Bavdegalutamide — Investigational Agent
Androgen Receptor Degrader · Phase 1/2 · Arvinas
Mechanism of Action
First-in-class oral PROTAC (PROteolysis-TArgeting Chimera) androgen receptor degrader. A bifunctional molecule linking an AR-binding ligand to an E3 ubiquitin ligase (cereblon) recruiter; it forms a ternary complex that ubiquitinates the androgen receptor and routes it for proteasomal degradation. Unlike AR antagonists, degradation eliminates the receptor entirely, retaining activity against certain AR resistance mutations (e.g., T878, H875) that confer resistance to enzalutamide/abiraterone.
Investigational Indications
- Metastatic castration-resistant prostate cancer (mCRPC), enriched for AR T878X/H875Y mutations