ARV-471 (ARV471) is a first-in-class, selective and orally bioavailable PROTAC-based Estrogen Receptor (AR) degrader. As a PROteolysis-TArgeting Chimera (PROTAC) small molecule, it induces degradation of wildtype and mutant ER. ARV-471 displays superior ER degradation and antitumor activity compared to fulvestrant in endocrine sensitive and resistant xenograft models. ARV-471 also demonstrated robust ER degradation in paired biopsy samples and encouraging clinical activity (41% CBR) in patients who received prior CDK 4/6 inhibitors. ARV-471 is now being evaluated in the VERITAC Phase 2 monotherapy expansion at 200 mg and 500 mg once daily.

纯度：≥98%

CAS：2229711-08-2