Drug Interaction Report

MONITOR: Coadministration with inhibitors of organic anion transporting polypeptides (OATP) 1B1 and/or 1B3 may increase the plasma concentrations and effects of momelotinib, which is a substrate of these hepatic uptake transporters. In a phase I study, coadministration of momelotinib (200 mg) with a single dose of the OATP1B1/1B3 inhibitor rifampin (600 mg) increased the peak plasma concentration (Cmax) and systemic exposure (AUC) of momelotinib by 40% and 57%, respectively. The Cmax and AUC of the active metabolite of momelotinib, M21, was also increased, by 6% and 12%, respectively.

MANAGEMENT: Caution is advised if momelotinib is used in combination with inhibitors of OATP1B1 and/or 1B3. Dosage adjustments of momelotinib may be required. Patients should be advised to report any momelotinib-related adverse reactions such as bacterial or viral infection, thrombocytopenia, neutropenia, hepatotoxicity, thrombosis, and adverse cardiovascular events.