Methasterone (Superdrol)

Overview

Methasterone — sold under the brand name "Superdrol" — is an anabolic-androgenic steroid (AAS). It is NOT a SARM and it is NOT a peptide. Chemically it is 17α-methyldrostanolone (2α,17α-dimethyl-5α-dihydrotestosterone), a 17α-alkylated oral steroid derived from DHT (PubChem CID 237186, CAS 3381-88-2, C21H34O2, MW 318.5 g/mol).

It was never approved as a medicine. It emerged as a "designer steroid" sold as a bodybuilding supplement, and it is frequently marketed as — or alongside — "SARMs" and "prohormones" to imply a mild, low-risk profile. That framing is false. Methasterone is a full anabolic steroid, and it is the opposite of mild: it is a documented cause of severe cholestatic liver injury.

If you have seen this compound described as a "mild SARM" or as "safer than steroids," that description is wrong. It is a steroid, and a particularly hepatotoxic one.

[!WARNING] Methasterone is a 17α-alkylated oral anabolic steroid and a documented cause of severe cholestatic drug-induced liver injury — including jaundice and marked hyperbilirubinemia in previously healthy young men. It also suppresses natural testosterone, worsens cholesterol/cardiovascular risk, and causes virilization. It was never approved for human use and is a US Schedule III controlled anabolic steroid. This page is educational only — not medical, legal, or dosing advice.

Chemistry and structure

The defining structural feature is 17α-alkylation — a methyl group at the 17α position. This is the chemical trick that lets a steroid survive first-pass liver metabolism and remain active when taken by mouth. It is also the same feature that drives the characteristic hepatotoxicity of oral AAS.

Mechanism of action

• Full agonist at the androgen receptor (AR) as an anabolic-androgenic steroid; it is a DHT-derived molecule (2α,17α-dimethyl-5α-DHT), not a selective or tissue-partial SARM. [Mechanism]
• 17α-alkylation blocks first-pass hepatic metabolism to allow oral activity — the same structural feature that drives its characteristic hepatotoxicity (cholestasis). [Mechanism]
• As an exogenous androgen it suppresses the hypothalamic-pituitary-testicular (HPTA) axis, lowering endogenous testosterone and gonadotropins (a class effect of oral AAS). [Mechanism]

The key contrast with a true SARM: SARMs are selective androgen receptor modulators intended to act as tissue-partial agonists. Methasterone is a full steroid with no such selectivity — it is a classic anabolic-androgenic steroid.

Research and evidence

There is little legitimate efficacy data for methasterone in humans. It was never developed or approved as a therapeutic drug, so there are no controlled trials establishing benefit, dose, or safety margin.

What does exist in the human literature is a record of harm — chiefly case reports of liver injury. The most cited is a published five-case series (Shah et al., Clinical Gastroenterology and Hepatology, 2008; PMID 18187367) describing previously healthy men who developed cholestatic liver injury with jaundice after using a methasterone-containing supplement, with bilirubin peaking over the following weeks. [Human]

More broadly, NIH LiverTox documents that 17α-alkylated androgenic steroids as a class are implicated in prolonged cholestasis, peliosis hepatis, nodular regeneration, and — with long-term use — hepatic adenomas and hepatocellular carcinoma. [Human]

Status and regulation

Methasterone is not an approved medicine. It was never evaluated or approved for human therapeutic use anywhere, so there is no established safe dose and no approved-drug pharmacokinetic data (including no established human half-life).

In the United States it is a Schedule III controlled anabolic steroid, formally scheduled in 2012 (DEA final rule classifying prostanozol and methasterone). The Designer Anabolic Steroid Control Act of 2014 later broadened federal control of designer steroids and criminalized false labeling of products containing them.

In sport, methasterone is prohibited by WADA as an exogenous anabolic androgenic steroid (S1.1a).

Safety

Liver injury is the headline harm. Methasterone is a documented cause of severe cholestatic drug-induced liver injury / cholestatic hepatitis — jaundice and marked hyperbilirubinemia — driven by its 17α-alkylation. Reported cases involve previously healthy young men. [Human]

Other documented and class-level harms of oral AAS:

• HPTA / endogenous testosterone suppression — a class effect of exogenous oral AAS; natural testosterone and gonadotropins fall. [Human]
• Adverse lipid / cardiovascular effects — 17α-alkylated oral AAS are associated with marked HDL suppression and cardiovascular risk. [Human]
• Virilization — androgenic effects, especially in women; some features (e.g. voice changes) can be irreversible. [Human]
• Renal injury — reported in at least one case (cholestasis with renal failure). [Human]
• Long-term tumor/peliosis risk — noted at class level for 17α-alkylated AAS (adenoma, hepatocellular carcinoma, peliosis hepatis); methasterone-specific long-term carcinogenicity data is Not established. [Human]

Adulteration and contamination. Methasterone is frequently the undeclared adulterant found inside products sold as "SARMs" or "prohormones." A 2017 JAMA analysis of products marketed as SARMs online (Van Wagoner et al., PMID 29183075) found that many did not contain what their labels claimed and some contained unapproved drugs. A label is not a reliable statement of contents — a product marketed as a "SARM" or a mild "prohormone" may actually contain a full anabolic steroid such as methasterone.

[!WARNING] There is no established safe dose of methasterone. It was never approved for human use, it is a documented liver toxin, and it is often hidden inside products labeled as something milder. Treat any "SARM" or "prohormone" product as potentially adulterated with a steroid like this one.

Legal status

Methasterone is a US Schedule III controlled anabolic steroid (scheduled 2012), and the Designer Anabolic Steroid Control Act of 2014 further tightened US federal control of designer steroids and false labeling. Controlled-substance status is distinct from anti-doping rules: separately, WADA prohibits it in sport as an exogenous AAS (S1.1a).

Legal status varies by country and changes over time, and this page does not assess the law in your jurisdiction. This is educational information, not legal advice — check the rules where you are.

How it compares

Methasterone is often shelved next to, or sold as, "SARMs" — but it is chemically and pharmacologically a different (and blunter) thing.

• True SARMs such as ostarine and testolone are non-steroidal selective androgen receptor modulators; WADA classes them under S1.2. They are still investigational and carry their own risks, but they are not 17α-alkylated steroids.
• Methasterone is a full anabolic-androgenic steroid — a 17α-alkylated oral DHT derivative — classed by WADA under S1.1 (exogenous AAS). It carries the hepatotoxicity profile characteristic of oral steroids, not of SARMs.

The practical point: if a product is marketed as a "SARM" but actually contains methasterone, the buyer is exposed to steroid-grade liver risk while believing they took something milder.

Common misconceptions

• "It's a mild SARM." False on two counts. It is not a SARM at all — it is an anabolic-androgenic steroid — and it is not mild; it is a documented cause of severe cholestatic liver injury.
• "It's safer than steroids." It is a steroid, and a particularly hepatotoxic 17α-alkylated oral one. There is nothing "safer than steroids" about it.
• "It's basically a prohormone/supplement." It was sold as a supplement, but it is a controlled anabolic steroid that was never approved for human use.
• "The label tells me what's in it." Products in this category are frequently mislabeled or adulterated. A label claiming "SARM" or "prohormone" is not a reliable statement of contents.