| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 2486783 | Journal of Pharmaceutical Sciences | 2011 | 4 Pages |
Abstract
ABSTRACTIvermectin is an antiparasitic drug frequently administered to humans. It has a limited brain exposure that is attributed to the efflux activity of ABCB1/Abcb1. ABCG2/Abcg2 is also a major transporter present in most pharmacologically important barriers. However, interaction of ivermectin with Abcg2 shows species specificity and in many studies was confounded by the masking effect of ABCB1/Abcb1. In this study using cellular and membrane assays we show that ivermectin displays a high-affinity interaction with human ABCG2 with IC50 values in the 1–1.5 µM range. This interaction may have implications in human ABCG2-mediated drug–drug interactions of ivermectin.
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Authors
Márton Jani, Ildikó Makai, Emese Kis, Pál Szabó, Tünde Nagy, Péter Krajcsi, Anne Lespine,