Ivermectin interacts with human ABCG2

Márton Jani, Ildikó Makai, Emese Kis, Pál Szabó, Tünde Nagy, Péter Krajcsi, Anne Lespine

Research output: Article

26 Citations (Scopus)

Abstract

Ivermectin 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 1-1.5μM range. This interaction may have implications in human ABCG2-mediated drug-drug interactions of ivermectin.

Original languageEnglish
Pages (from-to)94-97
Number of pages4
JournalJournal of pharmaceutical sciences
Volume100
Issue number1
DOIs
Publication statusPublished - jan. 2011

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ASJC Scopus subject areas

  • Pharmaceutical Science

Cite this

Jani, M., Makai, I., Kis, E., Szabó, P., Nagy, T., Krajcsi, P., & Lespine, A. (2011). Ivermectin interacts with human ABCG2. Journal of pharmaceutical sciences, 100(1), 94-97. https://doi.org/10.1002/jps.22262