rabeprazole + HMPL-760

rabeprazole + HMPL-760 is an investigational drug combination being evaluated in clinical pharmacology studies. HMPL-760 is a potent, third-generation, reversible, non-covalent inhibitor of Bruton's tyrosine kinase (BTK) discovered by HUTCHMED. It is designed to inhibit both wild-type BTK and the C481S-mutated enzyme, which is a common resistance mechanism against first-generation covalent BTK inhibitors. Rabeprazole is a proton pump inhibitor (PPI) that suppresses gastric acid secretion by inhibiting the H+/K+-ATPase enzyme. The combination is specifically utilized in Phase 1 clinical trials to assess the effect of food and gastric pH modulation (via rabeprazole) on the absorption and pharmacokinetics of HMPL-760 in healthy participants. While HMPL-760 is being developed for various B-cell malignancies, including diffuse large B-cell lymphoma (DLBCL), the rabeprazole combination serves as a tool for drug-drug interaction (DDI) characterization.