Methasterone is an oral anabolic steroid

Anabolic steroid

Anabolic steroids, technically known as anabolic-androgen steroids or colloquially simply as "steroids", are drugs that mimic the effects of testosterone and dihydrotestosterone in the body. They increase protein synthesis within cells, which results in the buildup of cellular tissue ,...

 that was never marketed through legitimate channels for medicinal purposes. It was brought to market, instead, in a clandestine fashion as a “designer steroid

Designer drug

Designer drug is a term used to describe drugs that are created to get around existing drug laws, usually by preparing analogs or derivatives of existing drugs by modifying their chemical structure to varying degrees, or less commonly by finding drugs with entirely different chemical structures...

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History

The synthesis of methasterone is first mentioned in the literature in 1956 in connection with research conducted by Syntex Corporation

Syntex

Laboratorios Syntex SA was a pharmaceutical company formed in Mexico City in 1944 by Russell Marker to manufacture therapeutic steroids from the Mexican yam....

 in order to discover a compound with anti-tumor properties. This initial mention is elaborated upon in a 1959 research journal article, where its method of synthesis is discussed in greater detail, its tumor inhibiting properties are verified, and it is noted as being a “potent orally active anabolic agent exhibiting only weak androgenic activity.” The results of subsequent assays to determine methasterone’s anabolic and androgenic activity were published in Vida’s Androgens and Anabolic Agents, a dated but still standard reference, where it was noted that methasterone possessed the oral bioavailability of methyl-testosterone while being 400% as anabolic and 20% as androgenic, yielding a Q-ratio (also known as an anabolic to androgenic ratio) of 20, which is considered very high.

Injectable counterpart

Methasterone was never a commercially available prescription drug. Its non-17α-alkylated counterpart, drostanolone

Drostanolone

Drostanolone is an anabolic steroid. Its main medical applications are to lower cholesterol levels, and as an antineoplastic agent in the treatment of some cancers. It is most commonly marketed as the ester drostanolone propionate .Ringold, H. J.; Batres, E.; Halpern, O.; Necoechea, E.; J. Amer....

, was commercialized by Syntex Corporation under the brand name Masteron.

"Designer steroid"

Methasterone resurfaced in 2005 as a “designer steroid”. It was brought to market by Anabolic Xtreme as the primary ingredient of a dietary supplement named Superdrol. Its introduction into commerce may have represented an attempted circumvention of the 1990 Anabolic Steroid Control Act (along with its 2004 revision), since the law is, in part, drug-specific; methasterone, as is the case with many designer steroids, was not declared a Schedule III class anabolic steroid in that act because it was not commercially available at the time the act, and its subsequent revision, were signed into law. Methasterone was therefore being sold as an over-the-counter dietary supplement.

Controversy and FDA involvement

It was in late 2005 that the status of methasterone (Superdrol), in addition to that of four other designer steroids, as a genuine anabolic steroid 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’s list of prohibited substances in sport.. Despite all of this, methasterone (Superdrol) has resurfaced within the supplement industry on several accusations since its banning by WADA

Anabolic efficacy

The anabolic efficacy of this compound can be attested to anecdotally on the many forums online where anabolic drug use practices are openly discussed, as can its hepatoxicity (toxicity to the liver). Many cases of liver damage due to the use of methasterone have been cited in the medical literature. Although the original manufacturer ceased production in the face of possible governmental action, methasterone remains commercially available through over-the-counter dietary supplement products sometimes referred to as “Superdrol clones” and through domestic or foreign chemical production companies.