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BGB-1663
- Development stage
- Unknown
- Lead developer
- BeiGene
- 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
BGB-1663 is an investigational, orally administered chimeric degradation activating compound (CDAC) developed by BeiGene that targets the Human Epidermal Growth Factor Receptor 2 (HER2). Unlike traditional HER2 inhibitors that only block signaling, BGB-1663 functions as a proteolysis-targeting chimera (PROTAC) by recruiting an E3 ubiquitin ligase to the HER2 protein, leading to its ubiquitination and subsequent degradation via the proteasome. This mechanism is designed to address resistance seen with existing HER2-targeted therapies and to provide deeper and more sustained inhibition of HER2-driven oncogenic pathways. It is currently in Phase 1 clinical development for patients with advanced solid tumors harboring HER2 alterations, including overexpression and mutations.
- Other names
- HER2 CDACHER-2 CDACHER 2 CDAC
02
Targets
CRBN (Cereblon)BTK (Bruton tyrosine kinase)
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