A Dual AR Degrader–Inhibitor for Prostate Cancer

Abstract: Small-molecule inhibitors of the androgen receptor are still a treatment mainstay for advanced prostate cancer, but increasingly, the field is moving toward AR degraders for complete target elimination. An investigational candidate, BMS-986365, has shown preliminary promise as a dual AR degrader and inhibitor. Through a screening platform, researchers are also homing in on a new compound that selectively targets the splice variant AR-V7, a known culprit in resistance to standard care for this disease.