Drug Interaction Report

GENERALLY AVOID: Coadministration of revefenacin with inhibitors of organic anion transporting polypeptide (OATP) 1B1 and/or 1B3 may increase systemic exposure to its active metabolite, which has been reported to be a substrate of the hepatic uptake transporters. No pharmacokinetic data are available, but increased anticholinergic adverse effects such as mydriasis, blurred vision, heat intolerance, fever, dry mouth, tachycardia, urinary retention, constipation, and glaucoma (onset or exacerbation) may occur. In study patients, revefenacin was rapidly converted to its active metabolite following inhaled administration, and plasma exposures of the metabolite exceeded those of revefenacin by approximately 4- to 6-fold. The activity of the metabolite at target muscarinic receptors is approximately one-third to one-tenth that of revefenacin and could potentially contribute to systemic antimuscarinic effects at therapeutic doses.

MANAGEMENT: Concomitant use of revefenacin with OATP 1B1 and/or 1B3 inhibitors is not recommended.