. Peginterferon mayy be related to increased ischemic and hemorrhagic cerebrovascular events. Patients with cirrhosis on Peginterferon alfa-2b are at risk of hepatic decompensation. Dyspnea, pulmonary infiltrates, pneumonia, bronchiolitis obliterans, interstitial pneumonitis, pulmonary hypertension and sarcoidosis may be induced or aggravated by Peginterferon alfa-2b. Serious and severe infections (bacterial, viral, or fungal) have been reported during treatment with Peginterferon alfa-2b. Ulcerative and hemorrhagic/ischemic colitis have been observed within 12 weeks of starting Peginterferon alfa-2b treatment. Pancreatitis and peripheral nephropathy have also been reported. Peginterferon alfa-2b is associated with growth inhibition in pediatric patients. Use of Peginterferon alfa-2b while pregant may result in delopmental abnormalities or death of the fetus.
|
The mean half-life of elimination of Peginterferon alfa-2b is 40 hours in a range of 22-60 hours [FDA Label].
| null |
Renal elimination accounts for 30% of Peginterferon alfa-2b elimination [FDA Label].
| null |
The estimated apparent clearance of Peginterferon alfa-2b is 22 milliters per hour per kilogram [FDA Label].
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved"
] |
[
"L03AB",
"L03A",
"L03",
"L",
"L03AB",
"L03A",
"L03",
"L"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "553.4",
"description": "Peg-Intron 50 mcg kit",
"unit": "kit"
},
{
"cost": "553.4",
"description": "Peg-Intron redipen 50 mcg",
"unit": "redipen"
},
{
"cost": "581.02",
"description": "Peg-Intron redipen 80 mcg",
"unit": "redipen"
},
{
"cost": "607.19",
"description": "Peg-Intron 50 mcg/0.5ml Kit",
"unit": "kit"
},
{
"cost": "609.26",
"description": "Peg-Intron 80 mcg Kit",
"unit": "kit"
},
{
"cost": "610.09",
"description": "Peg-Intron redipen 120 mcg",
"unit": "redipen"
},
{
"cost": "637.49",
"description": "Peg-Intron Redipen 80 mcg/0.5ml Kit",
"unit": "kit"
},
{
"cost": "639.74",
"description": "Peg-Intron 120 mcg Kit",
"unit": "kit"
},
{
"cost": "640.6",
"description": "Peg-Intron redipen 150 mcg 4pk",
"unit": "redipen"
},
{
"cost": "640.61",
"description": "Peg-Intron redipen 150 mcg",
"unit": "redipen"
},
{
"cost": "669.39",
"description": "Peg-Intron Redipen 120 mcg/0.5ml Kit",
"unit": "kit"
},
{
"cost": "671.74",
"description": "Peg-Intron 150 mcg Kit",
"unit": "kit"
},
{
"cost": "702.87",
"description": "Peg-Intron Redipen 150 mcg/0.5ml Kit",
"unit": "kit"
},
{
"cost": "2428.8",
"description": "Peg-Intron Redipen Pak 4 4 50 mcg/0.5ml Kit Box",
"unit": "kit"
}
] |
[
{
"approved": "2008-02-19",
"country": "Canada",
"expires": "2025-02-19",
"number": "1341567"
},
{
"approved": "2002-02-26",
"country": "Canada",
"expires": "2016-10-31",
"number": "2329474"
}
] |
Peginterferon alfa-2b | CRF2-1 | Cytokine receptor class-II member 1 | Cytokine receptor family 2 member 1 | IFN-alpha/beta receptor 1 | IFN-R-1 | IFNAR | Type I interferon receptor 1 | IFN-alpha binding protein | IFN-alpha/beta receptor 2 | IFN-R-2 | IFNABR | IFNARB | Interferon alpha binding protein | Type I interferon receptor 2 | 1.14.14.1 | Cholesterol 25-hydroxylase | CYPIA2 | Cytochrome P(3)450 | Cytochrome P450 4 | Cytochrome P450-P3 | Hydroperoxy icosatetraenoate dehydratase | 1.14.14.- | Cholesterol 25-hydroxylase | CYP2DL1 | CYPIID6 | Cytochrome P450-DB1 | Debrisoquine 4-hydroxylase | (R)-limonene 6-monooxygenase | (S)-limonene 6-monooxygenase | (S)-limonene 7-monooxygenase | 1.14.14.1 | Cholesterol 25-hydroxylase | CYP2C10 | CYPIIC9 | Cytochrome P-450MP | Cytochrome P450 MP-4 | Cytochrome P450 MP-8 | Cytochrome P450 PB-1 | S-mephenytoin 4-hydroxylase
|
[
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"PegIntron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"PegIntron",
"PegIntron",
"PegIntron",
"PegIntron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Pegintron",
"Sylatron",
"Sylatron",
"Sylatron",
"Sylatron",
"Sylatron",
"Sylatron",
"Unitron Peg",
"Unitron Peg",
"Unitron Peg",
"Unitron Peg",
"Victrelis Triple",
"Victrelis Triple",
"Victrelis Triple",
"Victrelis Triple"
] |
[
"PEG-Intron"
] |
[
"Pegetron",
"Pegetron",
"Pegetron",
"Victrelis Triple",
"Victrelis Triple",
"Victrelis Triple",
"Victrelis Triple",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron",
"Pegetron"
] |
[
"P17181",
"P48551"
] |
[
"P05177",
"P10635",
"P11712"
] |
[] |
[] |
DB00023
|
Asparaginase Escherichia coli
|
Asparaginase derived from _Escherichia coli_ (L-asparagine amidohydrolase, EC 3.5.1.1) is an enzyme responsible for the metabolism of L-asparagine, by catalyzing L-asparagine into L-aspartic acid and ammonia. It also facilitates the production of oxaloacetate which is needed for general cellular metabolism. Asparaginase from _E. coli_ has clinically shown to exhibit antitumor actions in models of leukaemias [A31996, A31997]. L-asparaginase of _E. coli_ is marketed under several different trade names, including Elspar, for the treatment of acute lymphoblastic leukemia (ALL) as part of a multi-agent chemotherapeutic regimen. It is available as intramuscular or intravenous injections. Therapeutic L-asparaginase from _E. coli_ works by depleting the levels of non-essential amino acid, asparagine, in lymphoblastic leukemic cells thus promoting apoptotic cell death [A31999]. For patients who develop hypersensitivity to _E. coli_-derived formulations of L-asparaginase, the use of PEGylated or non-PEGylated [DB08886] is recommended [A31999].
|
liquid
|
Indicated as a component of a multi-agent chemotherapeutic regimen for the treatment of patients with acute lymphoblastic leukemia (ALL).[L39809]
|
In clinical trials of patients with previously untreated, standard-risk ALL, administration of asparaginase resulted in a decrease of plasma asparagine levels from average of 41 μM to less than 3 μM [FDA Label]. The native asparaginase in whom plasma enzyme activity before treatment was greater than 0.1 International Units/mL [FDA Label]. In this study, cerebrospinal fluid asparagine levels in patients treated with asparaginase decreased from 2.8 μM (pretreatment) to 1.0 μM and 0.3 μM at day 7 and day 28 of induction, respectively [FDA Label]. Native E. coli asparaginase results in asparagine depletion in 14 to 23 days following administration [A31999].
|
Asparagine is a non-essential amino acid that maintains DNA, RNA and protein synthesis and promotes cell growth. While healthy and normal cells are capable of obtaining asparagine via dietary intake or synthesizing the asparagine from aspartate via asparagine synthetase activity, lymphoblastic leukemic cells lack the asparagine synthetase enzyme and cannot produce asparagine _de novo_ [A31999]. Thus, leukemic cells rely on exogenous source of asparagine for protein synthesis and cell survival [A31999]. L-asparagine from E. coli serves to deplete plasma levels of asparagine in leukemic cells by converting L-asparagine to L-aspartic acid and ammonia [A31999], leading to reduced reduced DNA, RNA and protein synthesis; inhibition of cell growth; and ultimately the activation of apoptotic cell-death mechanisms [A31999]. Normal cells, however, are able to synthesize asparagine and thus are affected less by the rapid depletion produced by treatment with the enzyme asparaginase [FDA Label].
|
In a study in patients with metastatic cancer and leukemia, daily intravenous administration of L-asparaginase derived from _E. coli_ resulted in a cumulative increase in plasma levels. Following intramuscular injection in patients with metastatic cancer and leukemia, peak plasma levels of asparaginase was achieved 14 to 24 hours post-dosing [FDA Label].
Peak asparaginase activity of native _E. coli_ asparaginase can be observed in 24 to 48 hours following administration [A31999].
| null |
No studies assessing the mutagenic or carcinogenic potential of _E. coli_ L-asparagine have been conducted. In the Ames assay, no mutagenic effect was demonstrated when tested against Salmonella typhimurium strains [FDA Label]. No studies have been performed on impairment of fertility [FDA Label]. Following a single, intravenous injection of 12,500 to 50,000 International Units L-asparagine/kg in rabbits, edema and necrosis of pancreatic islets were observed. The clinical relevance of this finding is unclear as it does not indicate pancreatitis [FDA Label].
|
Plasma half life of L-asparagine derived from _E. coli_ following intravenous injection was 8-30 hrs [FDA Label]. Plasma half-life was 34 to 49 hours after intramuscular injection [FDA Label]. Half-life (mean ± SD) of native _E. coli_ asparaginase is approximately 1.28 ± 0.35 days [A31999].
| null | null |
Apparent volume of distribution was slightly greater than the plasma volume. Asparaginase levels in cerebrospinal fluid were less than 1% of concurrent plasma levels [A31999].
| null |
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[
"L01XX",
"L01X",
"L01",
"L"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "74.6",
"description": "Elspar 10000 unit vial",
"unit": "vial"
}
] |
[] |
Asparaginase | Asparaginase (E. coli) | Colaspase | Escherichia coli L-asparaginase | L-asparaginase | L-asparagine amidohydrolase | Serpin A7 | T4-binding globulin | TBG
|
[
"Elspar",
"Kidrolase",
"Rylaze",
"Spectrila",
"Spectrila"
] |
[] |
[] |
[] |
[] |
[
"P05543"
] |
[] |
DB00024
|
Thyrotropin alfa
|
Thyrotropin alfa is a recombinant form of thyroid stimulating hormone used in performing certain tests in patients who have or have had thyroid cancer. It is also used along with a radioactive agent to destroy remaining thyroid tissue in certain patients who have had their thyroid gland removed because of thyroid cancer. It is a heterodimeric glycoprotein comprised of two non-covalently linked subunits, an alpha subunit of 92 amino acid residues containing two N-linked glycosylation sites and a beta subunit of 112 residues containing one N-linked glycosylation site. The alpha subunit of thyrotropin alfa, which is the effector region responsible for the stimulation of adenylate cyclase, displays close structural similarity with the alpha subunit of human chorionic gonadotropin (hCG), luteinizing hormone (LH), and follicle-stimulating hormone (FSH). The beta subunit (TSHB) bestows its receptor specificity due to the uniqueness to TSH. The amino acid sequence of thyrotropin alfa is identical to that of human pituitary thyroid stimulating hormone.
|
liquid
|
For detection of residueal or recurrent thyroid cancer
|
Binding of thyrotropin alfa to TSH receptors on normal thyroid epithelial cells or on well-differentiated thyroid cancer tissue stimulates iodine uptake and organification. Thyrogen is an exogenous source of human TSH that offers an additional diagnostic tool in the follow-up of patients with a history of well-differentiated thyroid cancer.
|
Thyrotropin Alfa binds to the thyrotropin receptors found on any residual thyroid cells or tissues. This stimulates radioactive iodine uptake for better radiodiagnostic imaging.
|
Time to peak: Median: 10 hours (range: 3-24 hours)
After a single intramuscular injection of 0.9 mg of thyrotropin alfa: Cmax= 116+38mU/L, Tmax=22+8.5 hours. AUC=5088+1728 mU·hr/L.
| null |
No difference in efficacy and toxicity between adult and geriatric patients. No studies in lactating women, pregnant women and pediatrics. Cautionary administration is advised.
|
25 ± 10 hours
| null |
kidney and liver
| null | null |
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"vet_approved"
] |
[
"H01AB",
"H01A",
"H01",
"H"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "1196.4",
"description": "Thyrogen 1.1 mg vial",
"unit": "vial"
}
] |
[
{
"approved": "1998-11-24",
"country": "United States",
"expires": "2015-11-24",
"number": "5840566"
}
] |
Recombinant Human Thyroid Stimulating Hormone | Recombinant thyrotropin alfa | rhTSH | rTSH | Thyrotropin alfa | Thyrotropin alpha | LGR3 | Thyroid-stimulating hormone receptor | TSH-R
|
[
"Thyrogen",
"Thyrogen",
"Thyrogen",
"Thyrogen",
"Thyrogen"
] |
[] |
[] |
[
"P16473"
] |
[] |
[] |
[] |
DB00025
|
Antihemophilic factor, human recombinant
|
Human recombinant antihemophilic factor (AHF) or Factor VIII, 2332 residues, glycosylated, produced by CHO cells
|
solid
|
The human recombinant antihemophilic factor is indicated for use in adults and children with hemophilia A for the control and prevention of bleeding episodes, perioperative management, and routine prophylaxis to prevent or reduce the frequency of bleeding episodes.[L41025, L36130]
|
Antihemophilic Factor binds factor IXa along with calcium and phospholipid, This complex converts factor X to factor Xa to facilitate clotting cascade.
|
Antihemophilic factor (AHF) is a protein found in normal plasma which is necessary for clot formation. The administration of AHF provides an increase in plasma levels of AHF and can temporarily correct the coagulation defect of patients with hemophilia A (classical hemophilia).
| null | null | null |
8.4-19.3 hrs
| null | null | null |
* 4.1 mL/h•kg [Previously treated pediatric patients]
|
Organic Compounds
|
Organic Acids
|
Carboxylic Acids and Derivatives
|
Amino Acids, Peptides, and Analogues
|
[
"approved",
"investigational"
] |
[
"B02BD",
"B02B",
"B02",
"B"
] |
[
"Humans and other mammals"
] |
[
{
"cost": "1.01",
"description": "Monoclate-p 1000 unit kit",
"unit": "kit"
},
{
"cost": "1.01",
"description": "Monoclate-p 1500 unit kit",
"unit": "kit"
},
{
"cost": "1.01",
"description": "Monoclate-p 250 unit kit",
"unit": "kit"
},
{
"cost": "1.01",
"description": "Monoclate-p 500ahfu kit",
"unit": "kit"
},
{
"cost": "1.2",
"description": "Alphanate 1000-1500 unit vial",
"unit": "vial"
},
{
"cost": "1.2",
"description": "Alphanate 250-500 unit vial",
"unit": "vial"
},
{
"cost": "1.2",
"description": "Humate-p 1000 unit kit",
"unit": "kit"
},
{
"cost": "1.2",
"description": "Humate-p 1200 unit kit",
"unit": "kit"
},
{
"cost": "1.2",
"description": "Humate-p 2000 unit kit",
"unit": "kit"
},
{
"cost": "1.2",
"description": "Humate-p 2400 unit kit",
"unit": "kit"
},
{
"cost": "1.2",
"description": "Humate-p 500 unit kit",
"unit": "kit"
},
{
"cost": "1.2",
"description": "Humate-p 600 unit kit",
"unit": "kit"
},
{
"cost": "1.31",
"description": "Koate-dvi 1000 unit kit",
"unit": "kit"
},
{
"cost": "1.31",
"description": "Koate-dvi 250 unit kit",
"unit": "kit"
},
{
"cost": "1.31",
"description": "Koate-dvi 500 unit kit",
"unit": "kit"
},
{
"cost": "1.31",
"description": "Refacto 1000 unit vial",
"unit": "vial"
},
{
"cost": "1.31",
"description": "Refacto 2000 unit vial",
"unit": "vial"
},
{
"cost": "1.31",
"description": "Refacto 250 unit vial",
"unit": "vial"
},
{
"cost": "1.31",
"description": "Refacto 500 unit vial",
"unit": "vial"
},
{
"cost": "1.34",
"description": "Hemofil m 1701-2000 unit vial",
"unit": "vial"
},
{
"cost": "1.34",
"description": "Hemofil m 220-400 unit vial",
"unit": "vial"
},
{
"cost": "1.34",
"description": "Hemofil m 401-800 unit vial",
"unit": "vial"
},
{
"cost": "1.34",
"description": "Hemofil m 801-1700 unit vial",
"unit": "vial"
},
{
"cost": "1.38",
"description": "Wilate 450-450 unit kit",
"unit": "kit"
},
{
"cost": "1.38",
"description": "Wilate 900-900 unit kit",
"unit": "kit"
},
{
"cost": "1.56",
"description": "Helixate fs 1000 unit vial",
"unit": "vial"
},
{
"cost": "1.56",
"description": "Helixate fs 250 unit vial",
"unit": "vial"
},
{
"cost": "1.56",
"description": "Helixate fs 3000 unit vial",
"unit": "vial"
},
{
"cost": "1.56",
"description": "Helixate fs 500 unit vial",
"unit": "vial"
},
{
"cost": "1.66",
"description": "Xyntha 1000 unit kit",
"unit": "kit"
},
{
"cost": "1.66",
"description": "Xyntha 2000 unit kit",
"unit": "kit"
},
{
"cost": "1.66",
"description": "Xyntha 250 unit kit",
"unit": "kit"
},
{
"cost": "1.66",
"description": "Xyntha 500 unit kit",
"unit": "kit"
},
{
"cost": "1.68",
"description": "Advate 1201-1800 unit vial",
"unit": "vial"
},
{
"cost": "1.68",
"description": "Advate 1801-2400 unit vial",
"unit": "vial"
},
{
"cost": "1.68",
"description": "Advate 200-400 unit vial",
"unit": "vial"
},
{
"cost": "1.68",
"description": "Advate 2400-3600 unit vial",
"unit": "vial"
},
{
"cost": "1.68",
"description": "Advate 401-800 unit vial",
"unit": "vial"
},
{
"cost": "1.68",
"description": "Advate 801-1200 unit vial",
"unit": "vial"
},
{
"cost": "1.68",
"description": "Kogenate fs 1000 unit vial",
"unit": "vial"
},
{
"cost": "1.68",
"description": "Kogenate fs 250 unit vial",
"unit": "vial"
},
{
"cost": "1.68",
"description": "Kogenate fs 3000 unit vial",
"unit": "vial"
},
{
"cost": "1.68",
"description": "Kogenate fs 500 unit vial",
"unit": "vial"
}
] |
[
{
"approved": "2007-09-11",
"country": "Canada",
"expires": "2013-10-01",
"number": "2124690"
},
{
"approved": "1997-09-23",
"country": "Canada",
"expires": "2014-09-23",
"number": "1339477"
}
] |
Antihemophilic factor (recombinant) | Antihemophilic factor recombinant | Antihemophilic factor, human recombinant | Antihemophilic factor, recombinant | Coagulation factor VIII, recombinant | Factor VIII (rDNA) | Factor VIII (Recombinant) | Factor VIII recombin | Factor VIII, recombinant | Human Factor VIII (Recombinant) | Human factor VIII recombinant | Octocog alfa | rAHF | Recombinant antihemophilic factor VIII | 3.4.21.6 | Stuart factor | Stuart-Prower factor | 3.4.21.22 | Christmas factor | Plasma thromboplastin component | PTC | F8VWF | vWF | 1.14.11.18 | PAHX | PhyH | Phytanic acid oxidase | Phytanoyl-CoA alpha-hydroxylase | ASGP-R 2 | ASGPR 2 | C-type lectin domain family 4 member H2 | CLEC4H2 | Hepatic lectin H2 | HL-2 | 3.6.4.10 | 78 kDa glucose-regulated protein | Binding-immunoglobulin protein | BiP | GRP-78 | GRP78 | Heat shock protein 70 family protein 5 | Heat shock protein family A member 5 | HSP70 family protein 5 | Immunoglobulin heavy chain-binding protein | Calregulin | CRP55 | CRTC | Endoplasmic reticulum resident protein 60 | ERp60 | grp60 | HACBP | IP90 | Major histocompatibility complex class I antigen-binding protein p88 | p90 | ER-Golgi intermediate compartment 53 kDa protein | ERGIC53 | F5F8D | Gp58 | Intracellular mannose-specific lectin MR60 | Lectin mannose-binding 1 | A2MR | Alpha-2-macroglobulin receptor | APOER | Apolipoprotein E receptor | APR | LRP-1 | Neural stem cell-derived neuronal survival protein | SDNSF | 3.4.21.5 | Coagulation factor II | 3.4.21.69 | Anticoagulant protein C | Autoprothrombin IIA | Blood coagulation factor XIV
|
[
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Advate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Adynovate",
"Esperoct",
"Esperoct",
"Helixate FS",
"Helixate FS",
"Helixate FS",
"Helixate FS",
"Helixate FS",
"Helixate FS",
"Helixate FS",
"Helixate FS",
"Helixate FS",
"Helixate FS",
"Helixate Nexgen",
"Helixate Nexgen",
"Helixate Nexgen",
"Helixate Nexgen",
"Helixate Nexgen",
"Iblias",
"Iblias",
"Iblias",
"Iblias",
"Iblias",
"Kogenate - Pws IV 1000I.U./vial",
"Kogenate - Pws IV 250I.U./vial",
"Kogenate - Pws IV 500I.U./vial",
"Kogenate Bayer",
"Kogenate Bayer",
"Kogenate Bayer",
"Kogenate Bayer",
"Kogenate Bayer",
"Kogenate Bayer",
"Kogenate Bayer",
"Kogenate Bayer",
"Kogenate Bayer",
"Kogenate Bayer",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS",
"Kogenate FS -(with Bio-set)",
"Kogenate FS -(with Bio-set)",
"Kogenate Pws 1000iu/vial",
"Kogenate Pws 250iu/vial",
"Kogenate Pws 500iu/vial",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Kovaltry",
"Novoeight",
"Novoeight",
"Novoeight",
"Novoeight",
"Novoeight",
"Novoeight",
"Recombinate",
"Recombinate",
"Recombinate",
"Recombinate",
"Recombinate",
"Recombinate",
"Recombinate",
"Recombinate",
"Recombinate Pws Inj 1000I.U./vial",
"Recombinate Pws Inj 250I.U./vial",
"Recombinate Pws Inj 500I.U./vial"
] |
[
"Bioclate",
"Helixate",
"Hyate:C",
"Koate-HP",
"Kogenate",
"Monarc-M",
"ReFacto"
] |
[] |
[
"P00742",
"P00740",
"P04275",
"O14832",
"P07307",
"P11021",
"P27797",
"P27824",
"P49257",
"Q07954",
"Q8NI22"
] |
[
"P00734",
"P04070"
] |
[] |
[] |
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