Methyltestosterone
Methyltestosterone is a synthetic androgen (male sex hormone) used primarily for testosterone replacement therapy in men with low testosterone levels. It is also occasionally used in women to treat certain types of breast cancer and in adolescent boys to treat delayed puberty. This medication is taken orally and works by mimicking the effects of naturally occurring testosterone in the body.
Methyltestosterone is an oral synthetic androgen used for testosterone replacement in men and certain breast cancer treatment in women.
This medication carries a boxed (black box) warning — the strongest type of FDA warning. Review the full prescribing information before use.
Key facts at a glance
- ATC
- G03BA02
- RxNorm
- 6904
- Generic
- Methyltestosterone
- Class
- atc-g03
- Brands
- Estratest, Methitest, Covaryx
- Availability
- rx
- Pregnancy
- X
- Lactation
- unsafe
- Routes
- oral
- Forms
- tablet, capsule
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Used in men for testosterone replacement due to hypogonadism, delayed puberty in adolescent males, and in women for palliative treatment of breast cancer. It may also be used in hormone therapy for transgender patients.
Methyltestosterone binds to androgen receptors in target tissues, mimicking the effects of endogenous testosterone. This leads to androgenic effects including development of male sexual characteristics, increased muscle mass, and stimulation of erythropoiesis.
This medication carries significant risk of hepatotoxicity and liver damage with long-term use. It is contraindicated in pregnancy, prostate cancer, and known cardiovascular disease. Regular monitoring of liver function, blood counts, and lipid profiles is recommended during treatment. May cause mood changes, acne, and fluid retention.
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed August 25, 2026. · Read our editorial policy