Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist with binding IC50 of 16 nM.
Apalutamide (ARN-509) targets the AR ligand-binding domain and prevents AR nuclear translocation, DNA binding, and transcription of AR gene targets, inhibits AR transcriptional activity and prostate cancer cell proliferation.
ARN-509 lacked significant agonist activity in preclinical models of CRPC compared to bicalutamide.
ARN-509 showed greater efficacy than MDV3100 in a clinically valid murine xenograft model of human CRPC.
