Pharmacodynamics Like other AAS,<unk>  is an agonist of the androgen receptor (AR).<unk>  is described as a very poor anabolic agent due to inactivation by 3α-hydroxysteroid dehydrogenase (3α-HSD) in skeletal muscle tissue, similarly to DHT and mestanolone (17α-methyl-DHT). In contrast, testosterone is a very poor substrate for 3α-HSD, and so is not similarly inactivated in skeletal muscle. Because of its lack of potentiation by 5α-reductase in "androgenic" tissues and its inactivation by 3α-HSD in skeletal muscle,<unk>  is relatively low in both its androgenic potency and its anabolic potency. However, it does still show a greater ratio of anabolic activity to androgenic activity relative to testosterone.<unk>  is not a substrate for 5α-reductase, as it is already 5α-reduced, and hence is not potentiated in so-called "androgenic" tissues such as the skin, hair follicles, and prostate gland.<unk>  is not a substrate for aromatase, and so cannot be converted into an estrogen. As such, it has no propensity for producing estrogenic side effects such as gynecomastia and fluid retention. It also has no progestogenic activity. Because<unk>  is not 17α-alkylated, it has little or no potential for hepatotoxicity. However, its risk of deleterious effects on the cardiovascular system is comparable to that of several other oral AAS. Pharmacokinetics The C1α methyl group of<unk>  inhibits its hepatic metabolism and thereby confers significant oral activity, although its oral bioavailability is still much lower than that of 17α-alkylated AAS. In any case,<unk>  is one of the few non-17α-alkylated AAS that is active with oral ingestion. Uniquely among AAS,<unk>  has very high affinity for human serum sex hormone-binding globulin (SHBG), about 440% that of DHT in one study and 82% of that of DHT in another study. As a result, it may displace endogenous testosterone from SHBG and thereby increase free testosterone concentrations, which may in part be involved in its effects.
Mesterolone
Vardenafil
Metenolone
Clascoterone
Avanafil
Dexrazoxane
Oleandrin
Ingenol mebutate