Regular ArticleIntestinal Absorption of HMG-CoA Reductase Inhibitor Pitavastatin Mediated by Organic Anion Transporting Polypeptide and P-Glycoprotein/Multidrug Resistance 1
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2016, Journal of Pharmaceutical SciencesCitation Excerpt :Previous studies indicate that the hepatic uptake of pitavastatin and many other statins is strongly dependent on several members of the OATP family, collectively accounting for 60%-90% of the hepatic uptake (Vildhede et al., unpublished data, 2015).69,85,86 An involvement of OATPs in the intestinal absorption of pitavastatin has also been suggested,87 but the extent to which absorptive—and exorptive—intestinal transporters contribute to the overall pitavastatin absorption in humans has not been quantified. Transport experiments in Caco-2 cells showed that OATP2B1 contributed between 60% and 70% of the total transport rate in the concentration range expected in the small intestine after standard clinical doses (1-4 mg).