Interaction of Sulfonylureas with Liver Uptake Transporters OATP1B1 and OATP1B3

Basic & Clinical Pharmacology & Toxicology
Yu ChenChunhua Xia

Abstract

Sulfonylureas (SUs) such as glibenclamide, gliclazide, glimepiride, glipizide and gliquidone are one of the first oral medicines available for the treatment of type 2 diabetes and are widely used for the treatment of hyperglycaemia. The hepatic transporters, organic anion transporting polypeptide 1B1 (OATP1B1) and organic anion transporting polypeptide 1B3 (OATP1B3), play an important role in the disposition of a variety of drugs by mediating their uptake from blood into hepatocytes. Drug-drug interactions mediated by OATP1B1/1B3 may result in the hepatic transporting change for drug substrates. The inhibitory effects of glibenclamide and glimepiride on sulfobromophthalein (BSP) uptake have been previously studied, and glibenclamide has been reported as the substrate of OATP1B3, but it remains unclear whether other SUs such as gliclazide, glipizide and gliquidone are substrates of OATP1B1 and OATP1B3. Here, we investigated the relationship between the five most commonly applied SUs (glibenclamide, gliclazide, glimepiride, glipizide, gliquidone) and OATP1B1 and OATP1B3. We performed uptake and inhibition assays in HEK293T cells stably expressing OATP1B1 or OATP1B3, respectively, and established a liquid chromatography-mass spect...Continue Reading

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Citations

Jun 11, 2019·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·Yingmin NieChunshan Gui
Jan 23, 2021·Pharmaceutics·Maria D AuxteroAna I Fernandes
Jun 3, 2021·Journal of Personalized Medicine·Tanja DujicAida Kulo
Jul 31, 2021·Biopharmaceutics & Drug Disposition·Jeffry Adiwidjaja, Lucy Sasongko
Oct 6, 2021·Diabetes Care·Adem Y DawedUNKNOWN MetGen Plus investigators:

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