Pharmacology
Pharmacodynamics
Darolutamide is a second- or third-generation nonsteroidal antiandrogen (NSAA). It acts as a selective competitive silent antagonist of the androgen receptor (AR), the biological target of androgens like testosterone and dihydrotestosterone (DHT). Its affinity (Ki) for the AR is 11 nM and its functional inhibition (IC50) of the AR is 26 nM. The major metabolite of darolutamide, ketodarolutamide, has similar antiandrogenic activity relative to darolutamide (Ki = 8 nM; IC50 = 38 nM). In addition to its actions as an AR antagonist, darolutamide has been found to act as a silent antagonist of the progesterone receptor (PR), with approximately 1% of the potency of its AR antagonism.A dosage of darolutamide of 1,200 mg/day has been found to result in a mean decrease in prostate specific antigen (PSA) levels of more than 90% in men with prostate cancer. The addition of darolutamide to castration has been found to decrease PSA levels by more than 50% in about 50% of men at 200 mg/day, 69% of men at 400 mg/day, 83% of men at 1,200 mg/day, and 86% of men at 1,400 mg/day.Darolutamide shows some advantages in comparison to enzalutamide and apalutamide, two other second-generation NSAAs. It appears to negligibly cross the blood–brain barrier, and hence has reduced risk of seizures and other central side effects from off-target GABAA receptor inhibition. In accordance with its diminished central penetration, darolutamide does not appear to increase testosterone levels.
However, EEs and CEEs differ in the sources of their contents and in the percentages of their constituents; CEEs consist of approximately 53% sodium estrone sulfate and 25% sodium equilin sulfate, while EEs contain about 75 to 85% sodium estrone sulfate and 6 to 11% sodium equilin sulfate. EEs have been found to produce similar serum levels of estrone and estradiol relative to CEEs, although with higher levels of estrone and lower levels of equilin. One study found that the risk of venous thrombosis may be less with EEs relative to CEEs. Chemistry
EEs contain synthetic, plant-derived estrogens and are manufactured from soybeans and yams. History
EEs were introduced for medical use by 1970. Society and culture
Generic names
Estrogens, esterified is the generic name of the drug and its USP. It is also known as esterified estrogens. Brand names
EEs are marketed under a variety of brand names including Amnestrogen, Estragyn, Estratab, Evex, Femibel, Femogen, Menest, Neo Estrone Tab, and Oestro-Feminal alone, and, in combination with methyltestosterone, under the brand names Covaryx, Delitan, Eemt, Essian, Estratest, Feminova-T, Menogen, and Syntest. Availability
EEs are or have been marketed in Argentina, Chile, Switzerland, and the United States. Both EEs and the combination of EEs and methyltestosterone are listed as being marketed only in Chile and the United States as of present. See also
Esterified estrogens/methyltestosterone
Estrogenic substances
Conjugated estriol
List of combined sex-hormonal preparations


== References ==