Drug intelligence / Profile preview

cyproterone + spironolactone

Development stage
Unknown
Lead developer
Bayer
Modality
Small Molecules
Administration
Oral, Intramuscular, Topical
01

Overview

This is a combination of two separate anti-androgenic medications, cyproterone acetate and spironolactone, that are sometimes used together or as alternatives in feminizing hormone therapy, particularly for transgender women. Cyproterone acetate is a steroidal anti-androgen that works both by blocking androgen receptors and by activating progesterone receptors to suppress testosterone production. Spironolactone is a potassium-sparing diuretic with anti-androgenic properties that works primarily by blocking androgen receptors without necessarily reducing testosterone levels. Studies have shown that cyproterone acetate generally provides stronger testosterone suppression than spironolactone, but it may have more serious potential side effects including association with meningioma at higher doses.

02

Targets

AR (Adrenergic receptors)PR (Progesterone receptor)MR (Mineralocorticoid receptor)

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