Methyltestosterone is testosterone with a methyl group added at carbon 17 (the 17α position). That one change lets the hormone survive its first pass through the liver, so it works as a pill. It is still FDA-approved in the US as 10 mg generic tablets and capsules for male hypogonadism.

It is also the androgen in estrogen-plus-methyltestosterone tablets for menopause (Estratest and its generics), which are listed on DailyMed as unapproved drugs. The most important fact about methyltestosterone is the trade-off built into its structure: the same 17α-methyl group that makes it orally active is linked to cholestatic jaundice, peliosis hepatis and liver tumors. The current label states that cholestatic hepatitis occurs “at a relatively low dose.”

This page summarizes what the FDA labels, clinical trials and regulators report. It is for education only and is not medical advice.

Property	Detail
Drug class	17α-alkylated oral androgen; anabolic-androgenic steroid
Current US products	Methitest tablets and generic capsules (ANDA 080767, 204851, 215270)
Former US brands	Android, Testred, Oreton Methyl, Metandren, Virilon (all discontinued)
Route	Oral; buccal/sublingual tablets were marketed in the past but are discontinued
Strengths	10 mg; 1.25 mg or 2.5 mg in estrogen combination tablets
Labeled dose	Men: 10–50 mg/day. Women with metastatic breast cancer: 50–200 mg/day
Half-life	Not stated in current US labels; the label says only that it is longer than testosterone’s
Liver	Label warns of cholestatic hepatitis and jaundice; monitor liver tests
US schedule	Schedule III; some estrogen combination tablets are DEA-exempt
WADA status	Prohibited at all times (S1.1 anabolic androgenic steroids)

What it is

Methyltestosterone is 17β-hydroxy-17-methylandrost-4-en-3-one: formula C₂₀H₃₀O₂, molecular weight 302.5 g/mol, CAS 58-18-4 (Methitest label; PubChem). Apart from the extra methyl group, the rest of the molecule is the same as testosterone, including the A-ring.

Plain testosterone works poorly as a pill. According to the label, the gut and liver clear much of an oral dose (44% by the liver on the first pass), and oral doses as high as 400 mg/day are needed to reach replacement levels. The 17α-methyl group slows this breakdown. The label describes methyltestosterone as “less extensively metabolized by the liver” with a longer half-life, which makes it “more suitable than testosterone for oral administration.”

The label also states that 17α-alkylation increases activity per unit weight compared with oral testosterone. The same structural feature is shared by other oral steroids in this library, such as Dianabol, Anadrol, Halotestin and Anavar. Oral testosterone undecanoate takes a different approach: it is an ester of testosterone, not a 17α-alkylated steroid.

US products listed in Drugs@FDA (FDA):

Product	Form	Strength	Status
Methitest / methyltestosterone tablets (ANDA 080767)	Oral tablet	10 mg	Prescription
Methyltestosterone capsules (ANDA 204851, 215270)	Oral capsule	10 mg	Prescription
Android 10, Android 25	Oral tablet	10 mg, 25 mg	Discontinued
Android 5, Oreton, Metandren	Buccal or sublingual tablet	5–25 mg	Discontinued
Testred, Virilon	Oral capsule	10 mg	Discontinued
Oreton Methyl (NDA 003158)	Oral tablet	10 mg, 25 mg	Discontinued

Pharmacokinetics

Reliable human pharmacokinetic data are sparse. The current labels give no half-life for methyltestosterone. Their half-life figure of 10–100 minutes refers to natural testosterone, not to methyltestosterone. We could not access a primary source that reports a human half-life, so we do not give one here.

What the available sources show:

Absorption. In 8 healthy men, a 10 mg tablet was absorbed to a similar extent as a 10 mg oral solution (Shinohara et al., J Pharm Sci 1986).
Sublingual vs oral. A 1973 study compared the two routes (Alkalay et al., 1973). PubChem’s Hazardous Substances Data Bank summarizes the finding as faster absorption and about double the bioavailability with the sublingual route (PubChem). Sublingual products are no longer sold in the US.
Metabolism. The main urinary metabolites in people are 17α-methyl-5α- and 5β-androstane-3α,17β-diol (Shinohara et al., J Chromatogr B 2000). Anti-doping labs have since identified additional long-lasting urinary metabolites that extend the detection window (Angelis et al., Drug Test Anal 2024).
SHBG. Methyltestosterone binds sex hormone-binding globulin (SHBG), the main carrier protein for testosterone. A modeling study predicted that therapeutic levels could displace about 48% of the testosterone bound to SHBG in a normal man (Pugeat et al., JCEM 1981). Trials in both men and women found that it lowers SHBG itself.

Testosterone blood tests are a poor guide to methyltestosterone exposure, and studies disagree on what they show. In one trial, men on 40 mg/day had serum testosterone under 15 nmol/L, against over 40 nmol/L on injected testosterone enanthate (Friedl et al., Metabolism 1990). In another, measured total testosterone rose above the normal range in every man (Morales et al., J Urol 1994). The label notes that testosterone levels “may be in the normal or subnormal range” in men misusing synthetic testosterone derivatives.

Approved medical use

The current labels for Methitest tablets and generic capsules cover the following uses (Methitest label; capsule label):

Indication	Labeled dose
Males: primary hypogonadism or hypogonadotropic hypogonadism	10–50 mg/day
Males: carefully selected boys with constitutionally delayed puberty	Lower part of that range, for a limited time such as 4–6 months
Females: secondary treatment of inoperable metastatic breast cancer, 1–5 years postmenopausal	50–200 mg/day

The diagnosis of hypogonadism should be confirmed with morning testosterone below the normal range on at least two separate days. The label states that safety and efficacy have not been established for “age-related hypogonadism,” and that the drug has not been shown to be safe and effective for enhancing athletic performance. It also notes a lack of substantial evidence that androgens help in fractures, surgery, convalescence or functional uterine bleeding.

Estrogen plus methyltestosterone for menopause

Tablets combining esterified estrogens with methyltestosterone are sold in two strengths: 0.625 mg estrogens with 1.25 mg methyltestosterone (“half strength”) and 1.25 mg estrogens with 2.5 mg methyltestosterone (“full strength”). Their label lists moderate to severe menopausal hot flashes not improved by estrogen alone (Estratest label).

These products are listed on DailyMed under the marketing category “unapproved drug other.” They are not FDA-approved applications, unlike the 10 mg methyltestosterone tablets and capsules. They also carry the estrogen class warnings, such as endometrial cancer with unopposed estrogen.

What the research shows

Most controlled human data on methyltestosterone come from two settings: low doses added to estrogen in postmenopausal women, and short, high-dose studies in healthy men. There are no modern trials of methyltestosterone for muscle mass or strength.

Men with hypogonadism and erectile dysfunction

A small 1994 study gave 22 hypogonadal men with erectile dysfunction oral methyltestosterone for one month (Morales et al., J Urol 1994). Results:

Measured total testosterone rose above the normal range in every patient, but free testosterone did not rise in proportion and often fell.
SHBG fell in all but one man, and the pituitary signals LH and FSH were strongly suppressed.
Only 9% reported full recovery of sexual function. The authors called oral methyltestosterone “of limited effectiveness” for this purpose.

Sexual desire in postmenopausal women

In a double-blind trial, 218 postmenopausal women with low sexual desire took 0.625 mg esterified estrogens alone (n = 111) or with 1.25 mg methyltestosterone (n = 107) for 4 months (Lobo et al., Fertil Steril 2003). The combination raised bioavailable testosterone, lowered SHBG and improved sexual interest and desire more than estrogen alone.

A 2019 meta-analysis of 36 randomized trials with 8,480 women confirmed that testosterone improves sexual desire and satisfaction after menopause (Islam et al., Lancet Diabetes Endocrinol 2019). It found an important difference by route, however:

Oral testosterone raised LDL (“bad”) cholesterol and lowered HDL (“good”) cholesterol.
Non-oral routes, such as patches and creams, did not have this effect.

The authors concluded that non-oral routes are preferred because their lipid profile is neutral.

Bone and menopausal symptoms

Two 2-year randomized trials in women whose ovaries had been removed compared estrogen alone with estrogen plus methyltestosterone:

Trial	n	Regimens	Main findings
Watts et al., Obstet Gynecol 1995	66	Esterified estrogens 1.25 mg, with or without methyltestosterone 2.5 mg/day	Both prevented bone loss. Spine bone density rose 3.4% (SE 1.2%) from baseline with the combination. HDL fell with the combination and rose with estrogen alone.
Barrett-Connor et al., J Reprod Med 1999	311	Conjugated estrogens 0.625 or 1.25 mg vs esterified estrogens 0.625 mg + methyltestosterone 1.25 mg or 1.25 mg + 2.5 mg	All prevented bone loss. The higher combination dose raised spine and hip density more (p under 0.002). HDL rose only with estrogen alone.

Mood and hormones in healthy men

The best-controlled data on high doses come from an NIH inpatient study of 20 healthy men with no prior steroid use (Su et al., JAMA 1993). It was a double-blind, fixed-order crossover with four 3-day phases:

Phase	Dose	What changed vs baseline
Placebo baseline	—	—
Low dose	40 mg/day	No significant changes reported
High dose	240 mg/day	Small but significant rises in euphoria, energy and sexual arousal, and also irritability, mood swings, violent feelings, hostility, distractibility and forgetfulness
Placebo withdrawal	—	—

One of the 20 men (5%) had an acute manic episode, and another became hypomanic, after only days of exposure. Follow-up analyses of the same study found the following:

Hormones. High-dose methyltestosterone lowered LH, FSH, the men’s own sex steroids, SHBG and thyroid-binding globulin within days (Daly et al., Psychoneuroendocrinology 2003).
Brain chemistry. In 17 men, levels of a serotonin metabolite in spinal fluid rose. These changes correlated with “activation” symptoms such as energy, sexual arousal and reduced sleep (Daly et al., Arch Gen Psychiatry 2001).

Side effects and risks

Liver

The labels warn of three kinds of liver harm from methyltestosterone:

Cholestatic hepatitis and jaundice. Bile flow is blocked. The label says this occurs with 17α-alkylated androgens “at a relatively low dose” and is reversible when the drug is stopped.
Peliosis hepatis. Blood-filled cysts form in the liver. This can be life-threatening.
Liver tumors. These include hepatocellular carcinoma after prolonged high-dose use. Stopping the drug did not always make the tumors regress.

The clearest clinical series followed 60 patients on long-term methyltestosterone at 50 mg three times daily (Westaby et al., Lancet 1977):

Finding	Patients
Abnormal liver function tests	19 of 60 (32%)
Abnormal liver scans	33 of 52 scanned (63%)
Early peliosis hepatis on biopsy	Reported
Liver adenoma	1

Scan abnormalities were most common after more than a year of treatment. In a review of 133 published cases of liver tumors after androgen therapy, methyltestosterone was one of the three most frequently involved androgens. Hepatocellular carcinoma was more often linked to methyltestosterone and oxymetholone than to other androgens (Velazquez & Alter, Am J Hematol 2004). Case reports cannot show how common this is, because the number of people exposed is unknown.

“Low doses are liver-safe.” The evidence does not support this. One case report describes a 64-year-old man who developed cholestatic jaundice after taking 20–40 mg/day for 6 months, within the labeled range (Borhan-Manesh & Farnum, Arch Intern Med 1989). The authors noted a typical pattern: high bilirubin with a normal or only mildly raised alkaline phosphatase. The label advises periodic liver function tests for everyone on 17α-alkylated androgens.

Lipids

Methyltestosterone lowers HDL cholesterol more than injected testosterone does. In a 12-week trial, 18 healthy young men received the same weekly androgen dose in one of three forms (Friedl et al., Metabolism 1990):

Group	HDL at baseline	HDL at 4 weeks
Methyltestosterone 20 mg twice daily	1.20 mmol/L (≈46 mg/dL)	0.77 mmol/L (≈30 mg/dL)
Testosterone enanthate 280 mg/week + testolactone (blocks estrogen formation)	1.18 mmol/L (≈46 mg/dL)	0.89 mmol/L (≈34 mg/dL)
Testosterone enanthate 280 mg/week	No decrease	No decrease

Methyltestosterone also lowered apolipoprotein A1 and raised LDL cholesterol. The HDL changes reversed within 2 weeks of stopping.

The same pattern appears at the much lower doses used in women:

Esterified estrogens with or without methyltestosterone, 6 months. In a randomized trial of 26 women, adding methyltestosterone lowered total cholesterol, HDL and apolipoprotein A1 compared with estrogen alone (Hickok et al., Obstet Gynecol 1993).
Methyltestosterone 1.25 mg/day plus percutaneous estradiol, 12 months. In 37 women, HDL fell only in the methyltestosterone group, and these women gained some weight and visceral (abdominal organ) fat (Leão et al., Eur J Endocrinol 2006).
Triglycerides. Adding methyltestosterone also lowered triglycerides and apolipoprotein C-III (Chiuve et al., JCEM 2004).

Hormonal suppression and fertility

The label explains that androgens suppress LH through feedback on the pituitary, and that larger doses also suppress FSH and sperm production. It lists low sperm counts (oligospermia) and reduced ejaculate volume after prolonged or excessive dosing. In the NIH study, 240 mg/day lowered gonadotropins within 3 days. In the Friedl trial, 40 mg/day did not change LH.

Other labeled warnings

The labels also list the following warnings:

venous thromboembolism (blood clots), from post-marketing reports;
increases in blood pressure;
edema, which can be serious in people with heart, kidney or liver disease;
gynecomastia, which “frequently develops” in men treated for hypogonadism;
virilization in women, such as voice deepening, facial hair and clitoral enlargement, which may not reverse;
early closure of growth plates in children, which can reduce adult height;
hypercalcemia in women with breast cancer;
abuse and dependence, including serious cardiovascular and psychiatric reactions at misuse doses.

Interactions

Drug	Labeled interaction
Oral anticoagulants (e.g. warfarin)	17α-substituted androgens can lower anticoagulant needs; monitor closely when starting or stopping
Insulin	Androgens may lower blood glucose and insulin requirements
Oxyphenbutazone	Blood levels of oxyphenbutazone may rise
Thyroid tests	Thyroxine-binding globulin falls, lowering total T4; free thyroid hormone stays normal

Who should not use it

The label contraindicates methyltestosterone in:

men with breast cancer, or known or suspected prostate cancer;
women who are or may become pregnant. It is Pregnancy Category X, because it can masculinize a female fetus.

Monitoring

These are the label’s monitoring recommendations:

What	When
Liver function tests	Periodically, for all patients on 17α-alkylated androgens
Hemoglobin and hematocrit	Periodically, at high doses
Bone age (hand and wrist X-ray)	Every 6 months in boys treated for delayed puberty
Urine and serum calcium	Frequently, in women with metastatic breast cancer
Blood pressure	Periodically, especially with hypertension

Legal status and use outside medicine

United States. Methyltestosterone is named in Schedule III of the Controlled Substances Act (21 CFR 1308.13), so it requires a prescription.
DEA-exempt products. The DEA’s list of exempt anabolic steroid products includes many esterified-estrogen and methyltestosterone tablets, such as Estratest and its generics, which removes some controlled-substance requirements for those products (DEA exempt list, 2020). The same list includes an investigational tilapia sex-reversal fish feed containing 60 mg/kg methyltestosterone, reflecting its use in aquaculture.
Sport. WADA lists methyltestosterone by name under S1.1 anabolic androgenic steroids, prohibited in and out of competition (WADA 2026 Prohibited List).

Key takeaways

Oral testosterone, chemically modified. A 17α-methyl group lets it survive first-pass liver metabolism. It is still FDA-approved as 10 mg tablets and capsules for male hypogonadism.
Liver risk is built into the structure. Labels warn of cholestatic jaundice “at a relatively low dose,” along with peliosis hepatis and liver tumors with long-term high-dose use.
HDL falls more than with injected testosterone. In healthy men, 40 mg/day cut HDL from about 46 to 30 mg/dL within 4 weeks. Even 1.25–2.5 mg/day in women lowered HDL.
Modest, mixed clinical results. Added to estrogen, it improved sexual desire and spine bone density in postmenopausal women. In hypogonadal men with erectile dysfunction, only 9% fully recovered sexual function.
High doses affect mood quickly. In healthy men, 240 mg/day for 3 days raised irritability and hostility, and 1 in 20 had a manic episode.
Half-life is poorly documented. Current labels give none, and standard testosterone blood tests are an unreliable guide to exposure.

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Methyltestosterone