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catadegbrutinib
- Development stage
- Phase 3
- Lead developer
- BeOne Medicines
- 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
Catadegbrutinib (BGB-16673) is an orally bioavailable, chimeric small-molecule degrader, specifically a Proteolysis-Targeting Chimera (PROTAC), that targets Bruton's Tyrosine Kinase (BTK). Developed by BeiGene using their Chimeric Degradation Activating Compound (CDAC) platform, it is designed to overcome resistance mechanisms associated with traditional covalent and non-covalent BTK inhibitors, such as the BTK C481S mutation. The molecule functions by simultaneously binding to BTK and the Cereblon (CRBN) E3 ubiquitin ligase, facilitating the polyubiquitination of BTK and its subsequent degradation via the 26S proteasome. This mechanism allows for the depletion of both wild-type and mutant BTK proteins. Catadegbrutinib is currently under clinical investigation for the treatment of various B-cell malignancies, including chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL), particularly in patients who have progressed on prior BTK inhibitor therapies.
- Other names
- catadegbrutinib
02
Targets
CRBN (Cereblon)BTK (Bruton tyrosine kinase)
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