Ivermectin Interacts With Human ABCG2
Résumé
Ivermectin is an antiparasitic drug frequently administered to humans. It has alimited brain exposure that is attributed to the efflux activity of ABCB1/Abcb1. ABCG2/Abcg2 isalso a major transporter present in most pharmacologically important barriers. However,interaction of ivermectin with Abcg2 shows species specificity and in many studies wasconfounded by the masking effect of ABCB1/Abcb1. In this study using cellular and membraneassays we show that ivermectin displays a high-affinity interaction with human ABCG2with IC50 values in the 1–1.5 mM range. This interaction may have implications in humanABCG2-mediated drug–drug interactions of ivermectin.
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