RD162

RD162 is a potent, second-generation small molecule androgen receptor (AR) antagonist. It was developed as a structural analog of enzalutamide (MDV3100) and apalutamide (ARN-509) during the research that led to the discovery of modern androgen receptor-targeted agents (ARTAs). RD162 works by binding with high affinity to the ligand-binding domain of the AR, effectively inhibiting its nuclear translocation, DNA binding, and recruitment of coactivators. Unlike first-generation antiandrogens such as bicalutamide, RD162 maintains its antagonistic profile even in the context of AR overexpression, a common feature of castration-resistant prostate cancer (CRPC). While enzalutamide proceeded to clinical approval, RD162 remains a widely used tool in preclinical research for studying AR signaling and mechanisms of resistance in prostate cancer models.

Other names

4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide