Flutamide

Flutamide (SCH 13521) and bicalutamide [B3206] are non-steroidal androgen receptor antagonists with antiandrogenic activity. Testosterone [T0027], the most important androgen, converted to 5α-dihydrotestosterone (DHT) [A0462] by 5α-reductase type 2 which reduces the 4,5-double bond of testosterone in prostate cells. DHT has two or three times greater androgen receptor (AR) affinity than testosterone. Upon DHT binding, the AR undergoes a conformational change and releases heat shock proteins (HSPs), resulting in mRNA expression and prostate cell proliferation. Flutamide is rapidly metabolized by hydroxylation of the side chain to primary active form 2-hydroxyflutamide [H1600]. Subsequently, 2-hydroxyflutamide acts as a potent and highly selective competitive antagonist of the AR, blocks the conversion of testosterone to DHT, and inhibits the proliferation of prostate cells. Flutamide and bicalutamide are used for the treatment of prostate cancer and other androgen-dependent conditions. (The product is for research purpose only.)