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bavdegalutamide
- Development stage
- Phase 2
- Lead developer
- Arvinas
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
Bavdegalutamide (ARV-110) is an investigational, orally bioavailable PROTAC (Proteolysis Targeting Chimera) protein degrader designed to selectively target and degrade the androgen receptor (AR). Developed by Arvinas, it functions by recruiting the cereblon (CRBN) E3 ubiquitin ligase to the AR, leading to the receptor's polyubiquitination and subsequent degradation by the 26S proteasome. This mechanism is intended to overcome resistance seen with traditional AR antagonists, such as AR overexpression or specific point mutations (e.g., T878A, H875Y). Bavdegalutamide was the first PROTAC protein degrader to enter human clinical trials and is primarily being evaluated for the treatment of patients with metastatic castration-resistant prostate cancer (mCRPC), both as a monotherapy and in combination with other agents like abiraterone.
- Other names
- bavdegalutamide
02
Targets
CRBN (Cereblon)AR (Adrenergic receptors)
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