01/01/2011 - Role of transporters in bioavailability of nutraceuticals and in risk assessement of environmental toxicants

Ivermectin interacts with human ABCG2.

M. Jani, I. Makai, E. Kis, P. Szabó, T. Nagy, P. Krajcsi and A. Lespine J PHARM SCI, J Pharm Sci. 2011 Jan;100(1):94-7


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

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