Preclinical Evaluation of Bavdegalutamide (ARV-110), a Novel PROteolysis TArgeting ...

Bavdegalutamide (ARV-110), a PROTAC protein degrader, selectively degrades wild-type and mutant AR with high potency, showing superior activity over enzalutamide in cell-based systems and AR-expressing xenograft models. It effectively inhibits tumor growth in enzalutamide- and abiraterone-resistant models and enhances abiraterone activity. Bavdegalutamide is the first PROTAC degrader in clinical trials for mCRPC.