Article
OCT1 mediates hepatic uptake of sumatriptan and loss-of-function OCT1 polymorphisms affect sumatriptan pharmacokinetics.
Clinical pharmacology and therapeutics - 1 Jun 2016
Matthaei J, Kuron D, Faltraco F, Knoch T, Dos Santos Pereira J N, Abu Abed M, Prukop T, Brockmöller J, Tzvetkov M V
Abstract excerpt
The low bioavailability of the anti-migraine drug sumatriptan is partially caused by first-pass hepatic metabolism. In this study, we analyzed the impact of the hepatic organic cation transporter OCT1 on sumatriptan cellular uptake, and of OCT1 polymorphisms on sumatriptan pharmacokinetics. OCT1 transported sumatriptan with high capacity and sumatriptan uptake into human hepatocytes was strongly inhibited by the...
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