HMPL-760

HMPL-760 is an investigational, highly selective, non-covalent, third-generation small molecule inhibitor of Bruton’s tyrosine kinase (BTK), developed by HUTCHMED. It is designed to target both wild-type and C481S-mutated BTK, the latter being a common mutation associated with resistance to first-generation covalent BTK inhibitors. The drug acts as a reversible inhibitor and demonstrates high potency and selectivity in preclinical studies. HMPL-760 is being developed primarily for hematological malignancies such as relapsed or refractory B-cell non-Hodgkin lymphomas—including chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL), diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL), mantle cell lymphoma (MCL), marginal zone lymphoma (MZL), and lymphoplasmacytic/macroglobulinemia (LPL/WM). It is administered orally and currently undergoing Phase 1/2 clinical trials in multiple countries[1][2][3][4][5][6][7].