Superdrol

An oral steroid that briefly sold as a legal "prohormone" supplement in the early 2000s before regulators acted. No therapeutic development exists; its published record is dominated by liver-injury case reports.

Methasterone is a designer steroid that was sold openly as a "prohormone" supplement in the United States until it was scheduled. It binds the androgen receptor strongly, does not aromatise, and is unusually potent by weight. Oral 17-alpha-alkylated steroids share one design feature: a methyl group added at the 17 position so the molecule survives first-pass liver metabolism instead of being destroyed. That modification is what makes them orally active and it is strongly associated with the highest cholestatic risk in this class, though the exact injury mechanism is not settled. Liver strain is not an unlucky accident with these compounds; it travels with the chemistry that makes them oral. Multiple case reports and small series document severe, protracted cholestatic injury with methasterone, sometimes alongside kidney failure. How often that happens, and how it ranks against other compounds, cannot be quantified: the exposures, the actual product contents and the denominator are all unknown.

Zero clinical development. Its evidence base is the supplement-era case literature — extensive because of how often it produced hepatology referrals.

• There is no legitimate clinical development record — it was never developed as a medicine and reached people through the supplement market.
• The human literature is almost entirely case reports of harm: cholestatic hepatitis, jaundice lasting months, acute kidney injury and hospital admission in young, otherwise healthy men. Case reports establish that severe injury happens; they cannot establish how often.
• Reported liver injury has occurred within weeks of starting, at amounts stated on product labels or reported by patients — these were unapproved supplement-era products, so actual content and true exposure were never verified.
• It featured prominently in the wave of supplement-associated liver injury that prompted regulatory action against designer steroids.

An orally active 17-alpha-alkylated anabolic steroid, scheduled in the US, with no FDA-approved product. It does not aromatise. Adding drugs to manage steroid side effects is unapproved and belongs with a clinician. There is no adequate human pharmacokinetic data, and the fact that matters is not a half-life figure but that serious liver injury has followed short exposures.

Published case reports document severe cholestatic liver injury, some requiring hospitalization, after short "supplement"-era exposures. Add severe lipid damage, blood-pressure elevation, marked HPG-axis suppression, and heavily-reported lethargy.

• Class-level severe outcomes reported with anabolic steroids, which no compound here is exempt from: cardiac arrest, heart attack, thickened heart muscle, heart failure and stroke; serious liver injury; and mania, paranoia, psychosis, hostility, aggression, dependence and depression on withdrawal.
• Pregnancy and breastfeeding: androgens can cause fetal harm including virilisation of a female fetus. Avoid in both.
• Everyone — there is no medical use, no clinical development record, and a severe documented liver-injury profile
• Most emphatically anyone with any liver condition, anyone drinking alcohol, and any child or adolescent
• Women, given virilisation risk on top of everything else

• Alcohol, paracetamol, and any hepatotoxic drug or supplement — with this compound the margin is genuinely thin.
• Anticoagulants.
• Other orals, where the liver burden is additive and has produced the worst reported outcomes.

Documented interactions with other things people research. A compound not listed here does not mean the combination is safe — only that no specific interaction is on file.

• Liver enzymes and bilirubin, and this is the compound where waiting for symptoms is most dangerous — jaundice often appears after significant injury is established.
• Any yellowing of eyes or skin, dark urine, pale stools, itching or right-upper-abdominal pain, all of which are stop-immediately-and-be-seen events.
• Lipids, which it suppresses severely.
• Blood pressure and kidney function.

Cholestatic injury from this compound is slow to resolve — published cases describe jaundice and itching persisting for months after stopping, sometimes requiring hospital management. Stopping is necessary but is not the end of it. Anyone who develops jaundice, dark urine or persistent itching needs medical care rather than waiting it out, and should say exactly what they took, because drug-induced liver injury is managed differently from viral hepatitis.

US: Schedule III — DEA added methasterone to the schedule in 2012. No approved product has ever existed.

Papers about this compound, not proof of the claims above. A title says what was studied, which is sometimes a negative result or a different question entirely.

• Severe cholestasis and renal failure associated with the use of the designer steroid Superdrol (methasteron): a case report and literature review
  Dig Dis Sci, 2009
• Unraveling binding interactions between methasterone and bovine serum albumin (BSA): A spectroscopic and computational study
  Steroids, 2025
• Multiplex Nontargeted Framework Enables Tracking Metabolic Profile of Oxymetholone and Methasterone In Vivo at Nanogram Level by GC-Orbitrap-HRMS for Antidoping Purpose
  Anal Chem, 2025

• Structural transformation of methasterone with Cunninghamella blakesleeana and Macrophomina phaseolinaRSC Adv · 2022
• Unraveling binding interactions between methasterone and bovine serum albumin (BSA): A spectroscopic and computational studySteroids · 2025
• Biotransformation of anabolic compound methasterone with Macrophomina phaseolina, Cunninghamella blakesleeana, and Fusarium lini, and TNF-α inhibitory effect of transformed productsSteroids · 2017
• Glomerella fusarioides-catalyzed structural transformation of steroidal drugs mesterolone and methasterone, and anti-inflammatory activity of resulting derivativesSteroids · 2023
• In vitro and in vivo metabolism studies of dimethazineBiomed Chromatogr · 2016
• Metabolic studies with promagnon, methylclostebol and methasterone in the uPA+/+-SCID chimeric miceJ Steroid Biochem Mol Biol · 2011
• New Potential Biomarker for Methasterone Misuse in Human Urine by Liquid Chromatography Quadrupole Time of Flight Mass SpectrometryInt J Mol Sci · 2016
• Multiplex Nontargeted Framework Enables Tracking Metabolic Profile of Oxymetholone and Methasterone In Vivo at Nanogram Level by GC-Orbitrap-HRMS for Antidoping PurposeAnal Chem · 2025
• Characterization and metabolic profiling of oxymetholone and methasterone metabolites studied with human liver S9 model using GC-Orbitrap-HRMS for anti-doping purposesAnal Bioanal Chem · 2025
• Classification of two steroids, prostanozol and methasterone, as Schedule III anabolic steroids under the Controlled Substance Act. Final ruleFed Regist · 2012
• Androgenic steroids in Over-the-Counter dietary Supplements: Analysis for association with adverse health effectsSteroids · 2023
• Assessment of the inhibitory potential of anabolic steroids towards human AKR1D1 by computational methods and in vitro evaluationToxicol Lett · 2023