(R)-Bicalutamide

R-Bicalutamide is a first-generation antiandrogen that inhibits androgen action by competitively binding to the androgen receptor (AR). With other anti-androgens, R-bicalutimide decreases levels of Bcl-2, Bcl-XL, caspase-3, and PARP, induces apoptosis, and inhibits cell growth of prostate cancer cells. In similar animal models, this compound decreases plasma PSA levels and suppresses tumor growth. Bicalutamide binds the androgen receptor in two sites, distorting coactivator binding and inhibiting transcription.