Gemfibrozil and its glucuronide inhibit the hepatic uptake of pravastatin mediated by OATP1B1

References

• Abdul-Ghaffar NU, El-Sonbaty MR. Pancreatitis and rhabdomyolysis associated with lovastatin-gemfibrozil therapy. Journal of Clinical Gastroenterology 1995; 21: 340–341
   PubMed Web of Science ®Google Scholar
• Abe T, Kakyo M, Tokui T, Nakagomi R, Nishio T, Nakai D, Nomura H, Unno M, Suzuki M, Naitoh T, et al. Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1. Journal of Biological Chemistry 1999; 274: 17159–17163
   PubMed Web of Science ®Google Scholar
• Bruno-Joyce J, Dugas JM, MacCausland OE. Cerivastatin and gemfibrozilassociated rhabdomyolysis. Annals of Pharmacotherapy 2001; 35: 1016–1019
   PubMed Web of Science ®Google Scholar
• Chan LM, Lowes S, Hirst BH. The ABCs of drug transport in intestine and liver: Efflux proteins limiting drug absorption and bioavailability. European Journal of Pharmaceutical Sciences 2004; 21: 25–51
   PubMed Web of Science ®Google Scholar
• Chang JT, Staffa JA, Parks M, Green L. Rhabdomyolysis with HMG-CoA reductase inhibitors and gemfibrozil combination therapy. Pharmacoepidemiol and Drug Safety 2004; 13: 417–426
   PubMed Web of Science ®Google Scholar
• Dix KJ, Coleman DP, Jeffcoat AR. Comparative metabolism and disposition of gemfibrozil in male and female Sprague-Dawley rats and Syrian golden hamsters. Drug Metabolism and Disposition 1999; 27: 138–146
   PubMed Web of Science ®Google Scholar
• Goldin A. Maintenance of Xenopus laevis and oocyte injection. Methods in Enzymology 1992; 207: 266–279
   PubMed Web of Science ®Google Scholar
• Groothuis GMM, Sandker GW, Prium J, Weert B, Slooff MJH, Meijer DKF. Comparison of human hepatocytes isolated from livers accepted or discarded for orthotopic transplantation_Toxicol In Vitro. 1995; 9: 951–958
   Google Scholar
• Hatanaka T. Clinical pharmacokinetics of pravastatin: Mechanisms of pharmacokinetic events. Clinical Pharmacokinetics 2000; 39: 397–412
   PubMed Web of Science ®Google Scholar
• Hirano M, Maeda K, Hayashi H, Kusuhara H, Sugiyama Y. Bile salt export pump (BSEP/ABCB11) can transport a nonbile acid substrate, pravastatin. Journal of Pharmacology and Experimental Therapeutics 2005; 314: 876–882
   PubMed Web of Science ®Google Scholar
• Ishikawa T, Muller M, Klunemann C, Schaub T, Keppler D. ATP-dependent primary active transport of cysteinyl leukotrienes across liver canalicular membrane. Role of the ATP-dependent transport system for glutathione S-conjugates. Journal of Biological Chemistry 1990; 265: 19279–19286
   PubMed Web of Science ®Google Scholar
• Kyrklund C, Backman JT, Neuvonen M, Neuvonen PJ. Gemfibrozil increases plasma pravastatin concentrations and reduces pravastatin renal clearance. Clinical Pharmacology and Therapeutics 2003; 73: 538–544
   PubMed Web of Science ®Google Scholar
• Letschert K, Komatsu M, Hummel-Eisenbeiss J, Keppler D. Vectorial transport of the peptide CCK-8 by double-transfected MDCKII cells stably expressing the organic anion transporter OATP1B3 (OATP8) and the export pump ABCC2. Journal of Pharmacology and Experimental Therapeutics 2005; 313: 549–556
   PubMed Web of Science ®Google Scholar
• Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y. Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. Journal of Pharmacology and Experimental Therapeutics 2005; 314: 1059–1067
   PubMed Web of Science ®Google Scholar
• Miller DB, Spence JD. Clinical pharmacokinetics of fibric acid derivatives (fibrates). Clinical Pharmacokinetics 1998; 34: 155–162
   PubMed Web of Science ®Google Scholar
• Nakagomi-Hagihara R, Nakai D, Kawai K, Yoshigae Y, Tokui T, Abe T, Ikeda T. Inhibition of human organic anion transporter 3 mediated pravastatin transport by gemfibrozil and the metabolites in humans. Xenobiotica 2007, (in press)
   Web of Science ®Google Scholar
• Nakai D, Nakagomi R, Furuta Y, Tokui T, Abe T, Ikeda T, Nishimura K. Human liver-specific organic anion transporter, LST-1, mediates uptake of pravastatin by human hepatocytes. Journal of Pharmacology and Experimental Therapeutics 2001; 297: 861–867
   PubMed Web of Science ®Google Scholar
• Niemi M, Schaeffeler E, Lang T, Fromm MF, Neuvonen M, Kyrklund C, Backman JT, Kerb R, Schwab M, Neuvonen PJ, et al. High plasma pravastatin concentrations are associated with single nucleotide polymorphisms and haplotypes of organic anion transporting polypeptide-C (OATP-C, SLCO1B1). Pharmacogenetics 2004; 14: 429–440
   PubMedGoogle Scholar
• Niemi M, Neuvonen PJ, Hofmann U, Backman JT, Schwab M, Lutjohann D, von Bergmann K, Eichelbaum M, Kivisto KT. Acute effects of pravastatin on cholesterol synthesis are associated with SLCO1B1 (encoding OATP1B1) haplotype *17. Pharmacogenetics and Genomics 2005; 15: 303–309
   PubMed Web of Science ®Google Scholar
• Nishizato Y, Ieiri I, Suzuki H, Kimura M, Kawabata K, Hirota T, Takane H, Irie S, Kusuhara H, Urasaki Y, et al. Polymorphisms of OATP-C (SLC21A6) and OAT3 (SLC22A8) genes: Consequences for pravastatin pharmacokinetics. Clinical Pharmacology and Therapeutics 2003; 73: 554–565
   PubMed Web of Science ®Google Scholar
• Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I. Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. Journal of Pharmacology and Experimental Therapeutics 2004; 308: 438–445
   PubMed Web of Science ®Google Scholar
• Ogilvie BW, Zhang D, Li W, Rodrigues AD, Gipson AE, Holsapple J, Toren P, Parkinson A. Glucuronidation converts gemfibrozil to a potent, metabolism-dependent inhibitor of CYP2C8: implications for drug-drug interactions. Drug Metabolism and Disposition 2006; 34: 191–197
   PubMed Web of Science ®Google Scholar
• Okerholm RA, Keeley FJ, Peterson FE, Glazko AJ. The metabolism of gemfibrozil. Proceedings of the Royal Society of Medicine 1976; 69(Suppl 2)11–14
   PubMedGoogle Scholar
• Prueksaritanont T, Zhao JJ, Ma B, Roadcap BA, Tang C, Qiu Y, Liu L, Lin JH, Pearson PG, Baillie TA. Mechanistic studies on metabolic interactions between gemfibrozil and statins. Journal of Pharmacology and Experimental Therapeutics 2002; 301: 1042–1051
   PubMed Web of Science ®Google Scholar
• Quion JA, Jones PH. Clinical pharmacokinetics of pravastatin. Clinical Pharmacokinetics 1994; 27: 94–103
   PubMed Web of Science ®Google Scholar
• Roca B, Calvo B, Monferrer R. Severe rhabdomyolysis and cerivastatingemfibrozil combination therapy. Annals of Pharmacotherapy 2002; 36: 730–731
   PubMed Web of Science ®Google Scholar
• Shitara Y, Sugiyama Y. Pharmacokinetic and pharmacodynamic alterations of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors: Drug–drug interactions and interindividual differences in transporter and metabolic enzyme functions. Pharmacology and Therapeutics 2006; 112: 71–105
   PubMed Web of Science ®Google Scholar
• Shitara Y, Hirano M, Sato H, Sugiyama Y. Gemfibrozil and its glucuronide inhibit the organic anion transporting polypeptide 2 (OATP2/OATP1B1:SLC21A6)-mediated hepatic uptake and CYP2C8-mediated metabolism of cerivastatin: Analysis of the mechanism of the clinically relevant drug-drug interaction between cerivastatin and gemfibrozil. Journal of Pharmacology and Experimental Therapeutics 2004; 311: 228–236
   PubMed Web of Science ®Google Scholar
• Todd PA, Ward A. Gemfibrozil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in dyslipidaemia Drugs 1988; 36: 314–339
   Google Scholar
• Tokui T, Nakai D, Nakagomi R, Yawo H, Abe T, Sugiyama Y. Pravastatin, an HMG-CoA reductase inhibitor, is transported by rat organic anion transporting polypeptide, oatp2. Pharmaceutical Research 1999; 16: 904–908
   PubMed Web of Science ®Google Scholar
• Wu CP, Klokouzas A, Hladky SB, Ambudkar SV, Barrand MA. Interactions of mefloquine with ABC proteins, MRP1 (ABCC1) and MRP4 (ABCC4) that are present in human red cell membranes. Biochemical Pharmacology 2005; 70: 500–510
   PubMed Web of Science ®Google Scholar
• Yamazaki M, Suzuki H, Hanano M, Tokui T, Komai T, Sugiyama Y. Na+-independent multispecific anion transporter mediates active transport of pravastatin into rat liver. American Journal of Physiology 1993; 264: G36–G44
   PubMed Web of Science ®Google Scholar
• Yamazaki M, Akiyama S, Ni’inuma K, Nishigaki R, Sugiyama Y. Biliary excretion of pravastatin in rats: Contribution of the excretion pathway mediated by canalicular multispecific organic anion transporter. Drug Metabolism and Disposition 1997; 25: 1123–1129
   PubMed Web of Science ®Google Scholar
• Yamazaki M, Li B, Louie SW, Pudvah NT, Stocco R, Wong W, Abramovitz M, Demartis A, Laufer R, Hochman JH, et al. Effects of fibrates on human organic anion-transporting polypeptide 1B1-, multidrug resistance protein 2- and P-glycoprotein-mediated transport. Xenobiotica 2005; 35: 737–753
   PubMed Web of Science ®Google Scholar