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Cyproterone acetate

AEMPS

Antiandrogen with progestogenic activity

ATC code: G03HA01

Brand names: Diane-35, Androcur, Cyprostat

Updated · Methodology

Indications

B

Acne vulgaris

Second line

In severe hormone-dependent acne in women, combined with ethinyl estradiol. 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.

Sources

  1. AEMPS: Ficha técnica de Acetato de ciproterona + Etinilestradiol (2024)

ICD-10: L70.0 · ICD-11: ED80

B

Hirsutism

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Used in moderate-to-severe hirsutism in women combined with ethinyl estradiol (Diane-35, withdrawn in France in 2013).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).

Sources

  1. AEMPS: Ficha técnica de Acetato de ciproterona + Etinilestradiol (2024)
  2. Endocrine Society: Evaluation and Treatment of Hirsutism in Premenopausal Women (2018)

ICD-10: L68.0 · ICD-11: ED72

B

Prostate cancer

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.

Sources

  1. AEMPS: Ficha técnica de Acetato de ciproterona + Etinilestradiol (2024)

ICD-10: C61 · ICD-11: 2C82

Marketing claims without evidence base

The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.

F

Anti-aging and longevity

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.

Sources

  1. AEMPS: Ficha técnica de Acetato de ciproterona + Etinilestradiol (2024)
  2. Cochrane: Antioxidant supplements for prevention of mortality in healthy participants and patients with various diseases (2012)
How to read tiers A–F
  • AStrong evidence – first or second line in international guidelines
  • BRecommended in selected cases
  • CStudy data contradict each other
  • DBenefit not proven, no documented harm
  • FDocumented harm, or risk without benefit

Mechanism of action

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.

Safety

Contraindications

  • Cyproterone hypersensitivity
  • Pregnancy and lactation
  • Meningioma, current or past
  • Active thromboembolic disease
  • Severe hepatic impairment, hepatic tumors
  • Dubin-Johnson and Rotor syndromes
  • Severe chronic depression
  • Adolescents before completing pubertal development

Serious adverse effects

  • Meningioma (risk depends on cumulative dose)
  • Venous thromboembolism
  • Hepatotoxicity up to acute liver failure
  • Depression and suicidal ideation
  • Adrenal insufficiency

Common adverse effects

  • Fatigue
  • Reduced libido
  • Breast tenderness and gynecomastia in men
  • Weight gain
  • Mood changes

Pregnancy: can you take Cyproterone acetate?

Absolute contraindication. Reliable contraception is mandatory in women of reproductive age on therapy.

Breastfeeding: can you take Cyproterone acetate?

Contraindicated during lactation.

Calculate RID

Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.

Practical notes

Special situations

In 2020 confirmed the association of high cumulative cyproterone acetate doses (over 10 g total) with meningioma risk. Doses above 25 mg/day are restricted: for hirsutism and severe acne – only after alternatives fail, with the minimum dose and shortest duration possible. In patients on long-term therapy who develop headache, visual or hearing disturbance, or behavioral change, brain MRI is required.
Label mentions10 mentions

Verbatim lines from the interaction sections, in the language of the label

From this drug’s label

  • Moderateantidiabéticosclass named in the label
    «Diabetes: Se precisa una estricta vigilancia médica si el paciente sufre diabetes, ya que la necesidad de tomar antidiabéticos orales o insulina puede cambiar durante el tratamiento con Androcur (ver…»

    AEMPS, section 4.4 · Open on CIMA

  • Moderateantidiabéticos oralesclass named in the label
    «Diabetes: Se precisa una estricta vigilancia médica si el paciente sufre diabetes, ya que la necesidad de tomar antidiabéticos orales o insulina puede cambiar durante el tratamiento con Androcur (ver…»

    AEMPS, section 4.4 · Open on CIMA

  • ModerateInsulin
    «Diabetes: Se precisa una estricta vigilancia médica si el paciente sufre diabetes, ya que la necesidad de tomar antidiabéticos orales o insulina puede cambiar durante el tratamiento con Androcur (ver…»

    AEMPS, section 4.4 · Open on CIMA

  • Moderateinsulinaclass named in the label
    «Diabetes: Se precisa una estricta vigilancia médica si el paciente sufre diabetes, ya que la necesidad de tomar antidiabéticos orales o insulina puede cambiar durante el tratamiento con Androcur (ver…»

    AEMPS, section 4.4 · Open on CIMA

  • Clotrimazole
    «Aunque no se han realizado estudios de interacción clínica, dado que este fármaco es metabolizado por el CYP3A4, es de esperar que ketoconazol, itraconazol, clotrimazol, ritonavir y otros inhibidores…»

    AEMPS, section 4.5 · Open on CIMA

  • Itraconazole
    «Aunque no se han realizado estudios de interacción clínica, dado que este fármaco es metabolizado por el CYP3A4, es de esperar que ketoconazol, itraconazol, clotrimazol, ritonavir y otros inhibidores…»

    AEMPS, section 4.5 · Open on CIMA

  • Ketoconazole
    «Aunque no se han realizado estudios de interacción clínica, dado que este fármaco es metabolizado por el CYP3A4, es de esperar que ketoconazol, itraconazol, clotrimazol, ritonavir y otros inhibidores…»

    AEMPS, section 4.5 · Open on CIMA

  • Phenytoin
    «Aunque no se han realizado estudios de interacción clínica, dado que este fármaco es metabolizado por el CYP3A4, es de esperar que ketoconazol, itraconazol, clotrimazol, ritonavir y otros inhibidores…»

    AEMPS, section 4.5 · Open on CIMA

  • Rifampicin
    «Aunque no se han realizado estudios de interacción clínica, dado que este fármaco es metabolizado por el CYP3A4, es de esperar que ketoconazol, itraconazol, clotrimazol, ritonavir y otros inhibidores…»

    AEMPS, section 4.5 · Open on CIMA

  • Ritonavir
    «Aunque no se han realizado estudios de interacción clínica, dado que este fármaco es metabolizado por el CYP3A4, es de esperar que ketoconazol, itraconazol, clotrimazol, ritonavir y otros inhibidores…»

    AEMPS, section 4.5 · Open on CIMA

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Frequently asked

What is Cyproterone acetate used for?

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.

What are the side effects of Cyproterone acetate?

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.

Is Cyproterone acetate safe during pregnancy?

Absolute contraindication. Reliable contraception is mandatory in women of reproductive age on therapy.

Is Cyproterone acetate compatible with breastfeeding?

Contraindicated during lactation.

Who should not take Cyproterone acetate?

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.

Official sources

Direct links to regulator labels. Open in a new tab.

Other drugs in this group

Cyproterone acetate + Ethinylestradiol, Desogestrel, Drospirenone + ethinylestradiol, Dydrogesterone, Estradiol, Ethinylestradiol + Gestodene, Levonorgestrel, Progesterone, micronized