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drug transporters

Interaction of Hydroxychloroquine with Pharmacokinetically Important Drug Transporters

October 1, 2020 - 15:20 -- Open Access
Author(s): 
Weiss J, Bajraktari-Sylejmani G, Haefeli WE
Reference: 
Pharmaceutics. 2020 Sep 25;12(10):E919

Hydroxychloroquine is used to treat malaria and autoimmune diseases, and its potential use against COVID-19 is currently under investigation. Thus far, information on interactions of hydroxychloroquine with drug transporters mediating drug-drug interactions is limited. We assessed the inhibition of important efflux (P-glycoprotein (P-gp), breast cancer resistance protein (BCRP)) and uptake transporters (organic anion transporting polypeptide (OATP)-1B1, OATP1B3, OATP2B1) by hydroxychloroquine, tested its P-gp and BCRP substrate characteristics, and evaluated the induction of pharmacokinetically relevant genes regulated by the nuclear pregnane X (PXR) (CYP3A4, ABCB1) and aryl hydrocarbon receptor (AhR) (CYP1A1, CYP1A2).

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