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Organic anion-transporting polypeptides (OATPs) mediate the hepatic uptake of many drugs. Hepatic uptake is crucial for the therapeutic effect of pravastatin, a cholesterol-lowering drug and OATP1A/1B substrate. We aimed to gain empirical insight into the relationship between OATPs and pravastatin pharmacokinetics and toxicity. We therefore compared the distribution and toxicity of pravastatin in wild-type and Oatp1a/1b-null mice. Intestinal absorption of pravastatin was not affected by Oatp1a/1b absence, but systemic plasma exposure (AUC) increased up to 30-fold after oral bolus administration. This increased plasma exposure resulted from reduced hepatic uptake, as evident from 10 to 100-fold lower liver-to-plasma concentration ratios. However, the reductions in liver exposure were far smaller (<2-fold) than the increases in plasma exposure. Reduced pravastatin liver uptake in Oatp1a/1b-null mice was more obvious shortly after intravenous administration, with 8-fold lower biliary pravastatin excretion. A...
| Authors: | Dilek Iusuf; Rolf W. Sparidans; Anita van Esch; Mike Hobbs; Kathryn E. Kenworthy; Evita van de Steeg; Els Wagenaar; Jos H. Beijnen; Alfred H. Schinkel | |
| Journal: | Molecular Pharmaceutics | |
| Year: | 2012 | |
| DOI: | 10.1021/mp300108c | |
| Publication date: | 03-08-2012 |
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