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tacabrutideg
- 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
Tacabrutideg (BGB-16673) is an orally bioavailable, chimeric degradation activating compound (CDAC) or proteolysis-targeting chimera (PROTAC) designed to target and degrade Bruton's tyrosine kinase (BTK). Developed by BeiGene, it is being investigated for the treatment of B-cell malignancies, including chronic lymphocytic leukemia (CLL) and small lymphocytic lymphoma (SLL), particularly in patients who have developed resistance to covalent and non-covalent BTK inhibitors. By recruiting the Cereblon (CRBN) E3 ubiquitin ligase to BTK, tacabrutideg induces the ubiquitination and subsequent proteasomal degradation of the target protein. This mechanism allows it to overcome common resistance mutations, such as BTK C481S, which impair the binding of covalent inhibitors. Tacabrutideg is currently in Phase 1/2 clinical development both as a monotherapy and in combination with other agents like obinutuzumab and sonrotoclax.
- Other names
- tacabrutideg
02
Targets
CRBN (Cereblon)BTK (Bruton tyrosine kinase)
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