Role of P-glycoprotein in the uptake/efflux transport of oral vitamin K antagonists and rivaroxaban through the caco-2 cell model

Basic and Clinical Pharmacology and Toxicology

Volumn 113, Issue 4, 2013, Pages 259-265

  Gschwind, Liliane ^a,b   Rollason, Victoria ^a   Daali, Youssef ^a   Bonnabry, Pascal ^a,b   Dayer, Pierre ^a   Desmeules, Jules Alexandre ^a  

^a GENEVA UNIVERSITY HOSPITALS   (Switzerland)

^b UNIVERSITY OF GENEVA   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

ACENOCOUMAROL; ANTIVITAMIN K; CYCLOSPORIN A; DIGOXIN; FEXOFENADINE; MULTIDRUG RESISTANCE PROTEIN; PHENPROCOUMON; RHODAMINE 123; RIVAROXABAN; VALSPODAR; WARFARIN;

ARTICLE; CELL STRAIN CACO 2; CONTROLLED STUDY; DRUG UPTAKE; EFFUSION; HUMAN; HUMAN CELL; IN VITRO STUDY; LIQUID CHROMATOGRAPHY; MASS SPECTROMETRY; PH; PRIORITY JOURNAL;

ACENOCOUMAROL; ANTICOAGULANTS; BIOLOGICAL TRANSPORT; CACO-2 CELLS; HUMANS; MICROSCOPY, ELECTRON, TRANSMISSION; MORPHOLINES; P-GLYCOPROTEIN; THIOPHENES; VITAMIN K; WARFARIN;

EID: 84883788040     PISSN: 17427835     EISSN: 17427843     Source Type: Journal    
DOI: 10.1111/bcpt.12084     Document Type: Article

References (35)

1. Hirsh J, Dalen JE, Anderson DR, Poller L, Bussey H, Ansell J et al. Oral anticoagulants: mechanism of action, clinical effectiveness, and optimal therapeutic range. Chest 1998;114:445S-69S.
2. Ufer M. Comparative pharmacokinetics of vitamin K antagonists: warfarin, phenprocoumon and acenocoumarol. Clin Pharmacokinet 2005;44:1227-46.
3. Thijssen HH, Flinois JP, Beaune PH. Cytochrome P4502C9 is the principal catalyst of racemic acenocoumarol hydroxylation reactions in human liver microsomes. Drug Metab Dispos 2000;28:1284-90.
4. Ansell J, Hirsh J, Hylek E, Jacobson A, Crowther M, Palareti G. Pharmacology and management of the vitamin K antagonists: American College of Chest Physicians Evidence-Based Clinical Practice Guidelines (8th Edition). Chest 2008;133:160S-98S.
5. Aithal GP, Day CP, Kesteven PJ, Daly AK. Association of polymorphisms in the cytochrome P450 CYP2C9 with warfarin dose requirement and risk of bleeding complications. Lancet 1999;353:717-9.
6. Stehle S, Kirchheiner J, Lazar A, Fuhr U. Pharmacogenetics of oral anticoagulants: a basis for dose individualization. Clin Pharmacokinet 2008;47:565-94.
7. Beinema M, Brouwers JR, Schalekamp T, Wilffert B. Pharmacogenetic differences between warfarin, acenocoumarol and phenprocoumon. Thromb Haemost 2008;100:1052-7.
8. Van Schie RM, Wessels JA, Le Cessie S, De Boer A, Schalekamp T, Van Der Meer FJ et al. Loading and maintenance dose algorithms for phenprocoumon and acenocoumarol using patient characteristics and pharmacogenetic data. Eur Heart J 2011;32:1909-17.
9. Visser LE, Van Schaik RH, Van Vliet M, Trienekens PH, De Smet PA, Vulto AG et al. The risk of bleeding complications in patients with cytochrome P450 CYP2C9*2 or CYP2C9*3 alleles on acenocoumarol or phenprocoumon. Thromb Haemost 2004;92:61-6.
10. Schalekamp T, Brasse BP, Roijers JF, Chahid Y, Van Geest-Daalderop JH, De Vries-Goldschmeding H et al. VKORC1 and CYP2C9 genotypes and acenocoumarol anticoagulation status: interaction between both genotypes affects overanticoagulation. Clin Pharmacol Ther 2006;80:13-22.
11. Schalekamp T, Brasse BP, Roijers JF, Van Meegen E, Van Der Meer FJ, Van Wijk EM et al. VKORC1 and CYP2C9 genotypes and phenprocoumon anticoagulation status: interaction between both genotypes affects dose requirement. Clin Pharmacol Ther 2007;81:185-93.
12. Dubuske LM. The role of P-glycoprotein and organic anion-transporting polypeptides in drug interactions. Drug Saf 2005;28:789-801.
13. Sissung TM, Baum CE, Kirkland CT, Gao R, Gardner ER, Figg WD. Pharmacogenetics of membrane transporters: an update on current approaches. Mol Biotechnol 2010;44:152-67.
14. Wacher VJ, Silverman JA, Zhang Y, Benet LZ. Role of P-glycoprotein and cytochrome P450 3A in limiting oral absorption of peptides and peptidomimetics. J Pharm Sci 1998;87:1322-30.
15. Wacher VJ, Wu CY, Benet LZ. Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and P-glycoprotein: implications for drug delivery and activity in cancer chemotherapy. Mol Carcinog 1995;13:129-34.
16. Sussman NL, Waltershied M, Butler T, Cali JJ, Riss T, Kelly HJ. The predictive nature of high-throughput Toxicity Screening Using a Human Hepatocyte Cell Line. Cell Notes 2002;3:7-10.
17. Wadelius M, Sorlin K, Wallerman O, Karlsson J, Yue QY, Magnusson PK et al. Warfarin sensitivity related to CYP2C9, CYP3A5, ABCB1 (MDR1) and other factors. Pharmacogenomics J 2004;4:40-8.
18. Wadelius M, Pirmohamed M. Pharmacogenetics of warfarin: current status and future challenges. Pharmacogenomics J 2007;7:99-111.
19. Saraeva RB, Paskaleva ID, Doncheva E, Eap CB, Ganev VS. Pharmacogenetics of acenocoumarol: CYP2C9, CYP2C19, CYP1A2, CYP3A4, CYP3A5 and ABCB1 gene polymorphisms and dose requirements. J Clin Pharm Ther 2007;32:641-9.
20. Gres MC, Julian B, Bourrie M, Meunier V, Roques C, Berger M et al. Correlation between oral drug absorption in humans, and apparent drug permeability in TC-7 cells, a human epithelial intestinal cell line: comparison with the parental Caco-2 cell line. Pharm Res 1998;15:726-33.
21. Hidalgo IJ, Raub TJ, Borchardt RT. Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology 1989;96:736-49.
22. Gnoth MJ, Buetehorn U, Muenster U, Schwarz T, Sandmann S. In vitro and in vivo P-glycoprotein transport characteristics of rivaroxaban. J Pharmacol Exp Ther 2011;338:372-80.
23. Siflinger-Birnboim A, Del Vecchio PJ, Cooper JA, Blumenstock FA, Shepard JM, Malik AB. Molecular sieving characteristics of the cultured endothelial monolayer. J Cell Physiol 1987;132:111-7.
24. Kanaan M, Daali Y, Dayer P, Desmeules J. Lack of interaction of the NMDA receptor antagonists dextromethorphan and dextrorphan with P-glycoprotein. Curr Drug Metab 2008;9:144-51.
25. Amidon GL, Lennernas H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995;12:413-20.
26. Karlsson J, Kuo SM, Ziemniak J, Artursson P. Transport of celiprolol across human intestinal epithelial (Caco-2) cells: mediation of secretion by multiple transporters including P-glycoprotein. Br J Pharmacol 1993;110:1009-16.
27. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO et al. Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther 2001;299:620-8.
28. FDA Guidance for Industry. Drug interaction studies. Study design, Data analysis, implications for dosing, and labeling recommendations http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/UCM292362.pdf, (last accessed on 12 February 2012).
29. Sun H, Chow EC, Liu S, Du Y, Pang KS. The Caco-2 cell monolayer: usefulness and limitations. Expert Opin Drug Metab Toxico 2008;4:395-411.
30. Press B, Di Grandi D. Permeability for intestinal absorption: Caco-2 assay and related issues. Curr Drug Metab 2008;9:893-900.
31. Seelig A. How does P-glycoprotein recognize its substrates? Int J Clin Pharmacol Ther 1998;36:50-4.
32. Seelig A, Landwojtowicz E. Structure-activity relationship of P-glycoprotein substrates and modifiers. Eur J Pharm Sci 2000;12:31-40.
33. Wang RB, Kuo CL, Lien LL, Lien EJ. Structure-activity relationship: analyses of p-glycoprotein substrates and inhibitors. J Clin Pharm Ther 2003;28:203-28.
34. PubChem. http://pubchem.ncbi.nlm.nih.gov/. (last accessed on 10 September 2012).
35. European Medicines Agency Evaluation of Medicines for Human Use (EMEA). CHMP Assessment report for Xarelto. http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Public_assessment_report/human/000944/WC500057122.pdf. (last accessed on 10 September 2012).