Drug Interaction Report

MONITOR: Coadministration with inducers of CYP450 3A4 and/or P-glycoprotein may decrease the plasma concentrations of gilteritinib, which is a substrate of both the isoenzyme and the efflux transporter. When gilteritinib was coadministered with rifampin, a combined P-gp and potent CYP450 3A4 inducer, gilteritinib peak plasma concentration (Cmax) and systemic exposure (AUC) decreased by 30% and 70%, respectively, compared to administration of gilteritinib alone. Reduced efficacy of gilteritinib may occur. The interaction has not been studied with other, less potent inducers or lone inducers of CYP450 3A4 or P-gp.

MANAGEMENT: The potential for diminished pharmacologic effects of gilteritinib should be considered during coadministration with CYP450 3A4 and/or P-gp inducers. Alternative treatments may be required if an interaction is suspected.

ADJUST DOSING INTERVAL: Coadministration with food increases the oral bioavailability of etravirine. The mechanism is unknown. Compared to administration following a meal, the systemic exposure (AUC) to etravirine was decreased by about 50% when the drug was administered under fasting conditions. The types of meal studied (ranging from 345 kilocalories containing 17 grams fat to 1160 kilocalories containing 70 grams fat) did not appear to make a difference with respect to impact on etravirine bioavailability.

MANAGEMENT: Etravirine should always be administered following a meal.