<clinical_study>
  <!-- This xml conforms to an XML Schema at:
    https://clinicaltrials.gov/ct2/html/images/info/public.xsd -->
  <required_header>
    <download_date>ClinicalTrials.gov processed this data on September 20, 2023</download_date>
    <link_text>Link to the current ClinicalTrials.gov record.</link_text>
    <url>https://clinicaltrials.gov/ct2/show/NCT01697020</url>
  </required_header>
  <id_info>
    <org_study_id>INV298</org_study_id>
    <nct_id>NCT01697020</nct_id>
  </id_info>
  <brief_title>Bioequivalence of An Oral Mercaptopurine Suspension 100 Mg / 5 Ml Versus Tablet in Healthy Male Subjects Under Fasting Conditions</brief_title>
  <official_title>A SINGLE CENTER, SINGLE-DOSE, OPEN-LABEL, RANDOMIZED, TWO-PERIOD CROSSOVER STUDY TO ASSESS THE BIOEQUIVALENCE OF AN ORAL MERCAPTOPURINE SUSPENSION 100 mg / 5 mL VERSUS AN ORAL MERCAPTOPURINE TABLET 50 mg (PURINETHOL®) IN AT LEAST 62 HEALTHY MALE SUBJECTS UNDER FASTING CONDITIONS</official_title>
  <sponsors>
    <lead_sponsor>
      <agency>Nova Laboratories Limited</agency>
      <agency_class>Industry</agency_class>
    </lead_sponsor>
  </sponsors>
  <source>Nova Laboratories Limited</source>
  <oversight_info>
    <has_dmc>No</has_dmc>
  </oversight_info>
  <brief_summary>
    <textblock>
      The primary objective of this study is to determine whether the test product, mercaptopurine&#xD;
      oral 100 mg/5 mL suspension, and the reference product, Purinethol® 50 mg tablets are&#xD;
      bioequivalent. For this purpose the PK profile of 6-mercaptopurine (6-MP) will be compared&#xD;
      after administration of a single dose of each of the two formulations, under fasting&#xD;
      conditions. The secondary objective is to assess the safety and tolerability of the test&#xD;
      product, mercaptopurine oral 100 mg/5 mL suspension.&#xD;
    </textblock>
  </brief_summary>
  <overall_status>Completed</overall_status>
  <start_date>September 2012</start_date>
  <completion_date type="Actual">November 2012</completion_date>
  <primary_completion_date type="Actual">November 2012</primary_completion_date>
  <phase>Phase 1</phase>
  <study_type>Interventional</study_type>
  <has_expanded_access>No</has_expanded_access>
  <study_design_info>
    <allocation>Randomized</allocation>
    <intervention_model>Crossover Assignment</intervention_model>
    <primary_purpose>Treatment</primary_purpose>
    <masking>None (Open Label)</masking>
  </study_design_info>
  <primary_outcome>
    <measure>Bioequivalence</measure>
    <time_frame>Within 7 days</time_frame>
    <description>At each treatment period, pharmacokinetic blood samples will be collected through the indwelling venous cannula at the following times: pre-dose and post-dose at 0.17, 0.33, 0.5, 0.75, 1.0, 1.33, 1.67, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 7.0, 8.0, 10.0 and 12.0 hours.&#xD;
The primary outcome measures will be&#xD;
Maximum observed plasma concentration (Cmax).&#xD;
AUC time zero to time of the last quantifiable concentration (AUC(0-t))&#xD;
Area under the plasma concentration versus time data pairs, with extrapolation to infinity (AUC(0-∞)).</description>
  </primary_outcome>
  <number_of_arms>2</number_of_arms>
  <enrollment type="Actual">70</enrollment>
  <condition>Acute Lymphoblastic Leukemia</condition>
  <arm_group>
    <arm_group_label>Arm 1</arm_group_label>
    <arm_group_type>Experimental</arm_group_type>
    <description>Mercaptopurine 20mg/ml Oral Suspension</description>
  </arm_group>
  <arm_group>
    <arm_group_label>Arm 2</arm_group_label>
    <arm_group_type>Active Comparator</arm_group_type>
    <description>Mercaptopurine 50mg tablets</description>
  </arm_group>
  <intervention>
    <intervention_type>Drug</intervention_type>
    <intervention_name>Mercaptopurine 20mg/ml oral suspension</intervention_name>
    <description>50mg</description>
    <arm_group_label>Arm 1</arm_group_label>
    <other_name>Xaluprine</other_name>
  </intervention>
  <intervention>
    <intervention_type>Drug</intervention_type>
    <intervention_name>Mercaptopurine 50mg tablet</intervention_name>
    <description>50mg</description>
    <arm_group_label>Arm 2</arm_group_label>
    <other_name>Purinethol</other_name>
  </intervention>
  <eligibility>
    <criteria>
      <textblock>
        Inclusion Criteria:&#xD;
&#xD;
          -  Healthy male subjects, 18 years to 50 years inclusive at time of last administration&#xD;
             of the IMP.&#xD;
&#xD;
          -  Body Mass Index (BMI) between 18.5 and 30 kg/m2.&#xD;
&#xD;
          -  Body mass not less than 50 kg.&#xD;
&#xD;
          -  Medical history, physical examination, standard 12-lead electrocardiogram (ECG) and&#xD;
             laboratory investigations: Findings clinically acceptable or within laboratory&#xD;
             reference ranges for the relevant laboratory tests, unless the investigator considers&#xD;
             the deviation to be irrelevant for the purpose of the study.&#xD;
&#xD;
          -  Non-smokers.&#xD;
&#xD;
        Exclusion Criteria:&#xD;
&#xD;
          -  Current alcohol use &gt; 21 units of alcohol per week for males.&#xD;
&#xD;
          -  Regular exposure to substances of abuse (other than alcohol) within the past year.&#xD;
&#xD;
          -  Use of any medication, prescribed or over-the-counter or herbal remedies, within 2&#xD;
             weeks prior to the first administration of IMP except if this will not affect the&#xD;
             outcome of the study in the opinion of the investigator.&#xD;
&#xD;
          -  Participation in another study with an experimental drug, where the last&#xD;
             administration of the previous IMP was within 8 weeks before the first administration&#xD;
             of IMP in this study.&#xD;
&#xD;
          -  Treatment within the previous 3 months before the first administration of IMP with any&#xD;
             drug with a well-defined potential for adversely affecting a major organ or system.&#xD;
&#xD;
          -  A major illness during the 3 months before commencement of the screening period.&#xD;
&#xD;
          -  Subjects with a deficient, low or intermediate TPMT enzyme activity by means of&#xD;
             phenotyping.&#xD;
&#xD;
          -  Subjects who participated in previous azathioprine/mercaptopurine studies within six&#xD;
             months will be excluded.&#xD;
&#xD;
          -  Relevant history or laboratory or clinical findings indicative of acute or chronic&#xD;
             disease, likely to influence study outcome.&#xD;
&#xD;
          -  Donation or loss of blood equal to or exceeding 500 mL during the 8 weeks before the&#xD;
             first administration of IMP.&#xD;
&#xD;
          -  Diagnosis of hypotension or hypertension made during the screening period or current&#xD;
             diagnosis of hypertension.&#xD;
&#xD;
          -  Resting pulse of &gt; 100 beats per minute or &lt; 45 beats per minute during the screening&#xD;
             period, either supine or standing.&#xD;
&#xD;
          -  Positive testing for HIV and/or Hepatitis B and/or Hepatitis C.&#xD;
&#xD;
          -  Positive urine screen for drugs of abuse.&#xD;
&#xD;
          -  Positive urine screen for tobacco use.&#xD;
&#xD;
          -  Subjects who plan to procreate within 12 weeks after IMP administration, or not&#xD;
             willing to practice reliable forms of contraception during the study and for at least&#xD;
             12 weeks after the last dose of IMP.&#xD;
&#xD;
          -  Immunization using a live organism vaccine within 4 weeks prior to the first dosing of&#xD;
             IMP.&#xD;
&#xD;
          -  Any specific IMP safety concern.&#xD;
      </textblock>
    </criteria>
    <gender>Male</gender>
    <minimum_age>18 Years</minimum_age>
    <maximum_age>50 Years</maximum_age>
    <healthy_volunteers>Accepts Healthy Volunteers</healthy_volunteers>
  </eligibility>
  <location>
    <facility>
      <name>Parexel International, Bloemfontein Early Phase Clinical Unit</name>
      <address>
        <city>Bloemfontein</city>
        <country>South Africa</country>
      </address>
    </facility>
  </location>
  <location_countries>
    <country>South Africa</country>
  </location_countries>
  <verification_date>November 2013</verification_date>
  <study_first_submitted>September 20, 2012</study_first_submitted>
  <study_first_submitted_qc>September 26, 2012</study_first_submitted_qc>
  <study_first_posted type="Estimate">October 2, 2012</study_first_posted>
  <last_update_submitted>November 28, 2013</last_update_submitted>
  <last_update_submitted_qc>November 28, 2013</last_update_submitted_qc>
  <last_update_posted type="Estimate">December 2, 2013</last_update_posted>
  <responsible_party>
    <responsible_party_type>Sponsor</responsible_party_type>
  </responsible_party>
  <condition_browse>
    <!-- CAUTION:  The following MeSH terms are assigned with an imperfect algorithm            -->
    <mesh_term>Precursor Cell Lymphoblastic Leukemia-Lymphoma</mesh_term>
  </condition_browse>
  <intervention_browse>
    <!-- CAUTION:  The following MeSH terms are assigned with an imperfect algorithm            -->
    <mesh_term>Mercaptopurine</mesh_term>
  </intervention_browse>
  <pending_results>
    <submitted>April 3, 2020</submitted>
    <returned>April 15, 2020</returned>
  </pending_results>
  <!-- Results have not yet been posted for this study                                          -->
</clinical_study>


download date: ClinicalTrials.gov processed this data on September 20, 2023
link text: Link to the current ClinicalTrials.gov record.
url: https://clinicaltrials.gov/ct2/show/NCT01697020
org study id: INV298
nct id: NCT01697020
lead sponsor: 
has dmc: No
The primary objective of this study is to determine whether the test product, mercaptopurine
      oral 100 mg/5 mL suspension, and the reference product, Purinethol® 50 mg tablets are
      bioequivalent. For this purpose the PK profile of 6-mercaptopurine (6-MP) will be compared
      after administration of a single dose of each of the two formulations, under fasting
      conditions. The secondary objective is to assess the safety and tolerability of the test
      product, mercaptopurine oral 100 mg/5 mL suspension.
allocation: Randomized
intervention model: Crossover Assignment
primary purpose: Treatment
masking: None (Open Label)
measure: Bioequivalence
time frame: Within 7 days
description: At each treatment period, pharmacokinetic blood samples will be collected through the indwelling venous cannula at the following times: pre-dose and post-dose at 0.17, 0.33, 0.5, 0.75, 1.0, 1.33, 1.67, 2.0, 2.5, 3.0, 3.5, 4.0, 4.5, 5.0, 6.0, 7.0, 8.0, 10.0 and 12.0 hours.
The primary outcome measures will be
Maximum observed plasma concentration (Cmax).
AUC time zero to time of the last quantifiable concentration (AUC(0-t))
Area under the plasma concentration versus time data pairs, with extrapolation to infinity (AUC(0-∞)).
arm group label: Arm 1
arm group type: Experimental
description: Mercaptopurine 20mg/ml Oral Suspension
arm group label: Arm 2
arm group type: Active Comparator
description: Mercaptopurine 50mg tablets
intervention type: Drug
intervention name: Mercaptopurine 20mg/ml oral suspension
description: 50mg
arm group label: Arm 1
other name: Xaluprine
intervention type: Drug
intervention name: Mercaptopurine 50mg tablet
description: 50mg
arm group label: Arm 2
other name: Purinethol
criteria: 
gender: Male
minimum age: 18 Years
maximum age: 50 Years
healthy volunteers: Accepts Healthy Volunteers
facility: 
country: South Africa
responsible party type: Sponsor
mesh term: Precursor Cell Lymphoblastic Leukemia-Lymphoma
mesh term: Mercaptopurine
submitted: April 3, 2020
returned: April 15, 2020