EPI-7170

EPI-7170 is a small molecule androgen receptor (AR) antagonist that specifically targets the N-terminal domain (NTD) of the receptor. As an analog of ralaniten (EPI-001), it is designed to overcome resistance mechanisms associated with conventional antiandrogens that target the ligand-binding domain (LBD), such as AR splice variants (e.g., AR-V7) and LBD mutations. By binding to the NTD, EPI-7170 inhibits AR-mediated transcriptional activity, leading to cell cycle arrest in the G1 and S phases. Research indicates that EPI-7170 may also induce DNA damage or impair the DNA damage response. It has demonstrated efficacy in preclinical models of castration-resistant prostate cancer (CRPC) and AR-positive breast cancer, particularly when used in combination with CDK4/6 inhibitors like palbociclib.

Other names

ralaniten analog