Integration of preclinical and clinical data with pharmacokinetic modeling and simulation to evaluate fexofenadine as a probe for hepatobiliary transport function

Pharmaceutical Research

Volumn 26, Issue 8, 2009, Pages 1942-1951

  Swift, Brandon ^a   Tian, Xianbin ^a,b   Brouwer, Kim L R ^a  

^a University of North Carolina   (United States)

^b Archemix Corporation   (United States)

Author keywords

Fexofenadine; Hepatic transport; Human pharmacokinetics; Rat perfused liver; Sandwich cultured hepatocytes

Indexed keywords

BOSENTAN; ELACRIDAR; FEXOFENADINE; TAUROCHOLIC ACID;

ANIMAL EXPERIMENT; ARTICLE; BILIARY EXCRETION; CLINICAL EVALUATION; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG EXCRETION; DRUG TRANSPORT; EXPOSURE; HEPATOBILIARY SYSTEM; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; HUMAN TISSUE; IN SITU HYBRIDIZATION; IN VITRO STUDY; LIVER CELL; LIVER PERFUSION; MALE; MOLECULAR PROBE; NONHUMAN; PRIORITY JOURNAL; RAT; SIMULATION;

ANIMALS; BILIARY TRACT; CELLS, CULTURED; HISTAMINE H1 ANTAGONISTS, NON-SEDATING; HUMANS; LIVER; MODELS, BIOLOGICAL; MOLECULAR PROBES; RATS; RATS, WISTAR; TERFENADINE;

EID: 67650034981     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-009-9909-z     Document Type: Article

References (45)

1. N Petri C Tannergren D Rungstad H Lennernas 2004 Transport characteristics of fexofenadine in the Caco-2 cell model Pharm Res 21 1398 404 10.1023/B:PHAM.0000036913.90332.b1
2. C Tannergren T Knutson L Knutson H Lennernas 2003 The effect of ketoconazole on the in vivo intestinal permeability of fexofenadine using a regional perfusion technique Br J Clin Pharmacol 55 182 90 10.1046/j.1365-2125. 2003.01722.x
3. C Tannergren N Petri L Knutson M Hedeland U Bondesson H Lennernas 2003 Multiple transport mechanisms involved in the intestinal absorption and first-pass extraction of fexofenadine Clin Pharmacol Ther 74 423 36 10.1016/S0009-9236(03) 00238-8
4. C Lippert J Ling P Brown S Burmaster M Eller L Cheng R Thompson S Weir 1995 Mass balance and pharmacokinetics of MDL 16,455A in healthy, male volunteers Pharmaceutical Research 12 S-390
5. H Tahara H Kusuhara E Fuse Y Sugiyama 2005 P-glycoprotein plays a major role in the efflux of fexofenadine in the small intestine and blood-brain barrier, but only a limited role in its biliary excretion Drug Metab Dispos 33 963 8 10.1124/dmd.105.004192
6. MA Hamman MA Bruce BD Haehner-Daniels SD Hall 2001 The effect of rifampin administration on the disposition of fexofenadine Clin Pharmacol Ther 69 114 21 10.1067/mcp. 2001.113697
7. C Banfield S Gupta M Marino J Lim M Affrime 2002 Grapefruit juice reduces the oral bioavailability of fexofenadine but not desloratadine Clin Pharmacokinet 41 311 8 10.2165/00003088-200241040-00004
8. H Glaeser DG Bailey GK Dresser JC Gregor UI Schwarz JS McGrath E Jolicoeur W Lee BF Leake RG Tirona RB Kim 2007 Intestinal drug transporter expression and the impact of grapefruit juice in humans Clin Pharmacol Ther 81 362 70 10.1038/sj.clpt.6100056
9. M Shimizu T Uno K Sugawara T Tateishi 2006 Effects of itraconazole and diltiazem on the pharmacokinetics of fexofenadine, a substrate of P-glycoprotein Br J Clin Pharmacol 61 538 44 10.1111/j.1365-2125.2006.02613.x
10. M Cvetkovic B Leake MF Fromm GR Wilkinson RB Kim 1999 OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine Drug Metab Dispos 27 866 71
11. Matsushima S, Maeda K, Ishiguro N, Igarashi T, and Sugiyama Y. Investigation of the inhibitory effects of various drugs on the hepatic uptake of fexofenadine in humans. Drug Metab Dispos (2008).
12. M Shimizu K Fuse K Okudaira R Nishigaki K Maeda H Kusuhara Y Sugiyama 2005 Contribution of OATP (organic anion-transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans Drug Metab Dispos 33 1477 81 10.1124/dmd.105.004622
13. GT Tucker JB Houston SM Huang 2001 Optimizing drug development: strategies to assess drug metabolism/transporter interaction potential-towards a consensus Br J Clin Pharmacol 52 107 17 10.1046/j.0306-5251.2001.temp. 1441.x
14. JH Shon YR Yoon WS Hong PM Nguyen SS Lee YG Choi IJ Cha JG Shin 2005 Effect of itraconazole on the pharmacokinetics and pharmacodynamics of fexofenadine in relation to the MDR1 genetic polymorphism Clin Pharmacol Ther 78 191 201 10.1016/j.clpt.2005.04.012
15. S Zhou E Chan SQ Pan M Huang EJ Lee 2004 Pharmacokinetic interactions of drugs with St John's wort J Psychopharmacol 18 262 76 10.1177/0269881104042632
16. GL Lemma Z Wang MA Hamman NA Zaheer JC Gorski SD Hall 2006 The effect of short- and long-term administration of verapamil on the disposition of cytochrome P450 3A and P-glycoprotein substrates Clin Pharmacol Ther 79 218 30 10.1016/j.clpt.2005.11.001
17. N Yasui-Furukori T Uno K Sugawara T Tateishi 2005 Different effects of three transporting inhibitors, verapamil, cimetidine, and probenecid, on fexofenadine pharmacokinetics Clin Pharmacol Ther 77 17 23 10.1016/j.clpt.2004. 08.026
18. X Tian MJ Zamek-Gliszczynski J Li AS Bridges K Nezasa NJ Patel TJ Raub KL Brouwer 2008 Multidrug resistance-associated protein 2 is primarily responsible for the biliary excretion of fexofenadine in mice Drug Metab Dispos 36 61 4 10.1124/dmd.107.017319
19. Matsushima S, Maeda K, Hayashi H, Debori Y, Schinkel AH, Schuetz JD, Kusuhara H, and Sugiyama Y. Involvement of multiple efflux transporters in hepatic disposition of fexofenadine. Mol Pharmacol (2008).
20. JA Byrne SS Strautnieks G Mieli-Vergani CF Higgins KJ Linton RJ Thompson 2002 The human bile salt export pump: characterization of substrate specificity and identification of inhibitors Gastroenterology 123 1649 58 10.1053/gast.2002.36591
21. M Hirano K Maeda H Hayashi H Kusuhara Y Sugiyama 2005 Bile salt export pump (BSEP/ABCB11) can transport a nonbile acid substrate, pravastatin J Pharmacol Exp Ther 314 876 82 10.1124/jpet.105.084830
22. V Lecureur D Sun P Hargrove EG Schuetz RB Kim LB Lan JD Schuetz 2000 Cloning and expression of murine sister of P-glycoprotein reveals a more discriminating transporter than MDR1/P-glycoprotein Mol Pharmacol 57 24 35 (Pubitemid 30033256)
23. U Hoffmannand HK Kroemer 2004 The ABC transporters MDR1 and MRP2: multiple functions in disposition of xenobiotics and drug resistance Drug Metab Rev 36 669 701 10.1081/DMR-200033473
24. S Kawabata M Oka K Shiozawa K Tsukamoto K Nakatomi H Soda M Fukuda Y Ikegami K Sugahara Y Yamada S Kamihira LA Doyle DD Ross S Kohno 2001 Breast cancer resistance protein directly confers SN-38 resistance of lung cancer cells Biochem Biophys Res Commun 280 1216 23 10.1006/bbrc.2001.4267
25. M Suzuki H Suzuki Y Sugimoto Y Sugiyama 2003 ABCG2 transports sulfated conjugates of steroids and xenobiotics J Biol Chem 278 22644 9 10.1074/jbc.M212399200
26. G Merino JW Jonker E Wagenaar AE van Herwaarden AH Schinkel 2005 The breast cancer resistance protein (BCRP/ABCG2) affects pharmacokinetics, hepatobiliary excretion, and milk secretion of the antibiotic nitrofurantoin Mol Pharmacol 67 1758 64 10.1124/mol.104.010439
27. K Fattinger C Funk M Pantze C Weber J Reichen B Stieger PJ Meier 2001 The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: a potential mechanism for hepatic adverse reactions Clin Pharmacol Ther 69 223 31 10.1067/mcp. 2001.114667
28. ZC Gatmaitan AT Nies IM Arias 1997 Regulation and translocation of ATP-dependent apical membrane proteins in rat liver Am J Physiol 272 G1041 9
29. H Kipp N Pichetshote IM Arias 2001 Transporters on demand: intrahepatic pools of canalicular ATP binding cassette transporters in rat liver J Biol Chem 276 7218 24 10.1074/jbc.M007794200
30. GK Dresser DG Bailey BF Leake UI Schwarz PA Dawson DJ Freeman RB Kim 2002 Fruit juices inhibit organic anion transporting polypeptide-mediated drug uptake to decrease the oral availability of fexofenadine Clin Pharmacol Ther 71 11 20 10.1067/mcp. 2002.121152 (Pubitemid 34124034)
31. EL LeCluyse PL Bullock A Parkinson JH Hochman 1996 Cultured rat hepatocytes. Pharm Biotechnol 8 121 59
32. X Liu EL LeCluyse KR Brouwer LS Gan JJ Lemasters B Stieger PJ Meier KL Brouwer 1999 Biliary excretion in primary rat hepatocytes cultured in a collagen-sandwich configuration Am J Physiol 277 G12 21
33. P Chandra BM Johnson P Zhang GM Pollack KL Brouwer 2005 Modulation of hepatic canalicular or basolateral transport proteins alters hepatobiliary disposition of a model organic anion in the isolated perfused rat liver Drug Metab Dispos 33 1238 43 10.1124/dmd.105.003665
34. ZE Wilson A Rostami-Hodjegan JL Burn A Tooley J Boyle SW Ellis GT Tucker 2003 Inter-individual variability in levels of human microsomal protein and hepatocellularity per gram of liver Br J Clin Pharmacol 56 433 40 10.1046/j.1365-2125.2003.01881.x
35. B Daviesand T Morris 1993 Physiological parameters in laboratory animals and humans Pharm Res 10 1093 5 10.1023/A:1018943613122
36. S Drescher E Schaeffeler M Hitzl U Hofmann M Schwab U Brinkmann M Eichelbaum MF Fromm 2002 MDR1 gene polymorphisms and disposition of the P-glycoprotein substrate fexofenadine Br J Clin Pharmacol 53 526 34 10.1046/j.1365-2125.2002.01591.x
37. RB Kim BF Leake EF Choo GK Dresser SV Kubba UI Schwarz A Taylor HG Xie J McKinsey S Zhou LB Lan JD Schuetz EG Schuetz GR Wilkinson 2001 Identification of functionally variant MDR1 alleles among European Americans and African Americans Clin Pharmacol Ther 70 189 99 10.1067/mcp. 2001.117412
38. M Niemi KT Kivisto U Hofmann M Schwab M Eichelbaum MF Fromm 2005 Fexofenadine pharmacokinetics are associated with a polymorphism of the SLCO1B1 gene (encoding OATP1B1) Br J Clin Pharmacol 59 602 4 10.1111/j.1365-2125.2005. 02354.x
39. PP Annaert RZ Turncliff CL Booth DR Thakker KL Brouwer 2001 P-glycoprotein-mediated in vitro biliary excretion in sandwich-cultured rat hepatocytes Drug Metab Dispos 29 1277 83
40. YA Bi D Kazolias DB Duignan 2006 Use of cryopreserved human hepatocytes in sandwich culture to measure hepatobiliary transport Drug Metab Dispos 34 1658 65 10.1124/dmd.105.009118
41. X Tian B Swift MJ Zamek-Gliszczynski MG Belinsky GD Kruh KL Brouwer 2008 Impact of basolateral multidrug resistance-associated protein (Mrp) 3 and Mrp4 on the hepatobiliary disposition of fexofenadine in perfused mouse livers Drug Metab Dispos 36 911 5 10.1124/dmd.107.019273
42. H Xiong KC Turner ES Ward PL Jansen KL Brouwer 2000 Altered hepatobiliary disposition of acetaminophen glucuronide in isolated perfused livers from multidrug resistance-associated protein 2-deficient TR(-) rats J Pharmacol Exp Ther 295 512 8
43. RW Milne LA Larsen KL Jorgensen J Bastlund GR Stretch AM Evans 2000 Hepatic disposition of fexofenadine: influence of the transport inhibitors erythromycin and dibromosulphothalein Pharm Res 17 1511 5 10.1023/A: 1007609225851
44. A Treiber R Schneiter S Delahaye M Clozel 2004 Inhibition of organic anion transporting polypeptide-mediated hepatic uptake is the major determinant in the pharmacokinetic interaction between bosentan and cyclosporin A in the rat J Pharmacol Exp Ther 308 1121 9 10.1124/jpet.103.061614
45. A Treiber R Schneiter S Hausler B Stieger 2007 Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil Drug Metab Dispos 35 1400 7 10.1124/dmd.106.013615