Bexlosteride (LY300502), a benzoquinolinone derivative, functions as a human type I 5α-reductase inhibitor. It demonstrates metabolic inhibition, antiproliferative, and antisecretory activities specifically in LNCaP human prostatic adenocarcinoma cell cultures, positioning it as a potent agent for prostate cancer research [1] [2].

Bexlosteride effectively inhibits the reductive metabolism of [3 H-T] in LNCaP cells in a concentration-dependent manner, displaying an IC 50 of 5.77 nM[1]. At concentrations above 10 nM, it significantly counteracts the Testosterone-induced promotion of LNCaP cellular proliferation and completely inhibits Testosterone's mitogenic effects on these cells at 1000 nM[1]. Furthermore, Bexlosteride markedly opposes Testosterone-induced PSA secretion at concentrations of 30 nM or higher[1].