670
Views
49
CrossRef citations to date
0
Altmetric
Reviews

Identification of interspecies difference in hepatobiliary transporters to improve extrapolation of human biliary secretion

, PhD
Pages 1175-1187 | Published online: 17 Jul 2009

Bibliography

  • Arias IM, Che M, Gatmaitan Z, et al. The biology of the bile canaliculus, 1993. Hepatology 1993;17(2):318-29
  • Muller M, Jansen PL. The secretory function of the liver: new aspects of hepatobiliary transport. J Hepatol 1998;28(2):344-54
  • Van Damme B, Fevery J, Heirwegh KP. Altered composition of bilirubin conjugates in rat bile after obstruction of the common bile duct. Experientia 1971;27(1):27-8
  • Kuenzle CC. Bilirubin conjugates of human bile. The excretion of bilirubin as the acyl glycosides of aldobiouronic acid, pseudoaldobiouronic acid and hexuronosylhexuronic acid, with a branched-chain hexuronic acid as one of the components of the hexuronosylhexuronide. Biochem J 1970;119(3):411-35
  • Durham S, Vore M. Taurocholate and steroid glucuronides: mutual protection against cholestasis in the isolated perfused rat liver. J Pharmacol Exp Ther 1986;237(2):490-5
  • Slikker W Jr, Vore M, Bailey JR, et al. Hepatotoxic effects of estradiol-17 beta-D-glucuronide in the rat and monkey. J Pharmacol Exp Ther 1983;225(1):138-43
  • Mahmood I, Sahajwalla C. Interspecies scaling of biliary excreted drugs. J Pharm Sci 2002;91(8):1908-14
  • Davies B, Morris T. Physiological parameters in laboratory animals and humans. Pharm Res 1993;10(7):1093-5
  • Shou M, Lu W, Kari PH, et al. Population pharmacokinetic modeling for enterohepatic recirculation in Rhesus monkey. Eur J Pharm Sci 2005;26(2):151-61
  • Roberts MS, Magnusson BM, Burczynski FJ, et al. Enterohepatic circulation: physiological, pharmacokinetic and clinical implications. Clin Pharmacokinet 2002;41(10):751-90
  • Suzuki H, Sugiyama Y. Transporters for bile acids and organic anions. Pharm Biotechnol 1999;12:387-439
  • Keppler D, Arias IM. Hepatic canalicular membrane. Introduction: transport across the hepatocyte canalicular membrane. FASEB J 1997;11(1):15-8
  • Muller M, Jansen PL. Molecular aspects of hepatobiliary transport. Am J Physiol 1997;272(6 Pt 1):G1285-303
  • Kullak-Ublick GA, Beuers U, Paumgartner G. Hepatobiliary transport. J Hepatol 2000;32(Suppl 1):3-18
  • Kullak-Ublick GA, Ismair MG, Stieger B, et al. Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology 2001;120(2):525-33
  • Kullak-Ublick GA, Stieger B, Hagenbuch B, et al. Hepatic transport of bile salts. Semin Liver Dis 2000;20(3):273-92
  • Keppler D, Konig J. Hepatic canalicular membrane 5: expression and localization of the conjugate export pump encoded by the MRP2 (cMRP/cMOAT) gene in liver. FASEB J 1997;11(7):509-16
  • Kamimoto Y, Gatmaitan Z, Hsu J, et al. The function of Gp170, the multidrug resistance gene product, in rat liver canalicular membrane vesicles. J Biol Chem 1989;264(20):11693-8
  • Schinkel AH, Mol CA, Wagenaar E, et al. Multidrug resistance and the role of P-glycoprotein knockout mice. Eur J Cancer 1995;31A(7-8):1295-8
  • Smit JJ, Schinkel AH, Oude Elferink RP, et al. Homozygous disruption of the murine mdr2 P-glycoprotein gene leads to a complete absence of phospholipid from bile and to liver disease. Cell 1993;75(3):451-62
  • van Asperen J, van Tellingen O, Tijssen F, et al. Increased accumulation of doxorubicin and doxorubicinol in cardiac tissue of mice lacking mdr1a P-glycoprotein. Br J Cancer 1999;79(1):108-13
  • Lecureur V, Courtois A, Payen L, et al. Expression and regulation of hepatic drug and bile acid transporters. Toxicology 2000;153(1-3):203-19
  • Gerloff T, Stieger B, Hagenbuch B, et al. The sister of P-glycoprotein represents the canalicular bile salt export pump of mammalian liver. J Biol Chem 1998;273(16):10046-50
  • Stieger B, Meier Y, Meier PJ. The bile salt export pump. Pflugers Arch 2007;453(5):611-20
  • Strautnieks SS, Bull LN, Knisely AS, et al. A gene encoding a liver-specific ABC transporter is mutated in progressive familial intrahepatic cholestasis. Nat Genet 1998;20(3):233-8
  • Noe J, Hagenbuch B, Meier PJ, et al. Characterization of the mouse bile salt export pump overexpressed in the baculovirus system. Hepatology 2001;33(5):1223-31
  • Byrne JA, Strautnieks SS, Mieli-Vergani G, et al. The human bile salt export pump: characterization of substrate specificity and identification of inhibitors. Gastroenterology 2002;123(5):1649-58
  • Hirano M, Maeda K, Hayashi H, et al. Bile salt export pump (BSEP/ABCB11) can transport a nonbile acid substrate, pravastatin. J Pharmacol Exp Ther 2005;314(2):876-82
  • Hirano H, Kurata A, Onishi Y, et al. High-speed screening and QSAR analysis of human ATP-binding cassette transporter ABCB11 (bile salt export pump) to predict drug-induced intrahepatic cholestasis. Mol Pharm 2006;3(3):252-65
  • Ogawa K, Suzuki H, Hirohashi T, et al. Characterization of inducible nature of MRP3 in rat liver. Am J Physiol Gastrointest Liver Physiol 2000;278(3):G438-46
  • Allikmets R, Schriml LM, Hutchinson A, et al. A human placenta-specific ATP-binding cassette gene (ABCP) on chromosome 4q22 that is involved in multidrug resistance. Cancer Res 1998;58(23):5337-9
  • Suzuki M, Suzuki H, Sugimoto Y, et al. ABCG2 transports sulfated conjugates of steroids and xenobiotics. J Biol Chem 2003;278(25):22644-9
  • Hirano M, Maeda K, Matsushima S, et al. Involvement of BCRP (ABCG2) in the biliary excretion of pitavastatin. Mol Pharmacol 2005;68(3):800-7
  • Aleksunes LM, Slitt AL, Maher JM, et al. Induction of Mrp3 and Mrp4 transporters during acetaminophen hepatotoxicity is dependent on Nrf2. Toxicol Appl Pharmacol 2008;226(1):74-83
  • Borst P, de Wolf C, van de Wetering K. Multidrug resistance-associated proteins 3, 4, and 5. Pflugers Arch 2007;453(5):661-73
  • Beck K, Hayashi K, Dang K, et al. Analysis of ABCC6 (MRP6) in normal human tissues. Histochem Cell Biol 2005;123(4-5):517-28
  • Akita H, Suzuki H, Sugiyama Y. Sinusoidal efflux of taurocholate is enhanced in Mrp2-deficient rat liver. Pharm Res 2001;18(8):1119-25
  • Shitara Y, Sato H, Sugiyama Y. Evaluation of drug-drug interaction in the hepatobiliary and renal transport of drugs. Annu Rev Pharmacol Toxicol 2005;45:689-723
  • Ahmed S, Vo NT, Thalhammer T, et al. Involvement of Mrp2 (Abcc2) in biliary excretion of moxifloxacin and its metabolites in the isolated perfused rat liver. J Pharm Pharmacol 2008;60(1):55-62
  • Sakurai A, Kurata A, Onishi Y, et al. Prediction of drug-induced intrahepatic cholestasis: in vitro screening and QSAR analysis of drugs inhibiting the human bile salt export pump. Expert Opin Drug Saf 2007;6(1):71-86
  • Merino G, van Herwaarden AE, Wagenaar E, et al. Sex-dependent expression and activity of the ATP-binding cassette transporter breast cancer resistance protein (BCRP/ABCG2) in liver. Mol Pharmacol 2005;67(5):1765-71
  • Allikmets R, Dean M. Cloning of novel ABC transporter genes. Methods Enzymol 1998;292:116-30
  • Merino G, van Herwaarden AE, Wagenaar E, et al. Sex-dependent expression and activity of the ATP-binding cassette transporter breast cancer resistance protein (BCRP/ABCG2) in liver. Mol Pharmacol 2005;67(5):1765-71
  • Zamek-Gliszczynski MJ, Hoffmaster KA, Humphreys JE, et al. Differential involvement of Mrp2 (Abcc2) and Bcrp (Abcg2) in biliary excretion of 4-methylumbelliferyl glucuronide and sulfate in the rat. J Pharmacol Exp Ther 2006;319(1):459-67
  • Enokizono J, Kusuhara H, Sugiyama Y. Involvement of breast cancer resistance protein (BCRP/ABCG2) in the biliary excretion and intestinal efflux of troglitazone sulfate, the major metabolite of troglitazone with a cholestatic effect. Drug Metab Dispos 2007;35(2):209-14
  • Kajosaari LI, Niemi M, Neuvonen M, et al. Cyclosporine markedly raises the plasma concentrations of repaglinide. Clin Pharmacol Ther 2005;78(4):388-99
  • Kullak-Ublick GA. Drug-induced cholestatic liver disease. Mol Pathog Cholestasis 2004;256-65
  • Moseley RH, Johnson TR, Morrissette JM. Inhibition of bile acid transport by cyclosporine A in rat liver plasma membrane vesicles. J Pharmacol Exp Ther 1990;253(3):974-80
  • Deters M, Klabunde T, Kirchner G, et al. Sirolimus/cyclosporine/tacrolimus interactions on bile flow and biliary excretion of immunosuppressants in a subchronic bile fistula rat model. Br J Pharmacol 2002;136(4):604-12
  • Funk C, Pantze M, Jehle L, et al. Troglitazone-induced intrahepatic cholestasis by an interference with the hepatobiliary export of bile acids in male and female rats. Correlation with the gender difference in troglitazone sulfate formation and the inhibition of the canalicular bile salt export pump (Bsep) by troglitazone and troglitazone sulfate. Toxicology 2001;167(1):83-98
  • Funk C, Ponelle C, Scheuermann G, et al. Cholestatic potential of troglitazone as a possible factor contributing to troglitazone-induced hepatotoxicity: in vivo and in vitro interaction at the canalicular bile salt export pump (Bsep) in the rat. Mol Pharmacol 2001;59(3):627-35
  • Paulusma CC, van Geer MA, Evers R, et al. Canalicular multispecific organic anion transporter/multidrug resistance protein 2 mediates low-affinity transport of reduced glutathione. Biochem J 1999;338 (Pt 2):393-401
  • Sugie M, Asakura E, Zhao YL, et al. Possible involvement of the drug transporters P glycoprotein and multidrug resistance-associated protein Mrp2 in disposition of azithromycin. Antimicrob Agents Chemother 2004;48(3):809-14
  • Moran D, De Buitrago JM, Fernandez E, et al. Inhibition of biliary glutathione secretion by cyclosporine A in the rat: possible mechanisms and role in the cholestasis induced by the drug. J Hepatol 1998;29(1):68-77
  • Ishizuka H, Konno K, Shiina T, et al. Species differences in the transport activity for organic anions across the bile canalicular membrane. J Pharmacol Exp Ther 1999;290(3):1324-30
  • Shilling AD, Azam F, Kao J, et al. Use of canalicular membrane vesicles (CMVs) from rats, dogs, monkeys and humans to assess drug transport across the canalicular membrane. J Pharmacol Toxicol Methods 2006;53(3):186-97
  • Lave T, Portmann R, Schenker G, et al. Interspecies pharmacokinetic comparisons and allometric scaling of napsagatran, a low molecular weight thrombin inhibitor. J Pharm Pharmacol 1999;51(1):85-91
  • Pahlman I, Andersson S, Gunnarsson K, et al. Extensive biliary excretion of the sulfasalazine analogue, susalimod, but different concentrations in the bile duct in various animal species correlating to species-specific hepatobiliary toxicity. Pharmacol Toxicol 1999;85(3):123-9
  • Ayrton A, Morgan P. Role of transport proteins in drug absorption, distribution and excretion. Xenobiotica 2001;31(8-9):469-97
  • Mahmood I. Interspecies scaling of biliary excreted drugs: a comparison of several methods. J Pharm Sci 2005;94(4):883-92
  • Kostrubsky VE, Vore M, Kindt E, et al. The effect of troglitazone biliary excretion on metabolite distribution and cholestasis in transporter-deficient rats. Drug Metab Dispos 2001;29(12):1561-6
  • Stieger B, Fattinger K, Madon J, et al. Drug- and estrogen-induced cholestasis through inhibition of the hepatocellular bile salt export pump (Bsep) of rat liver. Gastroenterology 2000;118(2):422-30
  • Kostrubsky VE, Strom SC, Hanson J, et al. Evaluation of hepatotoxic potential of drugs by inhibition of bile-acid transport in cultured primary human hepatocytes and intact rats. Toxicol Sci 2003;76(1):220-8
  • Lauer B, Tuschl G, Kling M, et al. Species-specific toxicity of diclofenac and troglitazone in primary human and rat hepatocytes. Chem Biol Interact 2009;179(1):17-24
  • Tuschl G, Lauer B, Mueller SO. Primary hepatocytes as a model to analyze species-specific toxicity and drug metabolism. Expert Opin Drug Metab Toxicol 2008;4(7):855-70
  • Gale EA. Lessons from the glitazones: a story of drug development. Lancet 2001;357(9271):1870-5
  • Skjodt NM, Davies NM. Clinical pharmacokinetics and pharmacodynamics of bromfenac. Clin Pharmacokinet 1999;36(6):399-408
  • Pacitto SR, Uetrecht JP, Boutros PC, et al. Changes in gene expression induced by tienilic Acid and sulfamethoxazole: testing the danger hypothesis. J Immunotoxicol 2007;4(4):253-66
  • Blum MD, Graham DJ, McCloskey CA. Temafloxacin syndrome: review of 95 cases. Clin Infect Dis 1994;18(6):946-50
  • Dedrick R, Bischoff KB, Zaharko DS. Interspecies correlation of plasma concentration history of methotrexate (NSC-740). Cancer Chemother Rep 1970;54(2):95-101
  • Ito K, Iwatsubo T, Kanamitsu S, et al. Quantitative prediction of in vivo drug clearance and drug interactions from in vitro data on metabolism, together with binding and transport. Annu Rev Pharmacol Toxicol 1998;38:461-99
  • Iwatsubo T, Hirota N, Ooie T, et al. Prediction of in vivo drug metabolism in the human liver from in vitro metabolism data. Pharmacol Ther 1997;73(2):147-71
  • Hayashi H, Takada T, Suzuki H, et al. Transport by vesicles of glycine- and taurine-conjugated bile salts and taurolithocholate 3-sulfate: a comparison of human BSEP with rat Bsep. Biochim Biophys Acta 2005;1738(1-3):54-62
  • Ward ES, Pollack GM, Brouwer KL. Probenecid-associated alterations in valproic acid pharmacokinetics in rats: can in vivo disposition of valproate glucuronide be predicted from in vitro formation data? Drug Metab Dispos 2000;28(12):1433-9
  • Ward ES, Pollack GM, Brouwer KL. Probenecid-associated alterations in valproate glucuronide hepatobiliary disposition: mechanistic assessment using mathematical modeling. J Pharmacol Exp Ther 2001;297(1):141-7
  • Ward KW, Azzarano LM, Bondinell WE, et al. Preclinical pharmacokinetics and interspecies scaling of a novel vitronectin receptor antagonist. Drug Metab Dispos 1999;27(11):1232-41
  • Li M, Yuan H, Li N, et al. Identification of interspecies difference in efflux transporters of hepatocytes from dog, rat, monkey and human. Eur J Pharm Sci 2008;35(1-2):114-26
  • Goh LB, Spears KJ, Yao D, et al. Endogenous drug transporters in in vitro and in vivo models for the prediction of drug disposition in man. Biochem Pharmacol 2002;64(11):1569-78
  • Lave T, Parrott N, Grimm HP, et al. Challenges and opportunities with modelling and simulation in drug discovery and drug development. Xenobiotica 2007;37(10-11):1295-310
  • Karim A, Kook C, Zitzewitz DJ, et al. Species differences in the metabolism and disposition of spironolactone. Drug Metab Dispos 1976;4(6):547-55
  • Duggan DE, Hooke KF, Noll RM, et al. Enterohepatic circulation of indomethacin and its role in intestinal irritation. Biochem Pharmacol 1975;24(19):1749-54
  • Chatfield DH, Green JN. Disposition and metabolism of benoxaprofen in laboratory animals and man. Xenobiotica 1978;8(3):133-44
  • Aldini R, Roda A, Morselli Labate A, et al. Species difference of the hepatic uptake of bile acids. Int J Gastroenterol 1986;19:1-4
  • Montagnani M, Aldini R, Roda A, et al. Species differences in hepatic bile acid uptake: comparative evaluation of taurocholate and tauroursodeoxycholate extraction in rat and rabbit. Comp Biochem Physiol A Physiol 1996;113(2):157-64
  • Katoh M, Suzuyama N, Takeuchi T, et al. Kinetic analyses for species differences in P-glycoprotein-mediated drug transport. J Pharm Sci 2006;95(12):2673-83
  • Booth-Genthe CL, Louie SW, Carlini EJ, et al. Development and characterization of LLC-PK1 cells containing Sprague-Dawley rat Abcb1a (Mdr1a): comparison of rat P-glycoprotein transport to human and mouse. J Pharmacol Toxicol Methods 2006;54(1):78-89
  • Baltes S, Gastens AM, Fedrowitz M, et al. Differences in the transport of the antiepileptic drugs phenytoin, levetiracetam and carbamazepine by human and mouse P-glycoprotein. Neuropharmacology 2007;52(2):333-46
  • Niinuma K, Kato Y, Suzuki H, et al. Primary active transport of organic anions on bile canalicular membrane in humans. Am J Physiol 1999;276(5 Pt 1):G1153-64
  • Ninomiya M, Ito K, Hiramatsu R, et al. Functional analysis of mouse and monkey multidrug resistance-associated protein 2 (Mrp2). Drug Metab Dispos 2006;34(12):2056-63
  • Ninomiya M, Ito K, Horie T. Functional analysis of dog multidrug resistance-associated protein 2 (Mrp2) in comparison with rat Mrp2. Drug Metab Dispos 2005;33(2):225-32
  • Vander Borght S, Libbrecht L, Katoonizadeh A, et al. Breast cancer resistance protein (BCRP/ABCG2) is expressed by progenitor cells/reactive ductules and hepatocytes and its expression pattern is influenced by disease etiology and species type: possible functional consequences. J Histochem Cytochem 2006;54(9):1051-9
  • Sun D, Lennernas H, Welage LS, et al. Comparison of human duodenum and Caco-2 gene expression profiles for 12,000 gene sequences tags and correlation with permeability of 26 drugs. Pharm Res 2002;19(10):1400-16
  • Tanaka Y, Slitt AL, Leazer TM, et al. Tissue distribution and hormonal regulation of the breast cancer resistance protein (Bcrp/Abcg2) in rats and mice. Biochem Biophys Res Commun 2005;326(1):181-7
  • Figge A, Lammert F, Paigen B, et al. Hepatic overexpression of murine Abcb11 increases hepatobiliary lipid secretion and reduces hepatic steatosis. J Biol Chem 2004;279(4):2790-9
  • Bleasby K, Castle JC, Roberts CJ, et al. Expression profiles of 50 xenobiotic transporter genes in humans and pre-clinical species: a resource for investigations into drug disposition. Xenobiotica 2006;36(10-11):963-88
  • Hilgendorf C, Ahlin G, Seithel A, et al. Expression of thirty-six drug transporter genes in human intestine, liver, kidney, and organotypic cell lines. Drug Metab Dispos 2007;35(8):1333-40
  • Li N, Nemirovskiy OV, Zhang Y, et al. Absolute quantification of multidrug resistance-associated protein 2 (MRP2/ABCC2) using liquid chromatography tandem mass spectrometry. Anal Biochem 2008;380(2):211-22
  • Haimeur A, Conseil G, Deeley RG, et al. The MRP-related and BCRP/ABCG2 multidrug resistance proteins: biology, substrate specificity and regulation. Curr Drug Metab 2004;5(1):21-53
  • Belinsky MG, Dawson PA, Shchaveleva I, et al. Analysis of the in vivo functions of Mrp3. Mol Pharmacol 2005;68(1):160-8
  • Behrens I, Kamm W, Dantzig AH, et al. Variation of peptide transporter (PepT1 and HPT1) expression in Caco-2 cells as a function of cell origin. J Pharm Sci 2004;93(7):1743-54
  • Taipalensuu J, Tavelin S, Lazorova L, et al. Exploring the quantitative relationship between the level of MDR1 transcript, protein and function using digoxin as a marker of MDR1-dependent drug efflux activity. Eur J Pharm Sci 2004;21(1):69-75
  • Jones BR, Li W, Cao J, et al. The role of protein synthesis and degradation in the post-transcriptional regulation of rat multidrug resistance-associated protein 2 (Mrp2, Abcc2). Mol Pharmacol 2005;68(3):701-10
  • Zhang Y, Li W, Vore M. Translational regulation of rat multidrug resistance-associated protein 2 expression is mediated by upstream open reading frames in the 5′ untranslated region. Mol Pharmacol 2007;71(1):377-83
  • Elferink MG, Olinga P, Draaisma AL, et al. LPS-induced downregulation of MRP2 and BSEP in human liver is due to a posttranscriptional process. Am J Physiol Gastrointest Liver Physiol 2004;287(5):G1008-16
  • Pulaski L, Kania K, Ratajewski M, et al. Differential regulation of the human MRP2 and MRP3 gene expression by glucocorticoids. J Steroid Biochem Mol Biol 2005;96(3-4):229-34
  • Meyer ZU, Schwabedissen HE, Jedlitschky G, et al. Variable expression of MRP2 (ABCC2) in human placenta: influence of gestational age and cellular differentiation. Drug Metab Dispos 2005;33(7):896-904
  • Li N, Zhang Y, Hua F, et al. Absolute difference of hepatobiliary transporter multidrug resistance-associated protein (MRP2/Mrp2) in liver tissues and isolated hepatocytes from rat, dog, monkey, and human. Drug Metab Dispos 2009;37(1):66-73
  • Wu SL, Amato H, Biringer R, et al. Targeted proteomics of low-level proteins in human plasma by LC/MSn: using human growth hormone as a model system. J Proteome Res 2002;1(5):459-65
  • Kuhn E, Wu J, Karl J, et al. Quantification of C-reactive protein in the serum of patients with rheumatoid arthritis using multiple reaction monitoring mass spectrometry and 13C-labeled peptide standards. Proteomics 2004;4(4):1175-86
  • Barnidge DR, Goodmanson MK, Klee GG, et al. Absolute quantification of the model biomarker prostate-specific antigen in serum by LC-Ms/MS using protein cleavage and isotope dilution mass spectrometry. J Proteome Res 2004;3(3):644-52
  • Lu Y, Bottari P, Turecek F, et al. Absolute quantification of specific proteins in complex mixtures using visible isotope-coded affinity tags. Anal Chem 2004;76(14):4104-11
  • Nemirovskiy OV, Dufield DR, Sunyer T, et al. Discovery and development of a type II collagen neoepitope (TIINE) biomarker for matrix metalloproteinase activity: from in vitro to in vivo. Anal Biochem 2007;361(1):93-101
  • Gerber SA, Rush J, Stemman O, et al. Absolute quantification of proteins and phosphoproteins from cell lysates by tandem MS. Proc Natl Acad Sci USA 2003;100(12):6940-5
  • Barnidge DR, Dratz EA, Martin T, et al. Absolute quantification of the G protein-coupled receptor rhodopsin by LC/MS/MS using proteolysis product peptides and synthetic peptide standards. Anal Chem 2003;75(3):445-51
  • Kamiie J, Ohtsuki S, Iwase R, et al. Quantitative atlas of membrane transporter proteins: development and application of a highly sensitive simultaneous LC/MS/MS method combined with novel in-silico peptide selection criteria. Pharm Res 2008;25(6):1469-83
  • Li N, Bi Y-A, Duignan DB, et al. Quantitative expression profile of hepatobiliary transporters in sandwich cultured rat and human hepatocytes. Mol Pharm 2009. In revision
  • Li N, Palandra J, Nemirovskiy OV, et al. LC-MS/MS Mediated absolute quantification and comparison of bile salt export pump and breast cancer resistance protein in livers and hepatocytes across species. Anal Chem 2009;81(6):2251-9
  • Li N, Nemirovskiy OV, Zhang Y, et al. Absolute quantification of multidrug resistance-associate protein 2 (MRP2/ABCC2) using LC-MS/MS. Anal Biochem 2008;380(2):211-22
  • Bow DA, Perry JL, Miller DS, et al. Localization of P-gp (Abcb1) and Mrp2 (Abcc2) in freshly isolated rat hepatocytes. Drug Metab Dispos 2008;36(1):198-202
  • Takekuma Y, Kakiuchi H, Yamazaki K, et al. Difference between pharmacokinetics of mycophenolic acid (MPA) in rats and that in humans is caused by different affinities of MRP2 to a glucuronized form. J Pharm Pharm Sci 2007;10(1):71-85
  • Iwatsubo T, Suzuki H, Shimada N, et al. Prediction of in vivo hepatic metabolic clearance of YM796 from in vitro data by use of human liver microsomes and recombinant P-450 isozymes. J Pharmacol Exp Ther 1997;282(2):909-19
  • Obach RS, Baxter JG, Liston TE, et al. The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data. J Pharmacol Exp Ther 1997;283(1):46-58
  • Ghibellini G, Johnson BM, Kowalsky RJ, et al. A novel method for the determination of biliary clearance in humans. AAPS J 2004;6(4):e33
  • Ando T, Kusuhara H, Merino G, et al. Involvement of breast cancer resistance protein (ABCG2) in the biliary excretion mechanism of fluoroquinolones. Drug Metab Dispos 2007;35(10):1873-9
  • Fukuda H, Ohashi R, Tsuda-Tsukimoto M, et al. Effect of plasma protein binding on in vitro-in vivo correlation of biliary excretion of drugs evaluated by sandwich-cultured rat hepatocytes. Drug Metab Dispos 2008;36(7):1275-82
  • Ghibellini G, Vasist LS, Leslie EM, et al. In vitro-in vivo correlation of hepatobiliary drug clearance in humans. Clin Pharmacol Ther 2007;81(3):406-13
  • Watanabe T, Kusuhara H, Maeda K, et al. Physiologically based pharmacokinetic modeling to predict transporter-mediated clearance and distribution of pravastatin in humans. J Pharmacol Exp Ther 2009;328(2):652-62
  • Hengstler JG, Utesch D, Steinberg P, et al. Cryopreserved primary hepatocytes as a constantly available in vitro model for the evaluation of human and animal drug metabolism and enzyme induction. Drug Metab Rev 2000;32(1):81-118
  • Gomez-Lechon MJ, Donato MT, Castell JV, et al. Human hepatocytes as a tool for studying toxicity and drug metabolism. Curr Drug Metab 2003;4(4):292-312
  • Lam JL, Benet LZ. Hepatic microsome studies are insufficient to characterize in vivo hepatic metabolic clearance and metabolic drug-drug interactions: studies of digoxin metabolism in primary rat hepatocytes versus microsomes. Drug Metab Dispos 2004;32(11):1311-6
  • Oude Elferink RP, Ottenhoff R, Liefting WG, et al. ATP-dependent efflux of GSSG and GS-conjugate from isolated rat hepatocytes. Am J Physiol 1990;258(5 Pt 1):G699-706
  • Bi YA, Kazolias D, Duignan DB. Use of cryopreserved human hepatocytes in sandwich culture to measure hepatobiliary transport. Drug Metab Dispos 2006;34(9):1658-65
  • Liu X, Chism JP, LeCluyse EL, et al. Correlation of biliary excretion in sandwich-cultured rat hepatocytes and in vivo in rats. Drug Metab Dispos 1999;27(6):637-44
  • Obach RS. In vitro drug metabolism information in the prediction of human pharmacokinetics In: Bonate P, Howard D, editors, Pharmacokinetics in Drug Development: Clinical Study Design and Analysis. New York: Springer 2004. p. 445-78

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.