Bexobrutideg — Investigational Agent
BTK Degrader · Phase 1/2 · Nurix Therapeutics
Mechanism of Action
Orally bioavailable, brain-penetrant chimeric targeting molecule (CRBN-based BTK degrader) that recruits the cereblon E3 ubiquitin ligase complex to Bruton tyrosine kinase, driving its ubiquitination and proteasomal degradation. Unlike covalent or non-covalent BTK inhibitors, degradation eliminates both enzymatic and scaffolding functions of BTK and retains activity against resistance mutations such as C481S, T474 gatekeeper, and L528W, as well as against kinase-dead BTK.
Investigational Indications
- Relapsed/refractory chronic lymphocytic leukemia
- Small lymphocytic lymphoma
- Relapsed/refractory B-cell non-Hodgkin lymphoma (MCL, DLBCL, FL, MZL, WM)
- Primary and secondary CNS lymphoma