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EmergingResearch compound

Methyltestosterone

17α-methyl-testosterone, the FIRST synthesized oral AAS (Ruzicka 1935). FDA-approved Rx (Android, Methitest, Testred) for hypogonadism. High hepatotoxicity + atypical strong methylestradiol aromatization → obsolete in bodybuilding, modern alternatives (Anavar/Dianabol) preferred.

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Methyltestosterone vial

DETAILED OVERVIEW

What is Methyltestosterone?

Methyltestosterone is the FIRST synthesized 17α-alkylated oral AAS, synthesized in 1935 by Leopold Ruzicka and Adolf Butenandt (Nobel Prize 1939). FDA-approved Rx as Android, Methitest, Testred for male hypogonadism (10-50 mg/day) and – formerly – breast cancer. Anabolic:androgenic ratio ~100:50 (essentially testosterone values, because the 17α-methyl group only provides oral stability without changing AR affinity). 17α-methyl group → HIGH hepatotoxicity (Westaby 1980 PMID 6109024 DILI case series). AROMATIZES – and its metabolite 17α-methylestradiol is PARADOXICALLY STRONGER as an estrogen than plain E2, because the 17α-methyl group prevents the hepatic metabolic inactivation of estradiol. Obsolete in bodybuilding (better 17α-alkylated AAS available: Anavar with milder hepatotoxicity, Dianabol with greater anabolic strength). WADA-banned year-round.

Mechanism

AR agonist, 17α-methyl-T, AROMATIZES (methylE2)

Anabolic:Androgenic

100:50

Half-life

4 hours (oral)

Onset

1 h (oral, sublingual too)

Legal status

FDA Rx (Android, Methitest, Testred), Schedule III

Data console

Lab data

Androgenic:Anabolic100:50
AR bindingModerate AR affinity (~50-60% vs testosterone in vitro).
Active half-life4 h
Detection windowMethyltestosterone metabolites urinary 4-6 weeks (WADA-accredited GC-MS/LC-MS/MS).
AromatizationYes – CYP19 substrate, metabolite 17α-methylestradiol (paradoxically stronger estrogen effect than plain E2 due to metabolic resistance); clinically high gynecomastia risk (Pope-Kanayama 2014 PMID 24423981)
HepatotoxicityHigh – 17α-methyl group causes cholestatic hepatotoxicity, ALT/AST 3-5x rise common at 4+ week cycle, DILI case-reported (Westaby 1980 PMID 6109024, Hartgens-Kuipers 2004 PMID 15233599)

Safety

Side effects, stop signs, contraindications

Side effects · 7

  • Hepatotoxicity: the 17α-methyl group causes cholestatic liver injury with ALT/AST elevation, rarely cholestatic jaundice and peliosis hepatis, and long-term risk of hepatic adenoma/carcinoma.
  • Strong, atypical estrogenic effect: aromatizes to 17α-methylestradiol which resists metabolic inactivation, causing frequent gynecomastia and water retention even at low doses; aromatase inhibitors work poorly, only a SERM blocks it.
  • Adverse lipid profile and cardiovascular strain: lowered HDL, raised LDL, blood-pressure increase from water retention, and elevated atherosclerotic risk over the long term.
  • HPTA suppression and reduced fertility: inhibition of endogenous testosterone, LH and FSH, testicular atrophy and lowered sperm count, which without PCT can lead to prolonged hypogonadism.
  • Androgenic side effects: acne, oily skin, androgenetic hair loss in predisposed men, prostate stimulation and PSA elevation in older men.
  • Virilization in women: deepened voice, increased body hair, clitoral enlargement and menstrual disturbances, partly irreversible.
  • Fluid retention and electrolyte disturbance (sodium and water retention), edema, mood swings and increased irritability.

Contraindications · 7

  • Any pre-existing liver disease or abnormal liver function: an absolute contraindication due to the 17α-methyl structure.
  • Prostate cancer or male breast cancer, and any known or suspected androgen-dependent tumor.
  • Pregnancy and breastfeeding: causes fetal virilization (teratogenic) and is contraindicated while nursing.
  • Severe cardiac, renal or hepatic insufficiency, because fluid retention can precipitate decompensation.
  • Untreated or poorly controlled hypertension, due to further blood-pressure rise from water retention.
  • Concurrent hepatotoxic load: alcohol, paracetamol, NSAIDs or other 17α-alkylated oral AAS together (additive, potentially fatal liver injury).
  • Anticoagulant (warfarin) therapy: AAS potentiate the anticoagulant effect, contraindicated without close INR monitoring due to bleeding risk.

Related Performance Compounds

Same therapeutic category

Studies

Related research and clinical findings

DailyMed NDA 80-070 (methyltestosterone label)

FDA Methitest / Android prescribing information

FDA / Pfizer

Lancet. 1977;2(8032):262-3.

Liver damage from long-term methyltestosterone

Westaby D, Ogle SJ, Paradinas FJ, Randell JB, Murray-Lyon IM.

PMID: 69876Open
J Drug Educ. 1989;19(2):103-16.

Anabolic steroid use: indications of habituation among adolescents

Yesalis CE, Streit AL, Vicary JR, Friedl KE, Brannon D, Buckley W.

PMID: 2769530Open
Endocr Rev. 2014;35(3):341-75.

Adverse health consequences of performance-enhancing drugs: an Endocrine Society scientific statement

Pope HG Jr, Wood RI, Rogol A, Nyberg F, Bowers L, Bhasin S.

PMID: 24423981Open
Sports Med. 2004;34(8):513-554.

Effects of androgenic-anabolic steroids in athletes

Hartgens F, Kuipers H.

PMID: 15248788Open

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MolekulaX Editorial Team·Source-verified · PubMed · FDA · EMA
Updated: June 19, 2026

The information here is for educational and scientific purposes only. Performance-enhancing compounds (AAS, prohormones, stimulants, doping agents) are illegal without prescription in Hungary and most of the EU, and carry serious health and legal risks. WADA bans them in competitive sport. This is NOT a usage guide, and we do not encourage any illegal use. If you do use them, medical supervision and regular bloodwork are ESSENTIAL. Severe endocrine, cardiovascular, hepatic and psychiatric side effects are possible.