Ivermectin interacts with human ABCG2.

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Jani M, Makai I, Kis E, Szabo P, Nagy T, Krajcsi P, Lespine A

Ivermectin interacts with human ABCG2.

J Pharm Sci. 2011 Jan;100(1):94-7. doi: 10.1002/jps.22262. Epub 2010 Jun 22.

PubMed ID

20574995 [ View in PubMed

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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 IC(50) values in the 1-1.5 microM range. This interaction may have implications in human ABCG2-mediated drug-drug interactions of ivermectin.

DrugBank Data that Cites this Article

Drug Transporters

Drug	Transporter	Kind	Organism	Pharmacological Action	Actions
Ivermectin	ATP-binding cassette sub-family G member 2	Protein	Humans	Unknown	Substrate	Details
Ivermectin	P-glycoprotein 1	Protein	Humans	Unknown	Substrate Inhibitor Inducer	Details