Ivermectin interacts with human ABCG2.
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.
Jani
Márton
M
Solvo Biotechnology, Budaörs, Hungary.
Makai
Ildikó
I
Kis
Emese
E
Szabó
Pál
P
Nagy
Tünde
T
Krajcsi
Péter
P
Lespine
Anne
A
D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters / Q000037:antagonists & inhibitors*; D000977:Antiparasitic Agents / Q000494:pharmacology*; D001693:Biological Transport, Active / Q000187:drug effects; D002460:Cell Line; D002462:Cell Membrane / Q000378:metabolism; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D004970:Estrone / Q000031:analogs & derivatives / Q000493:pharmacokinetics; D006801:Humans; D007559:Ivermectin / Q000494:pharmacology*; D007700:Kinetics; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors*
C116614:ABCG2 protein, human; D000070997:ATP Binding Cassette Transporter, Subfamily G, Member 2; D018528:ATP-Binding Cassette Transporters; D000977:Antiparasitic Agents; D004791:Enzyme Inhibitors; D009363:Neoplasm Proteins; D004970:Estrone; D007559:Ivermectin; C017296:estrone sulfate