Drug Interactions between momelotinib and Technivie

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.

MONITOR: Coadministration with momelotinib may increase the plasma concentrations of drugs that are substrates of the breast cancer resistance protein (BCRP) transporter. The mechanism is decreased clearance due to inhibition of BCRP-mediated intestinal and hepatobiliary efflux by momelotinib. Clinical studies have demonstrated that concomitant use of a single dose of rosuvastatin (10 mg) with multiple daily doses of momelotinib (200 mg) increased the peak plasma concentration (Cmax) and systemic exposure (AUC) by 220% and 170%, respectively.

MANAGEMENT: Caution is advised during concomitant use of momelotinib with drugs that are substrates of the BCRP transporter, particularly those with a narrow therapeutic range. Dosage adjustments as well as clinical and laboratory monitoring may be appropriate for some drugs whenever momelotinib is added to or withdrawn from therapy. The prescribing information for the BCRP substrate should consulted for further information.

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.