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Cyproterone acetate is a steroidal antiandrogen and potent progestin used for prostate cancer, severe acne and hirsutism, and for androgen suppression in several other settings.
- Cyproterone acetate is a steroidal antiandrogen and potent progestogen licensed across Europe and much of the world but never approved by the FDA in the United States.
- The French national cohort found a strong dose-response relationship with intracranial meningioma: after one year of high-dose use the risk was 1.8-fold higher, rising to 383 meningiomas per 100,000 person-years in the highest cumulative-dose group, with a noticeable fall after discontinuation [1].
- Meningiomas attributed to cyproterone cluster in the anterior and middle skull base, particularly the spheno-orbital region, a distribution the authors described as specific to the drug [1].
- Transgender participants in the same analysis showed 20.7 meningiomas per 100,000 person-years [1], and the 2024 case-control study extended the meningioma signal to other progestogens [2].
- A 2025 randomized trial found cyproterone acetate and spironolactone gave comparable breast growth in transgender people, weakening the case for choosing cyproterone given its risk profile [6].
- The EMA restricted high-dose cyproterone in 2020 to cases where other treatments have failed, and requires meningioma monitoring.
Mechanism
It blocks the directly and, as a strong progestogen, suppresses luteinising hormone and therefore testicular testosterone production, so it both lowers androgens and blocks what remains. Cumulative dose is the variable that governs its meningioma risk, which is why European regulators restricted the high dose indications in 2020.
receptor fingerprint
(AR, NR3C4)Competitive antagonist at the ligand-binding domain, blocking dihydrotestosterone and testosterone signalling in prostate, skin and hair follicle
Progesterone receptor (PGR)Potent agonist; this progestogenic activity suppresses hypothalamic GnRH pulsatility and therefore LH and endogenous testosterone
Meningeal progesterone receptor (arachnoid/meningothelial cells)Chronic high-dose PR agonism drives growth of PR-positive meningiomas, dose-dependently and reversibly on withdrawal
Glucocorticoid receptor (NR3C1)Weak partial agonism at high doses
Safetyrisks and cautions, not medical advice
a high potency antiandrogen and progestin with a cumulative dose dependent risk of meningioma and of liver injury, which needs endocrine follow up and in some cases imaging
Subjective profileweighing the evidence above
The sourcing question gets no answer on this page, and the reason is cumulative dose. Meningioma risk here tracks total lifetime exposure, so the harm from buying it quietly and taking it for years is precisely the harm that no single purchase looks like; European regulators restricted the high dose indications in 2020 for that reason, and liver injury sits alongside it. The page documents what the drug is and what it does. Taking it is a decision that needs endocrine follow up and in some cases imaging, and none of that arrives in a parcel.
Resources
No suppliers are provided for compounds like this. This entry is here for reference.
Research
- 2011first citedRisk of meningioma among users of high doses of cyproterone acetate as compared with the genera…
- 2025most recentCyproterone acetate for hirsutism
- 1.Use of high dose cyproterone acetate and risk of intracranial meningioma in women: cohort study
- 2.Use of progestogens and the risk of intracranial meningioma: national case-control study
- 3.Risk of meningioma among users of high doses of cyproterone acetate as compared with the general population: evidence from a population-based cohort study
- 4.Cyproterone acetate and meningioma: a nationwide-wide population based study
- 5.Cyproterone acetate for hirsutism
- 6.Effect of Spironolactone and Cyproterone Acetate on Breast Growth in Transgender People: A Randomized Clinical Trial
- 7.Cyproterone acetate or spironolactone in lowering testosterone concentrations for transgender individuals receiving oestradiol therapy
7 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
Notes and cautions
- Dose-dependent intracranial meningioma is the defining risk; the EMA's 2020 review restricted high-dose use and mandates stopping the drug permanently if a meningioma is diagnosed.
- Dose-dependent hepatotoxicity is the second major hazard, with fulminant hepatitis and deaths reported mainly at doses of 100 mg per day and above, requiring liver function monitoring.
- Venous thromboembolism risk is increased, especially in combination with oestrogen in feminising regimens, and the drug is contraindicated in pregnancy and in existing liver disease.
- Depression and marked loss of libido are common and are frequently underweighted when the drug is prescribed for acne or hirsutism.