Drug Interactions between cobicistat / darunavir and ticagrelor

CONTRAINDICATED: Coadministration with potent inhibitors of CYP450 3A4 may significantly increase the plasma concentrations of ticagrelor, which is primarily metabolized by the isoenzyme. In healthy volunteers, administration of ticagrelor in combination with the potent CYP450 3A4 inhibitor ketoconazole resulted in increased ticagrelor peak plasma concentration (Cmax) and systemic exposure (AUC) by 2.4-fold and 7.3-fold, respectively, and reduced Cmax and AUC of the active metabolite by 89% and 56%, respectively.

MANAGEMENT: Concomitant use of ticagrelor with potent CYP450 3A4 inhibitors is considered contraindicated by some foreign authorities. The U.S. labeling for ticagrelor recommends avoiding use with potent CYP450 3A4 inhibitors. Labeling for itraconazole, a potent CYP450 3A4 inhibitor, specifically contraindicates use with ticagrelor during and for 2 weeks after treatment with itraconazole.

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MONITOR: Coadministration with moderate inhibitors of CYP450 3A4 may increase the plasma concentrations of ticagrelor, which is primarily metabolized by the isoenzyme. In healthy volunteers, administration of ticagrelor in combination with the moderate CYP450 3A4 inhibitor diltiazem resulted in increased ticagrelor peak plasma concentration (Cmax) and systemic exposure (AUC) by 69% and 174%, respectively. For the active metabolite, the Cmax was decreased by 38% and the AUC was unchanged. Ticagrelor had no effect on the plasma levels of diltiazem.

MANAGEMENT: Although administration with moderate CYP450 3A4 inhibitors is thought to be generally safe, it may be advisable to monitor pharmacologic response to ticagrelor more closely following the addition and withdrawal of these agents. Discontinuation of the concomitant medication may be required if an interaction is suspected.

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