Drug Interaction Report

GENERALLY AVOID: Coadministration with rolapitant may increase the plasma concentrations of drugs that are substrates of the breast cancer resistance protein (BCRP) transporter. When a 500 mg dose of sulfasalazine, a BCRP substrate, was administered with a 180 mg dose of rolapitant on day 1 of a pharmacokinetic study, sulfasalazine peak plasma concentration (Cmax) and systemic exposure (AUC) increased by 140% and 130%, respectively. When sulfasalazine was administered on day 8 without rolapitant, Cmax and AUC increased by 17% and 32%, respectively. The duration of BCRP inhibition was not studied beyond 7 days.

MANAGEMENT: Concomitant use of rolapitant with drugs that are BCRP substrates should generally be avoided. If concomitant administration is unavoidable, caution is advised, particularly with drugs that have a narrow therapeutic range such as methotrexate, topotecan, and irinotecan. Dosage adjustments as well as clinical and laboratory monitoring may be appropriate for some drugs whenever rolapitant is added to or withdrawn from therapy. The lowest effective dose of rosuvastatin should be used when coadministered with rolapitant.