tcsc1296 Bicalutamide

Bicalutamide(Casodex) is an oral non-steroidal anti-androgen for prostate cancer; binds to the androgen receptor.

IC50 Value: 0.16uM.

Target: Androgen receptor

Bicalutamide (BIC) is a drug of choice for the treatment of progressive androgen-dependent prostate cancer.

in vitro: Bicalutamide treatment of LNCaP/AR(cs) cells in absence of the synthetic androgen R1881 resulted in altered gene-expression consistent with its well-documented agonist activity in context of AR over-expression. In absence of R1881, bicalutamide partially activated VP16-AR-mediated transcription, indicative of AR binding to DNA. In LNCaP/AR-luc cells with a stably integrated AR-driven luciferase reporter construct, bicalutamide was unable to activate wtAR[1]. ARN-509 (IC50=16 nM) binds AR with 7- to 10-fold greater affinity than the clinically approved anti-androgen, bicalutamide (median IC50=160 nM), and competes for the same binding-site in the ligand-binding pocket of the receptor.

in vivo: Ridaforolimus and bicalutamide combination treatment promotes cell cycle arrest in prostate cancer cells. The effect of combination treatment was more pronounced, resulting in an almost complete G1 arrest in this cell line[2].

Clinical trail: Phase II trial of RAD001 and bicalutamide for castration-resistant prostate cancer is reported in 2012[3].