Educational reference only. Informational material drawn from peer-reviewed literature. Not medical advice and not a recommendation to use, dose, or modify any therapy. Decisions about hormone therapy should be made with a qualified healthcare provider.
Overview
Overview
Methasterone, most commonly known by the trade name Superdrol, is a synthetic anabolic-androgenic steroid (AAS) and one of the most clinically documented examples of severe hepatotoxicity from a designer steroid. The compound was originally synthesized in the 1950s but never approved for medical use in any jurisdiction. It existed in academic literature for decades before reappearing dramatically in 2005 when it was marketed in the United States as an "over-the-counter dietary supplement" under the name Superdrol (a portmanteau of "super" and "Anadrol"), exploiting a regulatory loophole in the pre-2014 supplement industry.
Within months of widespread availability, case reports of severe hepatotoxicity began appearing in medical literature. Between 2005 and 2012 (when methasterone was finally added to Schedule III by the Designer Anabolic Steroid Control Act of 2014), multiple cases of cholestatic jaundice, acute liver failure, and acute renal failure were documented in previously healthy young men. The compound's reputation as one of the most hepatotoxic AAS in modern use is supported by an unusually large case report literature.
The compound has no injectable form in common use. All use is oral.
Forms
Available forms & half-lives
| Form | Approximate half-life |
|---|---|
| Oral tablet (not esterified) | ~8–12 hours |
What it does
Main effects
- Strong androgen receptor mediated activity: essentially "orally bioavailable Masteron", with the C2α methyl modification contributing to potency
- No aromatization to estrogen: inherited from drostanolone; no water retention, no estrogen-mediated gynecomastia
- Orally bioavailable via 17α-methyl modification (which is also the source of the severe hepatic risk)
- Resistance to 3α-HSD inactivation in muscle tissue (inherited from drostanolone's C2α methyl)
- "Dry, hard" muscle appearance commonly described in non-medical use, consistent with the absence of aromatization
What to watch for
Common side effects
- Severe hepatotoxicity at typical use doses: the defining safety concern; over 50 documented cases of methasterone-associated drug-induced liver injury PMC: 7678230; cholestatic jaundice, acute liver failure, and hepatic failure requiring transplantation all documented
- Post-cycle hepatic injury pattern, characteristic and insidious: jaundice frequently develops 2 weeks AFTER discontinuation, peaks 4–6 weeks after stopping; users may believe they "got away with it" until weeks later
- Acute renal failure: unusual feature for an AAS; IgA nephropathy documented; cases requiring dialysis have occurred
- Profound HPG axis suppression even at low doses
- Dramatic lipid changes: HDL reductions of 40–60% commonly reported; LDL elevations of similar magnitude
- Severe acne and androgenic skin effects
- Aggressive scalp hair loss in genetically predisposed users; 5α-reductase inhibitors do not protect (already 5α-reduced)
- Rapid, severe virilization in women: contraindicated for female use
- Underground / adulterated-supplement supply: despite being scheduled in 2014, methasterone continues to appear in unregulated products and international supplements; legacy of the "Superdrol" supplement era persists
Key facts
Key facts worth knowing
- Methasterone is structurally drostanolone (Masteron) with 17α-methylation added, making it essentially "orally bioavailable Masteron." This combination produces an orally active compound with strong androgen receptor mediated activity together with the severe hepatotoxicity inherited from the 17α-alkylation.
- The 2005-2012 "Superdrol era" produced an extensive medical literature on the compound. Key case series including Jasiurkowski et al. (2006), Shah et al. (2008) documenting acute renal failure in addition to liver injury, Singh et al. (2009), and Nasr & Ahmad (2009) established the severe adverse effect profile.
- A clinical case series by Singh et al. (2009) documented 5 cases of severe cholestatic liver injury in previously healthy young men with no other identifiable cause. The pattern was characteristic: jaundice developing 2 weeks after discontinuation, bilirubin peaking 4 weeks after presentation, and resolution over approximately 12 weeks with supportive care. Singh V et al., J Clin Gastroenterol 2009
- The compound was sold legally as an "over-the-counter supplement" from 2005 until the Designer Anabolic Steroid Control Act of 2014 placed methasterone in Schedule III. During this nearly decade-long window, the compound was widely available in supplement stores and on the internet, with users frequently unaware they were taking an active anabolic steroid rather than a dietary supplement.
- Cannot aromatize to estrogen (inherits drostanolone's lack of aromatization).
- The hepatotoxicity is particularly notable because severe outcomes have been documented after brief periods of exposure and in people with no prior hepatic disease, rather than only after prolonged or heavy exposure.
Legal status
Legal status
Schedule III controlled substance in the United States (DEA) following the Designer Anabolic Steroid Control Act of 2014. Previously sold legally as "dietary supplement" 2005-2012. No FDA approval; no current human therapeutic use anywhere. WADA-prohibited at all times in competitive sport.