Antiandrogen with progestogenic activity
ATC code: G03HA01 (Cyproterone acetate)
Brand names
Diane-35, Androcur, Cyprostat
Competitive androgen receptor antagonist in target tissues (prostate, skin, hair follicles). Additionally suppresses LH secretion via progestogenic activity, lowering testosterone synthesis. CYP3A4-metabolized. In Spain and Europe used in three groups: antiandrogen therapy for prostate cancer; hirsutism and severe acne in women (combined with ethinyl estradiol); gender-affirming hormone therapy for transgender women. In 2020 confirmed the link of high cumulative doses to meningioma and restricted long courses above 25 mg/day.
Second line
In severe hormone-dependent acne in women, combined with ethinyl . 2024 and AEDV 2023 set topical retinoids, benzoyl peroxide, and azelaic acid as first-line; hormonal therapy is second-line in acne with features of hyperandrogenism. Use is limited by meningioma risk ( 2020 warning) and thromboembolic events.
Second line
Used in moderate-to-severe hirsutism in women combined with ethinyl estradiol (Diane-35, withdrawn in France in 2013). Endocrine Society 2018 places estrogen-progestin contraceptives and spironolactone as first-line; cyproterone acetate is an alternative when those fail or are intolerable. Dose 25–50 mg for 10 days of the cycle (Hammerstein regimen).
Second line
In metastatic hormone-sensitive prostate cancer, used as monotherapy or with a GnRH agonist to prevent the testosterone flare. Dose 100–300 mg/day. EAU 2024 sets androgen-deprivation therapy (GnRH agonists or antagonists) ± abiraterone, enzalutamide, or docetaxel as first-line; cyproterone acetate is an alternative when access to newer agents is limited.
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Cyproterone acetate is an antiandrogen and progestogen. It is prescribed for men with prostate cancer on androgen deprivation therapy and severe hypersexuality; in women, for severe androgen-dependent acne or hirsutism when other drugs are ineffective (AEMPS Ficha Técnica). In men, cyproterone acetate is used off-label to suppress libido in anti-aging practice. In women with mild acne or hirsutism not meeting all AEMPS criteria, cyproterone acetate is not indicated. The drug has serious risks: meningiomas (dose-dependent risk; imposed strict dose and duration limits in 2020), hepatotoxicity, thromboembolic events, depression, and erectile dysfunction with reduced libido in men. If cyproterone acetate was prescribed for anti-aging or for mild acne, consider seeking a second opinion.
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Absolute contraindication. Reliable contraception is mandatory in women of reproductive age on therapy.
Contraindicated during lactation.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Cyproterone acetate is evaluated for the following indications with varying evidence strength: Prostate cancer (evidence tier B), Hirsutism (evidence tier B), Acne vulgaris (evidence tier B). See the full indication matrix with dosing and citations above on this page.
Common side effects of Cyproterone acetate (≥ 1 in 100): Fatigue, Reduced libido, Breast tenderness and gynecomastia in men, Weight gain, Mood changes. See the Safety section for uncommon and serious reactions.
FDA category X. Absolute contraindication. Reliable contraception is mandatory in women of reproductive age on therapy.
Contraindicated during lactation.
Cyproterone acetate is contraindicated in: Cyproterone hypersensitivity; Pregnancy and lactation; Meningioma, current or past; Active thromboembolic disease; Severe hepatic impairment, hepatic tumors. Full list in the Safety section.