At a glance
Effects
- Muscle growth: Promotes nitrogen retention and protein anabolism, supporting lean mass gains; anabolic potency is moderate and roughly equivalent to testosterone (close to 1:1 anabolic:androgenic ratio) [1].
- Strength: Androgenic stimulation increases neuromuscular drive and red blood cell production, contributing to strength improvements [6].
- Masculinisation: Drives development or maintenance of male secondary sexual characteristics — voice deepening, facial/body hair, libido — via AR activation [4].
- Erythropoiesis: Stimulates red blood cell production, increasing hematocrit; at high doses this can cause polycythemia and raise clot risk [6].
- Estrogenic effects: Aromatises to the potent estrogen 17α-methylestradiol, causing fluid retention and risk of gynecomastia [1][5].
17α-Alkylated Anabolic-Androgenic Steroid (AAS)
~150 min (approx. 2.5 hrs) [4]
Oral (tablet / capsule) [2]
Schedule III Controlled Substance (USA) [3]
High — 17α-alkylated; cholestasis & tumour risk [4][7]
~3–4 weeks (urine, anti-doping) [8]
About Methyltestosterone
Every point here is drawn from public medical and harm-reduction sources. A bracketed number after a claim — like [1]— is a reference: tap it to open the exact source it's based on (numbered list at the bottom). It is not a rating or score. Educational information, not medical advice.
Product specifics
- Est. delivery
- 3–7 business days · EU tracked
Product details as stated by the vendor (claims, not independently verified). Delivery is our standard EU estimate.
What it is
Methyltestosterone is a 17α-alkylated anabolic-androgenic steroid (AAS) and one of the first orally active synthetic derivatives of testosterone, developed in 1935 [1]. It is used medically for male hypogonadism, delayed puberty, and advanced breast cancer in women, and is also used illicitly for physique and performance enhancement [2][3].
How it works
Methyltestosterone acts as an agonist of the androgen receptor (AR), mimicking the action of endogenous testosterone and dihydrotestosterone [1]. A methyl group added at the C-17α position prevents first-pass hepatic degradation, making it orally bioavailable — but this same modification causes dose-related hepatic stress [4]. In tissues expressing 5α-reductase (skin, hair follicles, prostate), it is converted to the more potent mestanolone [1]. It also aromatises efficiently into 17α-methylestradiol, a synthetic estrogen more potent and longer-lasting than natural estradiol, elevating the risk of estrogenic side effects [1][5].
Risks & side effects
Most important: Methyltestosterone carries a serious, dose-dependent risk of liver toxicity — including cholestasis, peliosis hepatis, elevated liver enzymes, and potentially fatal hepatic tumours — due to its 17α-alkylation [4][7]. This is the substance's most clinically significant harm and has caused it to be discontinued in many countries.
Common
Serious
- Cholestatic hepatitis and jaundice [7]
- Cardiovascular events: heart attack, stroke, blood clots (DVT/PE) [3][6]
- Polycythemia / thrombotic events from excess red blood cell production [6]
- Suppression of endogenous testosterone / testicular atrophy [1]
- Virilisation in women (voice change, clitoral enlargement — may be irreversible) [2]
- Mood disturbances: aggression, mood swings [6]
- Impaired fertility / oligospermia or amenorrhea [3]
- Hypercalcaemia (especially in immobile patients or those with cancer) [3]
Rare
- Peliosis hepatis (blood-filled liver cysts) [4][7]
- Hepatocellular carcinoma with prolonged high-dose use [4]
- Psychiatric effects at high doses: mania, psychosis, suicidality [6]
- Benign prostatic hyperplasia / prostate cancer with long-term use [6]
- Premature epiphyseal closure in adolescents [5]
- Severe allergic reaction (anaphylaxis) [2]
Safety & harm reduction
- Existing liver disease or hepatic impairment [5]
- Pregnancy or breastfeeding — serious fetal/neonatal harm [2]
- Women with existing or history of breast cancer [2]
- Prostate cancer (androgen-sensitive) [3]
- Known hypersensitivity to methyltestosterone or any excipient [2]
- Nephrotic syndrome or severe renal impairment [3]
- Hypercalcaemia [3]
- Liver function tests (ALT, AST, bilirubin) — check before starting, then every 4–6 weeks during use [5]
- Full lipid panel (HDL/LDL) every 3–6 months [5]
- Hematocrit / CBC — polycythemia risk; check every 3–6 months [5]
- Blood pressure — cardiovascular risk [5]
- PSA and digital rectal exam in men over 40 [3]
- Bone age X-ray every 6 months in adolescents with delayed puberty [5]
- Vitamin K antagonists (warfarin) — androgens potentiate anticoagulant effect; INR must be closely monitored [3]
- Cyclosporine — androgens raise cyclosporine levels and add hepatotoxic risk [3]
- Insulin / oral hypoglycaemics — androgens can lower blood glucose, requiring dose adjustment [5]
- Other hepatotoxic drugs (e.g., high-dose paracetamol, certain antibiotics) — additive liver stress [5]
- Corticosteroids — combination increases fluid retention risk [3]
- Liver support: use N-acetyl cysteine (NAC) or TUDCA/UDCA throughout any oral AAS cycle; avoid alcohol entirely [5]
- Cycle length: keep oral runs short (4–6 weeks maximum) to limit cumulative hepatotoxic exposure [5]
- Estrogen management: given high aromatisation to methylestradiol, an aromatase inhibitor (AI) may be considered to manage gynecomastia and fluid retention [1]
- Post-cycle therapy (PCT): endogenous testosterone suppression requires PCT with a SERM (e.g., tamoxifen or clomiphene) after cessation [1]
- Avoid stacking with other 17α-alkylated orals — additive hepatotoxicity [5]
Dosage context
Methyltestosterone is a prescription-only drug in the USA. Clinically approved oral doses are typically 10–50 mg/day for hypogonadism in men (brand Methitest: 10 mg capsules) [2]. For inoperable breast cancer in women, doses of 50–200 mg/day have been used medically [3]. Off-label and illicit performance use doses vary widely; these are NOT recommended and carry substantially higher risk of hepatotoxicity at higher exposures. No safe non-medical dosage range is established. The figures above are commonly reported in clinical literature, not a prescription.
Sources
- 1.Wikipedia — Methyltestosterone
- 2.Drugs.com — Methyltestosterone Prescribing Information
- 3.Medicine.com — Methyltestosterone Dosage & Interactions
- 4.Medscape — Anabolic Steroid Biopharmacology (Methyltestosterone)
- 5.Biomedicus — Methyltestosterone Side Effects & Safety
- 6.Wikipedia — Methyltestosterone (Cardiovascular / Psychiatric)
- 7.RxList — Methyltestosterone Hepatic Warnings
- 8.PubMed — Methyltestosterone Detection Times (LC-MS/MS)
- 9.ScienceDirect — Methyltestosterone Overview (Oral AAS)
- 10.GoodRx — Methyltestosterone Uses & Side Effects
- 11.Drugs.com MTM — Methyltestosterone Patient Information
- 12.Cleveland Clinic — Methyltestosterone Tablets/Capsules
- 13.Medtigo — Methyltestosterone Contraindications & Warnings
- 14.Mayo Clinic — Esterified Estrogens/Methyltestosterone Oral Route
This information is provided for educational and harm-reduction purposes only. It is not medical advice. These substances can carry serious health risks; effects and safe use vary by individual. Consult a qualified healthcare professional before use. Legal status varies by country — it is your responsibility to know your local law. We do not encourage misuse.