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Cyproterone acetate in gender care

Cyproterone acetate (trade name Androcur) is the most prescribed anti-androgen in trans women in the Netherlands. It is a synthetic steroid with both anti-androgenic and progestative action.

Action

Cyproterone acetate blocks the androgen receptor and also inhibits the release of LH (luteinising hormone) by the pituitary gland. As a result, testosterone production in the testes decreases. The agent also has progestative activity and is prescribed in lower doses in women for severe acne and hirsutism.

Use in Dutch gender care

The Dutch Society for Endocrinology and the protocols of Amsterdam UMC name cyproterone acetate as the standard anti-androgen in feminising hormone therapy, combined with oestrogen. Internationally it also appears in the Endocrine Society guideline (2017) and the WPATH Standards of Care version 8 (2022).

Side effects

Known side effects include fatigue, weight gain, mood complaints, reduced libido and, in rare cases, liver damage. Mood complaints and depressive symptoms are regularly reported in research and clinical practice.

EMA warning meningioma (2020)

In 2020 the European Medicines Agency (EMA) established usage restrictions for cyproterone-containing medicines because of an increased risk of meningioma (benign tumour of the meninges). The risk is dose-dependent and increases with prolonged use at higher doses. The EMA advises treating with the lowest effective dose and discontinuing use upon diagnosis of meningioma.

Alternatives

Internationally, alternatives include spironolactone (especially in the US) and GnRH agonists. The choice between agents is partly determined by the side effect profile, availability and patient preference.