Drug Interaction Report

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as well as clinical and laboratory monitoring may be appropriate for some drugs whenever momelotinib is added to or withdrawn from therapy.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.