Drug Interaction Report

GENERALLY AVOID: Coadministration with oral tedizolid may increase the plasma concentrations and the risk of adverse effects of orally administered drugs that are substrates of the breast cancer resistance protein (BCRP) transporter. The proposed mechanism is decreased clearance due to inhibition of BCRP-mediated intestinal efflux by tedizolid. Administration of a single 10 mg dose of rosuvastatin, a known BCRP substrate, to healthy subjects who had received multiple daily doses of tedizolid 200 mg increased rosuvastatin peak plasma concentration (Cmax) and systemic exposure (AUC) by 55% and 70%, respectively.

MANAGEMENT: Consider temporarily interrupting treatment with the BCRP substrate during treatment with tedizolid, especially for BCRP substrates with a narrow therapeutic index. If coadministration cannot be avoided, monitor for adverse reactions related to concomitantly administered BCRP substrate. The prescribing information for concomitant medications should be consulted to assess the benefits versus risks of coadministration and for any dosage adjustments that may be required.

Food enhances the oral absorption and bioavailability of tenofovir, the active entity of tenofovir disoproxil fumarate. According to the product labeling, administration of the drug following a high-fat meal increased the mean peak plasma concentration (Cmax) and area under the concentration-time curve (AUC) of tenofovir by approximately 14% and 40%, respectively, compared to administration in the fasting state. However, administration with a light meal did not significantly affect the pharmacokinetics of tenofovir compared to administration in the fasting state. Food delays the time to reach tenofovir Cmax by approximately 1 hour. Tenofovir disoproxil fumarate may be administered without regard to meals.