Like other AAS, drostanolone is an agonist of the androgen receptor (AR).  It is not a substrate for 5α-reductase and is a poor substrate for 3α-hydroxysteroid dehydrogenase (3α-HSD), and therefore shows a high ratio of anabolic to androgenic activity.  As a DHT derivative, drostanolone is not a substrate for aromatase and hence cannot be aromatized into estrogenic metabolites .  While no data are available on the progestogenic activity of drostanolone, it is thought to have low or no such activity similarly to other DHT derivatives.  Since the drug is not 17α-alkylated , it is not known to cause hepatotoxicity . 
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It was in late 2005 that the status of methasterone, in addition to that of four other designer steroids, as an AAS was brought to public awareness by an article published in the Washington Post .  Don Catlin of the UCLA Olympic Laboratory, who conducted the studies, noted methasterone’s similarity to drostanolone. A warning by the FDA was issued soon after to the general public as well as to the distributor, Designer Supplements LLC, for the marketing of this compound.  Methasterone was subsequently added to the World Anti-Doping Agency (WADA) list of prohibited substances in sport.  Despite all of this, methasterone has resurfaced within the supplement industry on several occasions since its banning by WADA.