vecabrutinib

Vecabrutinib is an orally available, second-generation, reversible small molecule inhibitor of Bruton's tyrosine kinase (BTK), developed for the treatment of B-cell malignancies. Unlike first-generation BTK inhibitors that bind covalently to the C481 residue of BTK, vecabrutinib binds non-covalently and inhibits both wild-type and C481S mutant forms of BTK, a mutation associated with resistance to other BTK inhibitors. Vecabrutinib also inhibits interleukin-2-inducible T-cell kinase (ITK) with high potency. By blocking BTK activity, it disrupts B-cell receptor signaling pathways critical for malignant B-cell survival and proliferation. The drug has been investigated in clinical trials for various hematological cancers such as chronic lymphocytic leukemia (CLL), mantle cell lymphoma (MCL), and Waldenström macroglobulinemia (WM), particularly in patients resistant to covalent BTK inhibitors[1][3][4][5][6][7].

Other names

vecabrutinib succinate