Clinical relevance of drug efflux pumps in the gut

Current Opinion in Pharmacology

Volumn 13, Issue 6, 2013, Pages 847-852

  Misaka, Shingen ^a   Müller, Fabian ^a   Fromm, Martin F ^a  

^a UNIVERSITY OF ERLANGEN NUREMBERG   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

BREAST CANCER RESISTANCE PROTEIN; DABIGATRAN ETEXILATE; DIGOXIN; HYPERICUM PERFORATUM EXTRACT; MULTIDRUG RESISTANCE PROTEIN; MULTIDRUG RESISTANCE PROTEIN 2; RIFAMPICIN; SALAZOSULFAPYRIDINE; TALINOLOL; TOPOTECAN; VERAPAMIL;

AREA UNDER THE CURVE; ARTICLE; DOSE RESPONSE; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG DISPOSITION; DRUG ELIMINATION; DRUG METABOLISM; DRUG POTENTIATION; DRUG TRANSPORT; HUMAN; INTESTINE ABSORPTION; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; SINGLE DRUG DOSE; SINGLE NUCLEOTIDE POLYMORPHISM;

ANIMALS; GASTROINTESTINAL TRACT; HUMANS; INTESTINAL ABSORPTION; MEMBRANE TRANSPORT PROTEINS; PHARMACEUTICAL PREPARATIONS;

EID: 84888203130     PISSN: 14714892     EISSN: 14714973     Source Type: Journal    
DOI: 10.1016/j.coph.2013.08.010     Document Type: Review

References (55)

1. A. Hosomi, T. Nakanishi, T. Fujita, and I. Tamai Extra-renal elimination of uric acid via intestinal efflux transporter BCRP/ABCG2 PLoS ONE 7 2012 e30456 10.1371/journal.pone.0030456
2. K.M. Giacomini, S.M. Huang, D.J. Tweedie, L.Z. Benet, K.L. Brouwer, X. Chu, A. Dahlin, R. Evers, V. Fischer, and K.M. Hillgren International Transporter Consortium: membrane transporters in drug development Nat Rev Drug Discov 9 2010 215 236
3. O. Zolk, and M.F. Fromm Transporter-mediated drug uptake and efflux: important determinants of adverse drug reactions Clin Pharmacol Ther 89 2011 798 805
4. J. König, F. Müller, and M.F. Fromm Transporters and drug-drug interactions: important determinants of drug disposition and effects Pharmacol Rev 65 2013 944 966
5. T.G. Tucker, A.M. Milne, S. Fournel-Gigleux, K.S. Fenner, and M.W. Coughtrie Absolute immunoquantification of the expression of ABC transporters P-glycoprotein, breast cancer resistance protein and multidrug resistance-associated protein 2 in human liver and duodenum Biochem Pharmacol 83 2012 279 285
6. I. Ieiri Functional significance of genetic polymorphisms in P-glycoprotein (MDR1, ABCB1) and breast cancer resistance protein (BCRP, ABCG2) Drug Metab Pharmacokinet 27 2012 85 105
7. S. Haenisch, K. May, D. Wegner, A. Caliebe, I. Cascorbi, and W. Siegmund Influence of genetic polymorphisms on intestinal expression and rifampicin-type induction of ABCC2 and on bioavailability of talinolol Pharmacogenet Genomics 18 2008 357 365 (Pubitemid 351367529)
8. U. Gradhand, and R.B. Kim Pharmacogenomics of MRP transporters (ABCC1-5) and BCRP (ABCG2) Drug Metab Rev 40 2008 317 354 (Pubitemid 352000949)
9. S.C. Tang, J.J.M.A. Hendrikx, J.H. Beijnen, and A.H. Schinkel Genetically modified mouse models for oral drug absorption and disposition Curr Opin Pharmacol 13 2013 853 858
10. I. Cascorbi P-glycoprotein: tissue distribution, substrates, and functional consequences of genetic variations Handb Exp Pharmacol 201 2011 261 283
11. L.M. Hodges, S.M. Markova, L.W. Chinn, J.M. Gow, D.L. Kroetz, T.E. Klein, and R.B. Altman Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein) Pharmacogenet Genomics 21 2011 152 161
12. S. Mouly, and M.F. Paine P-glycoprotein increases from proximal to distal regions of human small intestine Pharm Res 20 2003 1595 1599 (Pubitemid 37268274)
13. A. Bruyère, X. Declèves, F. Bouzom, K. Ball, C. Marques, X. Treton, M. Pocard, P. Valleur, Y. Bouhnik, and Y. Panis Effect of variations in the amounts of P-glycoprotein (ABCB1), BCRP (ABCG2) and CYP3A4 along the human small intestine on PBPK models for predicting intestinal first pass Mol Pharm 7 2010 1596 1607
14. M. Estudante, J.G. Morais, G. Soveral, and L.Z. Benet Intestinal drug transporters: an overview Adv Drug Deliv Rev 2013 (epub)
15. M.V. Varma, C.M. Ambler, M. Ullah, C.J. Rotter, H. Sun, J. Litchfield, K.S. Fenner, and A.F. El-Kattan Targeting intestinal transporters for optimizing oral drug absorption Curr Drug Metab 11 2010 730 742
16. R.A. van Waterschoot, and A.H. Schinkel A critical analysis of the interplay between cytochrome P450 3A and P-glycoprotein: recent insights from knockout and transgenic mice Pharmacol Rev 63 2011 390 410
17. R.G. Tirona Molecular mechanisms of drug transporter regulation Handb Exp Pharmacol 201 2011 373 402
18. O. Burk, S.S. Brenner, U. Hofmann, H. Tegude, S. Igel, M. Schwab, M. Eichelbaum, and M.D. Alscher The impact of thyroid disease on the regulation, expression, and function of ABCB1 (MDR1/P glycoprotein) and consequences for the disposition of digoxin Clin Pharmacol Ther 88 2010 685 694
19. A.H. Schinkel, J.J. Smit, O. van Tellingen, J.H. Beijnen, E. Wagenaar, L. van Deemter, C.A. Mol, M.A. van der Valk, E.C. Robanus-Maandag, and H.P. te Riele Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs Cell 77 1994 491 502 (Pubitemid 24153990)
20. B. Greiner, M. Eichelbaum, P. Fritz, H.P. Kreichgauer, O. von Richter, J. Zundler, and H.K. Kroemer The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin J Clin Invest 104 1999 147 153
21. H. Glaeser Importance of P-glycoprotein for drug-drug interactions Handb Exp Pharmacol 201 2011 285 297
22. K.S. Fenner, M.D. Troutman, S. Kempshall, J.A. Cook, J.A. Ware, D.A. Smith, and C.A. Lee Drug-drug interactions mediated through P-glycoprotein: clinical relevance and in vitro-in vivo correlation using digoxin as a probe drug Clin Pharmacol Ther 85 2009 173 181
23. S. Igel, S. Drescher, T. Mürdter, U. Hofmann, G. Heinkele, H. Tegude, H. Glaeser, S.S. Brenner, A.A. Somogyi, and T. Omari Increased absorption of digoxin from the human jejunum due to inhibition of intestinal transporter-mediated efflux Clin Pharmacokinet 46 2007 777 785 (Pubitemid 47347449)
24. W. Siegmund, S. Altmannsberger, A. Paneitz, U. Hecker, M. Zschiesche, G. Franke, W. Meng, R. Warzok, E. Schroeder, and B. Sperker Effect of levothyroxine administration on intestinal P-glycoprotein expression: consequences for drug disposition Clin Pharmacol Ther 72 2002 256 264
25. K. Westphal, A. Weinbrenner, M. Zschiesche, G. Franke, M. Knoke, R. Oertel, P. Fritz, O. von Richter, R. Warzok, and T. Hachenberg Induction of P-glycoprotein by rifampin increases intestinal secretion of talinolol in human beings: a new type of drug/drug interaction Clin Pharmacol Ther 68 2000 345 355
26. A. Johne, J. Brockmöller, S. Bauer, A. Maurer, M. Langheinrich, and I. Roots Pharmacokinetic interaction of digoxin with an herbal extract from St John's wort (Hypericum perforatum) Clin Pharmacol Ther 66 1999 338 345 (Pubitemid 29494126)
27. U.I. Schwarz, H. Hanso, R. Oertel, S. Miehlke, E. Kuhlisch, H. Glaeser, M. Hitzl, G.K. Dresser, R.B. Kim, and W. Kirch Induction of intestinal P-glycoprotein by St John's wort reduces the oral bioavailability of talinolol Clin Pharmacol Ther 81 2007 669 678 (Pubitemid 46625125)
28. S. Drescher, H. Glaeser, T. Mürdter, M. Hitzl, M. Eichelbaum, and M.F. Fromm P-glycoprotein-mediated intestinal and biliary digoxin transport in humans Clin Pharmacol Ther 73 2003 223 231 (Pubitemid 36269673)
29. S. Hoffmeyer, O. Burk, O. von Richter, H.P. Arnold, J. Brockmöller, A. Johne, I. Cascorbi, T. Gerloff, I. Roots, and M. Eichelbaum Functional polymorphisms of the human multidrug-resistance gene: multiple sequence variations and correlation of one allele with P-glycoprotein expression and activity in vivo Proc Natl Acad Sci U S A 97 2000 3473 3478 (Pubitemid 30183327)
30. J.G. Shi, Y. Zhang, and S. Yeleswaram The relevance of assessment of intestinal P-gp inhibition using digoxin as an in vivo probe substrate Nat Rev Drug Discov 10 2011 75
31. European Medicines Agency Guideline on the Investigation of Drug Interactions 2012 http://www.ema.europa.eu/ema/pages/includes/document/open- document.jsp?webContentId=WC500129606
32. ®) after co-medication with verapamil in healthy subjects Br J Clin Pharmacol 75 2013 1053 1062
33. S. Blech, T. Ebner, E. Ludwig-Schwellinger, J. Stangier, and W. Roth The metabolism and disposition of the oral direct thrombin inhibitor, dabigatran, in humans Drug Metab Dispos 36 2008 386 399 (Pubitemid 351185753)
34. M. Ufer Comparative efficacy and safety of the novel oral anticoagulants dabigatran, rivaroxaban and apixaban in preclinical and clinical development Thromb Haemost 103 2010 572 585
35. S. Härtter, M. Koenen-Bergmann, A. Sharma, G. Nehmiz, U. Lemke, W. Timmer, and P.A. Reilly Decrease in the oral bioavailability of dabigatran etexilate after co-medication with rifampicin Br J Clin Pharmacol 74 2012 490 500
36. R. Schnepf, and O. Zolk Effect of the ATP-binding cassette transporter ABCG2 on pharmacokinetics: experimental findings and clinical implications Expert Opin Drug Metab Toxicol 9 2013 287 306
37. Z. Ni, Z. Bikadi, M.F. Rosenberg, and Q. Mao Structure and function of the human breast cancer resistance protein (BCRP/ABCG2) Curr Drug Metab 11 2010 603 617
38. K. Noguchi, K. Katayama, J. Mitsuhashi, and Y. Sugimoto Functions of the breast cancer resistance protein (BCRP/ABCG2) in chemotherapy Adv Drug Deliv Rev 61 2009 26 33
39. J.W. Jonker, M. Buitelaar, E. Wagenaar, M.A. Van Der Valk, G.L. Scheffer, R.J. Scheper, T. Plosch, F. Kuipers, R.P. Elferink, and H. Rosing The breast cancer resistance protein protects against a major chlorophyll-derived dietary phototoxin and protoporphyria Proc Natl Acad Sci U S A 99 2002 15649 15654 (Pubitemid 35403986)
40. C.M. Kruijtzer, J.H. Beijnen, H. Rosing, W.W. ten Bokkel Huinink, M. Schot, R.C. Jewell, E.M. Paul, and J.H. Schellens Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918 J Clin Oncol 20 2002 2943 2950 (Pubitemid 34728888)
41. H. Zaher, A.A. Khan, J. Palandra, T.G. Brayman, L. Yu, and J.A. Ware Breast cancer resistance protein (Bcrp/abcg2) is a major determinant of sulfasalazine absorption and elimination in the mouse Mol Pharm 3 2006 55 61 (Pubitemid 43331751)
42. H. Kusuhara, H. Furuie, A. Inano, A. Sunagawa, S. Yamada, C. Wu, S. Fukizawa, N. Morimoto, I. Ieiri, and M. Morishita Pharmacokinetic interaction study of sulphasalazine in healthy subjects and the impact of curcumin as an in vivo inhibitor of BCRP Br J Pharmacol 166 2012 1793 1803
43. R.N. Peroni, S.S. Di Gennaro, C. Hocht, D.A. Chiappetta, M.C. Rubio, A. Sosnik, and G.F. Bramuglia Efavirenz is a substrate and in turn modulates the expression of the efflux transporter ABCG2/BCRP in the gastrointestinal tract of the rat Biochem Pharmacol 82 2011 1227 1233
44. B.L. Urquhart, J.A. Ware, R.G. Tirona, R.H. Ho, B.F. Leake, U.I. Schwarz, H. Zaher, J. Palandra, J.C. Gregor, and G.K. Dresser Breast cancer resistance protein (ABCG2) and drug disposition: intestinal expression, polymorphisms and sulfasalazine as an in vivo probe Pharmacogenet Genomics 18 2008 439 448 (Pubitemid 351535945)
45. P.J. Neuvonen Drug interactions with HMG-CoA reductase inhibitors (statins): the importance of CYP enzymes, transporters and pharmacogenetics Curr Opin Investig Drugs 11 2010 323 332
46. O.M. Woodward, A. Kottgen, J. Coresh, E. Boerwinkle, W.B. Guggino, and M. Kottgen Identification of a urate transporter, ABCG2, with a common functional polymorphism causing gout Proc Natl Acad Sci U S A 106 2009 10338 10342
47. A.T. Nies, and D. Keppler The apical conjugate efflux pump ABCC2 (MRP2) Pflügers Arch 453 2007 643 659 (Pubitemid 46192536)
48. H.R. Kast, B. Goodwin, P.T. Tarr, S.A. Jones, A.M. Anisfeld, C.M. Stoltz, P. Tontonoz, S. Kliewer, T.M. Willson, and P.A. Edwards Regulation of multidrug resistance-associated protein 2 (ABCC2) by the nuclear receptors pregnane X receptor, farnesoid X-activated receptor, and constitutive androstane receptor J Biol Chem 277 2002 2908 2915 (Pubitemid 34953324)
49. M.F. Fromm, H.M. Kauffmann, P. Fritz, O. Burk, H.K. Kroemer, R.W. Warzok, M. Eichelbaum, W. Siegmund, and D. Schrenk The effect of rifampin treatment on intestinal expression of human MRP transporters Am J Pathol 157 2000 1575 1580
50. T. Giessmann, K. May, C. Modess, D. Wegner, U. Hecker, M. Zschiesche, P. Dazert, M. Grube, E. Schroeder, and R. Warzok Carbamazepine regulates intestinal P-glycoprotein and multidrug resistance protein MRP2 and influences disposition of talinolol in humans Clin Pharmacol Ther 76 2004 192 200 (Pubitemid 39221793)
51. C.G. Dietrich, D.R. de Waart, R. Ottenhoff, A.H. Bootsma, A.H. van Gennip, and R.P. Elferink Mrp2-deficiency in the rat impairs biliary and intestinal excretion and influences metabolism and disposition of the food-derived carcinogen 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) Carcinogenesis 22 2001 805 811 (Pubitemid 32447929)
52. C.G. Dietrich, D.R. de Waart, R. Ottenhoff, I.G. Schoots, and R.P. Elferink Increased bioavailability of the food-derived carcinogen 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine in MRP2-deficient rats Mol Pharmacol 59 2001 974 980 (Pubitemid 32381575)
53. M.L. Vlaming, K. Mohrmann, E. Wagenaar, D.R. de Waart, R.P. Elferink, J.S. Lagas, O. van Tellingen, L.D. Vainchtein, H. Rosing, and J.H. Beijnen Carcinogen and anticancer drug transport by Mrp2 in vivo: studies using Mrp2 (Abcc2) knockout mice J Pharmacol Exp Ther 318 2006 319 327
54. T. Giessmann, C. Modess, U. Hecker, M. Zschiesche, P. Dazert, C. Kunert-Keil, R. Warzok, G. Engel, W. Weitschies, and I. Cascorbi CYP2D6 genotype and induction of intestinal drug transporters by rifampin predict presystemic clearance of carvedilol in healthy subjects Clin Pharmacol Ther 75 2004 213 222 (Pubitemid 38314871)
55. S. Oswald, T. Giessmann, D. Luetjohann, D. Wegner, D. Rosskopf, W. Weitschies, and W. Siegmund Disposition and sterol-lowering effect of ezetimibe are influenced by single-dose coadministration of rifampin, an inhibitor of multidrug transport proteins Clin Pharmacol Ther 80 2006 477 485 (Pubitemid 44767877)