Drug-drug interactions between rosuvastatin and oral antidiabetic drugs occurring at the level of OATP1B1
| Autor: | Marieke Schreurs, Jeroen DeGroot, Heleen M. Wortelboer, Maarten T. Huisman, E. van de Steeg, Kitty C.M. Verhoeckx, Roeland Hanemaaijer, D. Ripken, Miriam Verwei, Rick Greupink, Frans G. M. Russel, Irene Nooijen, Maria L. H. Vlaming, Mario Monshouwer |
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| Rok vydání: | 2012 |
| Předmět: |
medicine.medical_specialty
Pharmaceutical Science Administration Oral Organic Anion Transporters Pharmacology Transfection Tolbutamide Tandem Mass Spectrometry Internal medicine medicine Humans Hypoglycemic Agents Gliclazide Rosuvastatin Drug Interactions Rosuvastatin Calcium Sulfonamides Dose-Response Relationship Drug Estradiol Liver-Specific Organic Anion Transporter 1 Troglitazone Membrane transport and intracellular motility IGMD 9: Renal disorder [NCMLS 5] Fluorobenzenes Glimepiride Kinetics Endocrinology HEK293 Cells Pyrimidines Pioglitazone medicine.drug Glipizide Chromatography Liquid |
| Zdroj: | Drug Metabolism and Disposition, 41, 3, pp. 592-601 Drug Metabolism and Disposition, 41, 592-601 |
| ISSN: | 1521-009X 0090-9556 |
| Popis: | Organic anion-transporting polypeptide 1B1 (OATP1B1) is an important hepatic uptake transporter, of which the polymorphic variant OATP1B1*15 (Asn130Asp and Val174Ala) has been associated with decreased transport activity. Rosuvastatin is an OATP1B1 substrate and often concomitantly prescribed with oral antidiabetics in the clinic. The aim of this study was to investigate possible drug-drug interactions between these drugs at the level of OATP1B1 and OATP1B1*15. We generated human embryonic kidney (HEK)293 cells stably overexpressing OATP1B1 or OATP1B1*15 that showed similar protein expression levels of OATP1B1 and OATP1B1*15 at the cell membrane as measured by liquid chromatography-tandem mass spectrometry. In HEK-OATP1B1*15 cells, the Vmax for OATP1B1-mediated transport of E217b-G (estradiol 17b-D-glucuronide) was decreased |
| Databáze: | OpenAIRE |
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