Androgen receptor antagonist
- Suppresses androgen-driven tissue/tumor growth
- Added to GnRH-based androgen deprivation in prostate cancer; also used alone
- Receptor blockade, not androgen deprivation: as monotherapy in men testosterone and estradiol RISE → gynecomastia; hot flashes and fatigue
- Newer agents lower seizure threshold
Drugs with this mechanism (4)
- Apalutamide — Androgen-receptor antagonist for prostate cancer; GABA-A effects give seizure risk.
- Bicalutamide — Androgen-receptor antagonist for prostate cancer.
- Darolutamide — Androgen-receptor inhibitor for advanced prostate cancer; minimal CNS penetration.
- Enzalutamide — Androgen-receptor antagonist for prostate cancer; GABA-A effects give seizure risk.
Self-check
- During androgen-receptor blocker monotherapy in men, what happens to testosterone and estradiol?
They rise. - How do newer androgen-receptor antagonists affect seizure threshold?
Lower it.
All mechanisms · Open Androgen receptor antagonist in the interactive console ↗