EPI-7245

EPI-7245 is a next-generation small molecule inhibitor of the androgen receptor (AR) N-terminal domain (NTD), developed by ESSA Pharmaceuticals. It belongs to a class of compounds known as Anitens. Unlike traditional anti-androgens that target the ligand-binding domain (LBD), EPI-7245 binds to the NTD, allowing it to inhibit AR-driven transcription even in the presence of LBD-linked resistance mechanisms, such as AR splice variants (e.g., AR-V7). Preclinical studies in castration-resistant prostate cancer (CRPC) models have demonstrated that EPI-7245 possesses significantly improved potency (IC50 < 500 nM) and metabolic stability compared to first-generation inhibitors like EPI-002. It is designed to treat both hormone-sensitive and castration-resistant prostate cancer by selectively inhibiting AR transcription.