Drug Interaction Report

CONTRAINDICATED: Coadministration with potent inhibitors of CYP450 2C8 may significantly increase the plasma concentrations of selexipag and its active metabolite. In 20 healthy male subjects, treatment with the potent CYP450 2C8 inhibitor gemfibrozil (600 mg twice a day on days 1 to 9) in combination with selexipag (400 mcg once in the morning on day 4) resulted in a 1.4 and 2-fold increase in the Cmax and AUC of selexipag, respectively, and a 3.6 and 11.1-fold increase in the Cmax and AUC of its active metabolite, respectively.

MANAGEMENT: Concomitant use of selexipag with potent CYP450 2C8 inhibitors is contraindicated by the manufacturer.

Food prolongs the gastrointestinal absorption of selexipag. When taken with food, the time to peak concentration (Tmax) was delayed and peak plasma concentration (Cmax) was approximately 30% lower. Selexipag systemic exposure (AUC) and that of its active metabolite did not significantly change, however. Selexipag may be taken with or without food. Tolerability may be improved when taken with food.