Intestinal drug transporters: An overview

Advanced Drug Delivery Reviews

Volumn 65, Issue 10, 2013, Pages 1340-1356

  Estudante, Margarida ^a,b   Morais, José G ^a   Soveral, Graça ^a,c   Benet, Leslie Z ^b  

^a UNIVERSITY OF LISBON   (Portugal)

^b UNIVERSITY OF CALIFORNIA   (United States)

^c UNIVERSIDADE NOVA DE LISBOA   (Portugal)

Author keywords

BCRP; BDDCS; Intestinal drug transport; MCT; MRP; OATP; OCT; OCTN; P gp; PEPT; Transporter enzyme interplay

Indexed keywords

BCRP; BDDCS; DRUG TRANSPORT; MCT; MRP; OATP; OCT; OCTN; P-GP; PEPT; TRANSPORTER-ENZYME INTERPLAY;

BIOCHEMISTRY; CELL CULTURE; PHARMACOKINETICS;

ENZYMES;

ABC TRANSPORTER; ALISKIREN; BREAST CANCER RESISTANCE PROTEIN; CARRIER PROTEIN; CYTOCHROME P450 3A4; DIGOXIN; ELACRIDAR; MONOCARBOXYLATE TRANSPORTER 1; MULTIDRUG RESISTANCE PROTEIN; MULTIDRUG RESISTANCE PROTEIN 1; MULTIDRUG RESISTANCE PROTEIN 2; ORGANIC ANION TRANSPORTER; ORGANIC ANION TRANSPORTER POLYPEPTIDE; ORGANIC CATION TRANSPORTER; ORGANIC CATION TRANSPORTER 1; ORGANIC CATION TRANSPORTER 2; OSELTAMIVIR; PEPTIDE TRANSPORTER; PLASMA MEMBRANE MONOAMINE TRANSPORTER; RIFAMPICIN; TALINOLOL; TOPOTECAN; UNCLASSIFIED DRUG;

AREA UNDER THE CURVE; DRUG ABSORPTION; DRUG ANTAGONISM; DRUG BIOAVAILABILITY; DRUG CLASSIFICATION; DRUG HALF LIFE; DRUG TRANSPORT; ENZYME ACTIVITY; FOOD DRUG INTERACTION; GRAPEFRUIT JUICE; HUMAN; INTESTINE ABSORPTION; INTESTINE MUCOSA PERMEABILITY; MAXIMUM PLASMA CONCENTRATION; MILK; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; PROTEIN LOCALIZATION; REVIEW; SINGLE DRUG DOSE; SOLID TUMOR; TIME TO MAXIMUM PLASMA CONCENTRATION;

BCRP; BDDCS; INTESTINAL DRUG TRANSPORT; MCT; MRP; OATP; OCT; OCTN; P-GP; PEPT; TRANSPORTER-ENZYME INTERPLAY;

ANIMALS; BIOLOGICAL TRANSPORT; CYTOCHROME P-450 CYP3A; HUMANS; INTESTINES; MEMBRANE TRANSPORT PROTEINS; PHARMACEUTICAL PREPARATIONS;

EID: 84885390032     PISSN: 0169409X     EISSN: 18728294     Source Type: Journal    
DOI: 10.1016/j.addr.2012.09.042     Document Type: Review

References (227)

1. Giacomini K.M., Huang S.M., Tweedie D.J., Benet L.Z., Brouwer K.L., Chu X., Dahlin A., Evers R., Fischer V., Hillgren K.M., Hoffmaster K.A., Ishikawa T., Keppler D., Kim R.B., Lee C.A., Niemi M., Polli J.W., Sugiyama Y., Swaan P.W., Ware J.A., Wright S.H., Yee S.W., Zamek-Gliszczynski M.J., Zhang L. Membrane transporters in drug development. Nat. Rev. Drug Discov. 2010, 9:215-236.
2. Shitara Y., Horie T., Sugiyama Y. Transporters as a determinant of drug clearance and tissue distribution. Eur. J. Pharm. Sci. 2006, 27:425-446.
3. DeGorter M.K., Kim R.B. Hepatic drug transporters, old and new: pharmacogenomics, drug response, and clinical relevance. Hepatology 2009, 50:1014-1016.
4. Li P., Wang G.J., Robertson T.A., Roberts M.S. Liver transporters in hepatic drug disposition: an update. Curr. Drug Metab. 2009, 10:482-498.
5. Faber K.N., Muller M., Jansen P.L. Drug transport proteins in the liver. Adv. Drug Deliv. Rev. 2003, 55:107-124.
6. van Montfoort J.E., Hagenbuch B., Groothuis G.M., Koepsell H., Meier P.J., Meijer D.K. Drug uptake systems in liver and kidney. Curr. Drug Metab. 2003, 4:185-211.
7. Kikuchi R., Yagi S., Kusuhara H., Imai S., Sugiyama Y., Shiota K. Genome-wide analysis of epigenetic signatures for kidney-specific transporters. Kidney Int. 2010, 78:569-577.
8. Oswald S., Grube M., Siegmund W., Kroemer H.K. Transporter-mediated uptake into cellular compartments. Xenobiotica 2007, 37:1171-1195.
9. Wu C.Y., Benet L.Z. Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm. Res. 2005, 22:11-23.
10. Hediger M.A., Romero M.F., Peng J.B., Rolfs A., Takanaga H., Bruford E.A. The ABCs of solute carriers: physiological, pathological and therapeutic implications of human membrane transport proteinsIntroduction. Pflugers Arch. 2004, 447:465-468.
11. Sai Y. Biochemical and molecular pharmacological aspects of transporters as determinants of drug disposition. Drug Metab. Pharmacokinet. 2005, 20:91-99.
12. Shugarts S., Benet L.Z. The role of transporters in the pharmacokinetics of orally administered drugs. Pharm. Res. 2009, 26:2039-2054.
13. Franke R.M., Gardner E.R., Sparreboom A. Pharmacogenetics of drug transporters. Curr. Pharm. Des. 2010, 16:220-230.
14. Klaassen C.D., Aleksunes L.M. Xenobiotic, bile acid, and cholesterol transporters: function and regulation. Pharmacol. Rev. 2010, 62:1-96.
15. Shu Y. Research progress in the organic cation transporters. J. Cent. South Univ. (MedSci) 2011, 36:913-926.
16. Varma M.V., Ambler C.M., Ullah M., Rotter C.J., Sun H., Litchfield J., Fenner K.S., El-Kattan A.F. Targeting intestinal transporters for optimizing oral drug absorption. Curr. Drug Metab. 2010, 11:730-742.
17. Tucker T.G., Milne A.M., Fournel-Gigleux S., Fenner K.S., Coughtrie M.W. 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. 2012, 83:279-285.
18. Shibayama Y., Iwashita Y., Yoshikawa Y., Kondo T., Ikeda R., Takeda Y., Osada T., Sugawara M., Yamada K., Iseki K. Effect of 5-fluorouracil treatment on SN-38 absorption from intestine in rats. Biol. Pharm. Bull. 2011, 34:1418-1425.
19. Maeng H.J., Durk M.R., Chow E.C., Ghoneim R., Pang K.S. 1Alpha,25-dihydroxyvitamin D3 on intestinal transporter function: studies with the rat everted intestinal sac. Biopharm. Drug Dispos. 2011, 32:112-125.
20. Bhardwaj R. Intestinal transporters in drug absorption. Biopharmaceutics Applications in Drug Development 2008, 175-225. Springer. K. Rajesh, Y. Lawrence (Eds.).
21. Chan L.M., Lowes S., Hirst B.H. The ABCs of drug transport in intestine and liver: efflux proteins limiting drug absorption and bioavailability. Eur. J. Pharm. Sci. 2004, 21:25-51.
22. Muller F., Fromm M.F. Transporter-mediated drug-drug interactions. Pharmacogenomics 2011, 12:1017-1037.
23. Kunta J.R., Sinko P.J. Intestinal drug transporters: in vivo function and clinical importance. Curr. Drug Metab. 2004, 5:109-124.
24. Hunter J., Jepson M.A., Tsuruo T., Simmons N.L., Hirst B.H. Functional expression of P-glycoprotein in apical membranes of human intestinal Caco-2 cells. Kinetics of vinblastine secretion and interaction with modulators. J. Biol. Chem. 1993, 268:14991-14997.
25. Shapiro A.B., Fox K., Lam P., Ling V. Stimulation of P-glycoprotein-mediated drug transport by prazosin and progesterone. Evidence for a third drug-binding site. Eur. J. Biochem. 1999, 259:841-850.
26. He S.M., Sneed K.B., Chen X.W., Cao C., Zhou S.F. Herb-drug interactions and mechanistic and clinical considerations. Curr. Drug Metab. 2012, (Epub ahead of print).
27. Kim W.Y., Benet L.Z. P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro. Pharm. Res. 2004, 21:1284-1293.
28. Zhou S.F. Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica 2008, 38:802-832.
29. Hoffmann U., Kroemer H.K. The ABC transporters MDR1 and MRP2: multiple functions in disposition of xenobiotics and drug resistance. Drug Metab. Rev. 2004, 36:669-701.
30. Brown R.S., Lomri N., De Voss J., Rahmaoui C.M., Xie M.H., Hua T., Lidofsky S.D., Scharschmidt B.F. Enhanced secretion of glycocholic acid in a specially adapted cell line is associated with overexpression of apparently novel ATP-binding cassette proteins. Proc. Natl. Acad. Sci. U. S. A. 1995, 92:5421-5425.
31. Yang J.J., Milton M.N., Yu S., Liao M., Liu N., Wu J.T., Gan L., Balani S.K., Lee F.W., Prakash S., Xia C.Q. P-glycoprotein and breast cancer resistance protein affect disposition of tandutinib, a tyrosine kinase inhibitor. Drug Metab. Lett. 2010, 4:201-212.
32. Swed A., Eyal S., Madar I., Zohar-Kontante H., Weiss L., Hoffman A. The role of P-glycoprotein in intestinal transport versus the BBB transport of tetraphenylphosphonium. Mol. Pharm. 2009, 6:1883-1890.
33. Bailey D.G., Malcolm J., Arnold O., Spence J.D. Grapefruit juice-drug interactions. Br. J. Clin. Pharmacol. 1998, 46:101-110.
34. Benet L.Z. The drug transporter-metabolism alliance: uncovering and defining the interplay. Mol. Pharm. 2009, 6:1631-1643.
35. Spahn-Langguth H., Langguth P. Grapefruit juice enhances intestinal absorption of the P-glycoprotein substrate talinolol. Eur. J. Pharm. Sci. 2001, 12:361-367.
36. Custodio J.M., Wu C.Y., Benet L.Z. Predicting drug disposition, absorption/elimination/transporter interplay and the role of food on drug absorption. Adv. Drug Deliv. Rev. 2008, 60:717-733.
37. Gurley B.J., Swain A., Williams D.K., Barone G., Battu S.K. Gauging the clinical significance of P-glycoprotein-mediated herb-drug interactions: comparative effects of St. John's wort, Echinacea, clarithromycin, and rifampin on digoxin pharmacokinetics. Mol. Nutr. Food Res. 2008, 52:772-779.
38. Greiner B., Eichelbaum M., Fritz P., Kreichgauer H.P., von Richter O., Zundler J., Kroemer H.K. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J. Clin. Invest. 1999, 104:147-153.
39. Westphal K., Weinbrenner A., Zschiesche M., Franke G., Knoke M., Oertel R., Fritz P., von Richter O., Warzok R., Hachenberg T., Kauffmann H.M., Schrenk D., Terhaag B., Kroemer H.K., Siegmund W. Induction of P-glycoprotein by rifampin increases intestinal secretion of talinolol in human beings: a new type of drug/drug interaction. Clin. Pharmacol. Ther. 2000, 68:345-355.
40. Kurata Y., Ieiri I., Kimura M., Morita T., Irie S., Urae A., Ohdo S., Ohtani H., Sawada Y., Higuchi S., Otsubo K. Role of human MDR1 gene polymorphism in bioavailability and interaction of digoxin, a substrate of P-glycoprotein. Clin. Pharmacol. Ther. 2002, 72:209-219.
41. FDA Drug Interaction Studies 2006, Department of Health and Human Services, Center for Drug Evaluation Research (CDER), Rockville, MD.
42. Benet L.Z. Predicting drug disposition via application of a Biopharmaceutics Drug Disposition Classification System. Basic Clin. Pharmacol. Toxicol. 2010, 106:162-167.
43. Murakami T., Takano M. Intestinal efflux transporters and drug absorption. Expert Opin. Drug Metab. Toxicol. 2008, 4:923-939.
44. Broccatelli F., Larregieu C.A., Cruciani G., Oprea T.I., Benet L.Z. Improving the prediction of the brain disposition for orally administered drugs using BDDCS. Adv. Drug Deliv. Rev. 2012, 64:95-109.
45. Liu Y.H., Di Y.M., Zhou Z.W., Mo S.L., Zhou S.F. Multidrug resistance-associated proteins and implications in drug development. Clin. Exp. Pharmacol. Physiol. 2010, 37:115-120.
46. Yazdanian M., Glynn S.L., Wright J.L., Hawi A. Correlating partitioning and caco-2 cell permeability of structurally diverse small molecular weight compounds. Pharm. Res. 1998, 15:1490-1494.
47. Yu X.Q., Xue C.C., Wang G., Zhou S.F. Multidrug resistance associated proteins as determining factors of pharmacokinetics and pharmacodynamics of drugs. Curr. Drug Metab. 2007, 8:787-802.
48. Zhou S.F., Wang L.L., Di Y.M., Xue C.C., Duan W., Li C.G., Li Y. Substrates and inhibitors of human multidrug resistance associated proteins and the implications in drug development. Curr. Med. Chem. 2008, 15:1981-2039.
49. Kitamura Y., Hirouchi M., Kusuhara H., Schuetz J.D., Sugiyama Y. Increasing systemic exposure of methotrexate by active efflux mediated by multidrug resistance-associated protein 3 (mrp3/abcc3). J. Pharmacol. Exp. Ther. 2008, 327:465-473.
50. de Waart D.R., van de Wetering K., Kunne C., Duijst S., Paulusma C.C., Oude Elferink R.P. Oral availability of cefadroxil depends on ABCC3 and ABCC4. Drug Metab. Dispos. 2012, 40:515-521.
51. Cole S.P., Bhardwaj G., Gerlach J.H., Mackie J.E., Grant C.E., Almquist K.C., Stewart A.J., Kurz E.U., Duncan A.M., Deeley R.G. Overexpression of a transporter gene in a multidrug-resistant human lung cancer cell line. Science 1992, 258:1650-1654.
52. Peng K.C., Cluzeaud F., Bens M., Duong Van Huyen J.P., Wioland M.A., Lacave R., Vandewalle A. Tissue and cell distribution of the multidrug resistance-associated protein (MRP) in mouse intestine and kidney. J. Histochem. Cytochem. 1999, 47:757-768.
53. Schinkel A.H., Jonker J.W. Mammalian drug efflux transporters of the ATP binding cassette (ABC) family: an overview. Adv. Drug Deliv. Rev. 2003, 55:3-29.
54. Johnson D.R., Finch R.A., Lin Z.P., Zeiss C.J., Sartorelli A.C. The pharmacological phenotype of combined multidrug-resistance mdr1a/1b- and mrp1-deficient mice. Cancer Res. 2001, 61:1469-1476.
55. Payen L., Sparfel L., Courtois A., Vernhet L., Guillouzo A., Fardel O. The drug efflux pump MRP2: regulation of expression in physiopathological situations and by endogenous and exogenous compounds. Cell Biol. Toxicol. 2002, 18:221-233.
56. Akamine Y., Miura M., Sunagawa S., Kagaya H., Yasui-Furukori N., Uno T. Influence of drug-transporter polymorphisms on the pharmacokinetics of fexofenadine enantiomers. Xenobiotica 2010, 40:782-789.
57. van Waterschoot R.A., Heine R.T., Wagenaar E., van der Kruijssen C.M., Rooswinkel R.W., Huitema A.D., Beijnen J.H., Schinkel A.H. Effects of cytochrome P450 3A (CYP3A) and the drug transporters P-glycoprotein (MDR1/ABCB1) and MRP2 (ABCC2) on the pharmacokinetics of lopinavir. Br. J. Pharmacol. 2010, 160:1224-1233.
58. Green B.R., Bain L.J. Mrp2 is involved in the efflux and disposition of fosinopril. J. Appl. Toxicol. 2011, 10.1002/jat.1767.
59. Gerk P.M., Vore M. Regulation of expression of the multidrug resistance-associated protein 2 (MRP2) and its role in drug disposition. J. Pharmacol. Exp. Ther. 2002, 302:407-415.
60. Gao S., Jiang W., Yin T., Hu M. Highly variable contents of phenolics in St. John's Wort products affect their transport in the human intestinal Caco-2 cell model: pharmaceutical and biopharmaceutical rationale for product standardization. J. Agric. Food Chem. 2010, 58:6650-6659.
61. Fromm M.F., Kauffmann H.M., Fritz P., Burk O., Kroemer H.K., Warzok R.W., Eichelbaum M., Siegmund W., Schrenk D. The effect of rifampin treatment on intestinal expression of human MRP transporters. Am. J. Pathol. 2000, 157:1575-1580.
62. Ruiz M.L., Villanueva S.S., Luquita M.G., Pellegrino J.M., Rigalli J.P., Arias A., Sanchez Pozzi E.J., Mottino A.D., Catania V.A. Induction of intestinal multidrug resistance-associated protein 2 (Mrp2) by spironolactone in rats. Eur. J. Pharmacol. 2009, 623:103-106.
63. Mottino A.D., Hoffman T., Jennes L., Vore M. Expression and localization of multidrug resistant protein mrp2 in rat small intestine. J. Pharmacol. Exp. Ther. 2000, 293:717-723.
64. Dietrich C.G., de Waart D.R., Ottenhoff R., Schoots I.G., Elferink R.P. Increased bioavailability of the food-derived carcinogen 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine in MRP2-deficient rats. Mol. Pharmacol. 2001, 59:974-980.
65. Fujimoto H., Higuchi M., Watanabe H., Koh Y., Ghosh A.K., Mitsuya H., Tanoue N., Hamada A., Saito H. P-glycoprotein mediates efflux transport of darunavir in human intestinal Caco-2 and ABCB1 gene-transfected renal LLC-PK1 cell lines. Biol. Pharm. Bull. 2009, 32:1588-1593.
66. Yokooji T., Kida M., Mori M., Akashi H., Mori N., Yoshihara S., Murakami T. Interaction of Rhei Rhizoma extract with cytochrome P450 3A and efflux transporters in rats. Pharmazie 2010, 65:367-374.
67. Nait Chabane M., Al Ahmad A., Peluso J., Muller C.D., Ubeaud G. Quercetin and naringenin transport across human intestinal Caco-2 cells. J. Pharm. Pharmacol. 2009, 61:1473-1483.
68. Diaconu C.H., Cuciureanu M., Vlase L., Cuciureanu R. Food-drug interactions: grapefruit juice. Rev. Med. Chir. Soc. Med. Nat. Iasi 2011, 115:245-250.
69. Dahan A., Amidon G.L. MRP2 mediated drug-drug interaction: indomethacin increases sulfasalazine absorption in the small intestine, potentially decreasing its colonic targeting. Int. J. Pharm. 2010, 386:216-220.
70. Miyake K., Mickley L., Litman T., Zhan Z., Robey R., Cristensen B., Brangi M., Greenberger L., Dean M., Fojo T., Bates S.E. Molecular cloning of cDNAs which are highly overexpressed in mitoxantrone-resistant cells: demonstration of homology to ABC transport genes. Cancer Res. 1999, 59:8-13.
71. Allikmets R., Schriml L.M., Hutchinson A., Romano-Spica V., Dean M. A human placenta-specific ATP-binding cassette gene (ABCP) on chromosome 4q22 that is involved in multidrug resistance. Cancer Res. 1998, 58:5337-5339.
72. Bruyere A., Decleves X., Bouzom F., Ball K., Marques C., Treton X., Pocard M., Valleur P., Bouhnik Y., Panis Y., Scherrmann J.M., Mouly S. 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. 2010, 7:1596-1607.
73. Taipalensuu J., Tornblom H., Lindberg G., Einarsson C., Sjoqvist F., Melhus H., Garberg P., Sjostrom B., Lundgren B., Artursson P. Correlation of gene expression of ten drug efflux proteins of the ATP-binding cassette transporter family in normal human jejunum and in human intestinal epithelial Caco-2 cell monolayers. J. Pharmacol. Exp. Ther. 2001, 299:164-170.
74. Ni Z., Bikadi Z., Rosenberg M.F., Mao Q. Structure and function of the human breast cancer resistance protein (BCRP/ABCG2). Curr. Drug Metab. 2010, 11:603-617.
75. Sesink A.L., Arts I.C., de Boer V.C., Breedveld P., Schellens J.H., Hollman P.C., Russel F.G. Breast cancer resistance protein (Bcrp1/Abcg2) limits net intestinal uptake of quercetin in rats by facilitating apical efflux of glucuronides. Mol. Pharmacol. 2005, 67:1999-2006.
76. Ohura K., Nozawa T., Murakami K., Imai T. Evaluation of transport mechanism of prodrugs and parent drugs formed by intracellular metabolism in Caco-2 cells with modified carboxylesterase activity: temocapril as a model case. J. Pharm. Sci. 2011, 100:3985-3994.
77. Vlaming M.L., Lagas J.S., Schinkel A.H. Physiological and pharmacological roles of ABCG2 (BCRP): recent findings in Abcg2 knockout mice. Adv. Drug Deliv. Rev. 2009, 61:14-25.
78. Peroni R.N., Di Gennaro S.S., Hocht C., Chiappetta D.A., Rubio M.C., Sosnik A., Bramuglia G.F. 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. 2011, 82:1227-1233.
79. Haslam I.S., Wright J.A., O'Reilly D.A., Sherlock D.J., Coleman T., Simmons N.L. Intestinal ciprofloxacin efflux: the role of breast cancer resistance protein (ABCG2). Drug Metab. Dispos. 2011, 39:2321-2328.
80. Kruijtzer C.M., Beijnen J.H., Rosing H., ten Bokkel Huinink W.W., Schot M., Jewell R.C., Paul E.M., Schellens J.H. Increased oral bioavailability of topotecan in combination with the breast cancer resistance protein and P-glycoprotein inhibitor GF120918. J. Clin. Oncol. 2002, 20:2943-2950.
81. Hendricks C.B., Rowinsky E.K., Grochow L.B., Donehower R.C., Kaufmann S.H. Effect of P-glycoprotein expression on the accumulation and cytotoxicity of topotecan (SK&F 104864), a new camptothecin analogue. Cancer Res. 1992, 52:2268-2278.
82. Arimori K., Kuroki N., Hidaka M., Iwakiri T., Yamsaki K., Okumura M., Ono H., Takamura N., Kikuchi M., Nakano M. Effect of P-glycoprotein modulator, cyclosporin A, on the gastrointestinal excretion of irinotecan and its metabolite SN-38 in rats. Pharm. Res. 2003, 20:910-917.
83. Dohse M., Scharenberg C., Shukla S., Robey R.W., Volkmann T., Deeken J.F., Brendel C., Ambudkar S.V., Neubauer A., Bates S.E. Comparison of ATP-binding cassette transporter interactions with the tyrosine kinase inhibitors imatinib, nilotinib, and dasatinib. Drug Metab. Dispos. 2010, 38:1371-1380.
84. Sandborn W.J., Hanauer S.B. Systematic review: the pharmacokinetic profiles of oral mesalazine formulations and mesalazine pro-drugs used in the management of ulcerative colitis. Aliment. Pharmacol. Ther. 2003, 17:29-42.
85. Kasim N.A., Whitehouse M., Ramachandran C., Bermejo M., Lennernas H., Hussain A.S., Junginger H.E., Stavchansky S.A., Midha K.K., Shah V.P., Amidon G.L. Molecular properties of WHO essential drugs and provisional biopharmaceutical classification. Mol. Pharm. 2004, 1:85-96.
86. Dahan A., Amidon G.L. Small intestinal efflux mediated by MRP2 and BCRP shifts sulfasalazine intestinal permeability from high to low, enabling its colonic targeting. Am. J. Physiol. Gastrointest. Liver Physiol. 2009, 297:G371-G377.
87. Juan M.E., Gonzalez-Pons E., Planas J.M. Multidrug resistance proteins restrain the intestinal absorption of trans-resveratrol in rats. J. Nutr. 2010, 140:489-495.
88. Xu H., Kulkarni K.H., Singh R., Yang Z., Wang S.W., Tam V.H., Hu M. Disposition of naringenin via glucuronidation pathway is affected by compensating efflux transporters of hydrophilic glucuronides. Mol. Pharm. 2009, 6:1703-1715.
89. Vlaming M.L., Pala Z., van Esch A., Wagenaar E., de Waart D.R., van de Wetering K., van der Kruijssen C.M., Oude Elferink R.P., van Tellingen O., Schinkel A.H. Functionally overlapping roles of Abcg2 (Bcrp1) and Abcc2 (Mrp2) in the elimination of methotrexate and its main toxic metabolite 7-hydroxymethotrexate in vivo. Clin. Cancer Res. 2009, 15:3084-3093.
90. de Waart D.R., Vlaming M.L., Kunne C., Schinkel A.H., Oude Elferink R.P. Complex pharmacokinetic behavior of ezetimibe depends on abcc2, abcc3, and abcg2. Drug Metab. Dispos. 2009, 37:1698-1702.
91. Tamaki H., Satoh H., Hori S., Ohtani H., Sawada Y. Inhibitory effects of herbal extracts on breast cancer resistance protein (BCRP) and structure-inhibitory potency relationship of isoflavonoids. Drug Metab. Pharmacokinet. 2010, 25:170-179.
92. Polgar O., Robey R.W., Bates S.E. ABCG2: structure, function and role in drug response. Expert Opin. Drug Metab. Toxicol. 2008, 4:1-15.
93. Ahmed-Belkacem A., Pozza A., Macalou S., Perez-Victoria J.M., Boumendjel A., Di Pietro A. Inhibitors of cancer cell multidrug resistance mediated by breast cancer resistance protein (BCRP/ABCG2). Anticancer Drugs 2006, 17:239-243.
94. van Loevezijn A., Allen J.D., Schinkel A.H., Koomen G.J. Inhibition of BCRP-mediated drug efflux by fumitremorgin-type indolyl diketopiperazines. Bioorg. Med. Chem. Lett. 2001, 11:29-32.
95. Rabindran S.K., He H., Singh M., Brown E., Collins K.I., Annable T., Greenberger L.M. Reversal of a novel multidrug resistance mechanism in human colon carcinoma cells by fumitremorgin C. Cancer Res. 1998, 58:5850-5858.
96. Allen J.D., van Loevezijn A., Lakhai J.M., van der Valk M., van Tellingen O., Reid G., Schellens J.H., Koomen G.J., Schinkel A.H. Potent and specific inhibition of the breast cancer resistance protein multidrug transporter in vitro and in mouse intestine by a novel analogue of fumitremorgin C. Mol. Cancer Ther. 2002, 1:417-425.
97. Zhou M., Xia L., Wang J. Metformin transport by a newly cloned proton-stimulated organic cation transporter (plasma membrane monoamine transporter) expressed in human intestine. Drug Metab. Dispos. 2007, 35:1956-1962.
98. Ogihara H., Suzuki T., Nagamachi Y., Inui K., Takata K. Peptide transporter in the rat small intestine: ultrastructural localization and the effect of starvation and administration of amino acids. Histochem. J. 1999, 31:169-174.
99. Ogihara T., Kano T., Wagatsuma T., Wada S., Yabuuchi H., Enomoto S., Morimoto K., Shirasaka Y., Kobayashi S., Tamai I. Oseltamivir (tamiflu) is a substrate of peptide transporter 1. Drug Metab. Dispos. 2009, 37:1676-1681.
100. Fujiwara K., Shin M., Yoshizaki Y., Miyazaki T., Saita T. Immunocytochemistry for bestatin and its application to drug accumulation studies in rat intestine and kidney. J. Mol. Histol. 2011, 42:589-596.
101. Bergan T. Pharmacokinetic properties of the cephalosporins. Drugs 1987, 34(Suppl. 2):89-104.
102. de Waart D.R., van de Wetering K., Kunne C., Duijst S., Paulusma C.C., Oude Elferink R.P. Oral availability of cefadroxil depends on ABCC3 and ABCC4. Drug Metab. Dispos. 2011, 40:515-521.
103. Hellwig M., Geissler S., Matthes R., Peto A., Silow C., Brandsch M., Henle T. Transport of free and peptide-bound glycated amino acids: synthesis, transepithelial flux at Caco-2 cell monolayers, and interaction with apical membrane transport proteins. ChemBioChem 2011, 12:1270-1279.
104. Morimoto K., Kishimura K., Nagami T., Kodama N., Ogama Y., Yokoyama M., Toda S., Chiyoda T., Shimada R., Inano A., Kano T., Tamai I., Ogihara T. Effect of milk on the pharmacokinetics of oseltamivir in healthy volunteers. J. Pharm. Sci. 2011, 100:3854-3861.
105. Liu Z., Wang C., Liu Q., Meng Q., Cang J., Mei L., Kaku T., Liu K. Uptake, transport and regulation of JBP485 by PEPT1 in vitro and in vivo. Peptides 2011, 32:747-754.
106. Yan Z., Sun J., Chang Y., Liu Y., Fu Q., Xu Y., Sun Y., Pu X., Zhang Y., Jing Y., Yin S., Zhu M., Wang Y., He Z. Bifunctional peptidomimetic prodrugs of didanosine for improved intestinal permeability and enhanced acidic stability: synthesis, transepithelial transport, chemical stability and pharmacokinetics. Mol. Pharm. 2011, 8:319-329.
107. Zhang L., Luo T., Zhou J., Sun L., Xu Y. Synthesis and evaluation of a dipeptide-drug conjugate library as substrates for PEPT1. ACS Comb. Sci. 2012, 14:108-114.
108. Hu M., Subramanian P., Mosberg H.I., Amidon G.L. Use of the peptide carrier system to improve the intestinal absorption of l-alpha-methyldopa: carrier kinetics, intestinal permeabilities, and in vitro hydrolysis of dipeptidyl derivatives of l-alpha-methyldopa. Pharm. Res. 1989, 6:66-70.
109. Wang H.P., Lu H.H., Lee J.S., Cheng C.Y., Mah J.R., Ku C.Y., Hsu W., Yen C.F., Lin C.J., Kuo H.S. Intestinal absorption studies on peptide mimetic alpha-methyldopa prodrugs. J. Pharm. Pharmacol. 1996, 48:270-276.
110. +/peptide transporters revisited. J. Pharmacol. Exp. Ther. 2008, 327:432-441.
111. Miao Q., Liu Q., Wang C., Meng Q., Guo X., Peng J., Kaku T., Liu K. Inhibitory effect of zinc on the absorption of JBP485 via the gastrointestinal oligopeptide transporter (PEPT1) in rats. Drug Metab. Pharmacokinet. 2011, 26:494-502.
112. Ma K., Hu Y., Smith D.E. Influence of fed-fasted state on intestinal PEPT1 expression and in vivo pharmacokinetics of glycylsarcosine in wild-type and Pept1 knockout mice. Pharm. Res. 2012, 29:535-545.
113. Hindlet P., Barraud C., Boschat L., Farinotti R., Bado A., Buyse M. Rosiglitazone and metformin have opposite effects on intestinal absorption of oligopeptides via the proton-dependant PepT1 transporter. Mol. Pharmacol. 2012, 81:319-327.
114. Ingersoll S.A., Ayyadurai S., Charania M.A., Laroui H., Yan Y., Merlin D. The role and pathophysiological relevance of membrane transporter PepT1 in intestinal inflammation and inflammatory bowel disease. Am. J. Physiol. Gastrointest. Liver Physiol. 2011, 302:G484-G492.
115. Morita N., Kusuhara H., Sekine T., Endou H., Sugiyama Y. Functional characterization of rat organic anion transporter 2 in LLC-PK1 cells. J. Pharmacol. Exp. Ther. 2001, 298:1179-1184.
116. Yamamoto-Furusho J.K., Mendivil-Rangel E.J., Villeda-Ramirez M.A., Fonseca-Camarillo G., Barreto-Zuniga R. Gene expression of carnitine organic cation transporters 1 and 2 (OCTN) is downregulated in patients with ulcerative colitis. Inflamm. Bowel. Dis. 2011, 17:2205-2206.
117. Wojtal K.A., Eloranta J.J., Hruz P., Gutmann H., Drewe J., Staumann A., Beglinger C., Fried M., Kullak-Ublick G.A., Vavricka S.R. Changes in mRNA expression levels of solute carrier transporters in inflammatory bowel disease patients. Drug Metab. Dispos. 2009, 37:1871-1877.
118. Ringseis R., Wege N., Wen G., Rauer C., Hirche F., Kluge H., Eder K. Carnitine synthesis and uptake into cells are stimulated by fasting in pigs as a model of nonproliferating species. J. Nutr. Biochem. 2009, 20:840-847.
119. Ringseis R., Ludi S., Hirche F., Eder K. Treatment with pharmacological peroxisome proliferator-activated receptor alpha agonist clofibrate increases intestinal carnitine absorption in rats. Pharmacol. Res. 2008, 58:58-64.
120. Ringseis R., Luci S., Spielmann J., Kluge H., Fischer M., Geissler S., Wen G., Hirche F., Eder K. Clofibrate treatment up-regulates novel organic cation transporter (OCTN)-2 in tissues of pigs as a model of non-proliferating species. Eur. J. Pharmacol. 2008, 583:11-17.
121. Koch A., Konig B., Luci S., Stangl G.I., Eder K. Dietary oxidised fat up regulates the expression of organic cation transporters in liver and small intestine and alters carnitine concentrations in liver, muscle and plasma of rats. Br. J. Nutr. 2007, 98:882-889.
122. Hirano T., Yasuda S., Osaka Y., Kobayashi M., Itagaki S., Iseki K. Mechanism of the inhibitory effect of zwitterionic drugs (levofloxacin and grepafloxacin) on carnitine transporter (OCTN2) in Caco-2 cells. Biochim. Biophys. Acta 2006, 1758:1743-1750.
123. Grundemann D., Gorboulev V., Gambaryan S., Veyhl M., Koepsell H. Drug excretion mediated by a new prototype of polyspecific transporter. Nature 1994, 372:549-552.
124. Mizuno N., Niwa T., Yotsumoto Y., Sugiyama Y. Impact of drug transporter studies on drug discovery and development. Pharmacol. Rev. 2003, 55:425-461.
125. Steffansen B., Nielsen C.U., Brodin B., Eriksson A.H., Andersen R., Frokjaer S. Intestinal solute carriers: an overview of trends and strategies for improving oral drug absorption. Eur. J. Pharm. Sci. 2004, 21:3-16.
126. Engel K., Zhou M., Wang J. Identification and characterization of a novel monoamine transporter in the human brain. J. Biol. Chem. 2004, 279:50042-50049.
127. Engel K., Wang J. Interaction of organic cations with a newly identified plasma membrane monoamine transporter. Mol. Pharmacol. 2005, 68:1397-1407.
128. Okura T., Kato S., Takano Y., Sato T., Yamashita A., Morimoto R., Ohtsuki S., Terasaki T., Deguchi Y. Functional characterization of rat plasma membrane monoamine transporter in the blood-brain and blood-cerebrospinal fluid barriers. J. Pharm. Sci. 2011, 100:3924-3938.
129. Barnes K., Dobrzynski H., Foppolo S., Beal P.R., Ismat F., Scullion E.R., Sun L., Tellez J., Ritzel M.W., Claycomb W.C., Cass C.E., Young J.D., Billeter-Clark R., Boyett M.R., Baldwin S.A. Distribution and functional characterization of equilibrative nucleoside transporter-4, a novel cardiac adenosine transporter activated at acidic pH. Circ. Res. 2006, 99:510-519.
130. Xia L., Engel K., Zhou M., Wang J. Membrane localization and pH-dependent transport of a newly cloned organic cation transporter (PMAT) in kidney cells. Am. J. Physiol. Renal. Physiol. 2007, 292:F682-F690.
131. Takane H., Shikata E., Otsubo K., Higuchi S., Ieiri I. Polymorphism in human organic cation transporters and metformin action. Pharmacogenomics 2008, 9:415-422.
132. Mikkaichi T., Suzuki T., Tanemoto M., Ito S., Abe T. The organic anion transporter (OATP) family. Drug Metab. Pharmacokinet. 2004, 19:171-179.
133. Konig J., Seithel A., Gradhand U., Fromm M.F. Pharmacogenomics of human OATP transporters. Naunyn Schmiedebergs Arch. Pharmacol. 2006, 372:432-443.
134. Tamai I. Oral drug delivery utilizing intestinal OATP transporters. Adv. Drug Deliv. Rev. 2012, 64:508-514.
135. Visentin M., Chang M.H., Romero M.F., Zhao R., Goldman I.D. Substrate- and pH-specific antifolate transport mediated by organic anion-transporting polypeptide 2B1 (OATP2B1-SLCO2B1). Mol. Pharmacol. 2012, 81:134-142.
136. Kobayashi D., Nozawa T., Imai K., Nezu J., Tsuji A., Tamai I. Involvement of human organic anion transporting polypeptide OATP-B (SLC21A9) in pH-dependent transport across intestinal apical membrane. J. Pharmacol. Exp. Ther. 2003, 306:703-708.
137. Shirasaka Y., Suzuki K., Nakanishi T., Tamai I. Intestinal absorption of HMG-CoA reductase inhibitor pravastatin mediated by organic anion transporting polypeptide. Pharm. Res. 2010, 27:2141-2149.
138. Tamai I., Takanaga H., Maeda H., Ogihara T., Yoneda M., Tsuji A. Proton-cotransport of pravastatin across intestinal brush-border membrane. Pharm. Res. 1995, 12:1727-1732.
139. Triscari J., O'Donnell D., Zinny M., Pan H.Y. Gastrointestinal absorption of pravastatin in healthy subjects. J. Clin. Pharmacol. 1995, 35:142-144.
140. Shirasaka Y., Suzuki K., Shichiri M., Nakanishi T., Tamai I. Intestinal absorption of HMG-CoA reductase inhibitor pitavastatin mediated by organic anion transporting polypeptide and P-glycoprotein/multidrug resistance 1. Drug Metab. Pharmacokinet. 2011, 26:171-179.
141. Konig J., Glaeser H., Keiser M., Mandery K., Klotz U., Fromm M.F. Role of organic anion-transporting polypeptides for cellular mesalazine (5-aminosalicylic acid) uptake. Drug Metab. Dispos. 2011, 39:1097-1102.
142. Nozawa T., Imai K., Nezu J., Tsuji A., Tamai I. Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J. Pharmacol. Exp. Ther. 2004, 308:438-445.
143. Tapaninen T., Neuvonen P.J., Niemi M. Grapefruit juice greatly reduces the plasma concentrations of the OATP2B1 and CYP3A4 substrate aliskiren. Clin. Pharmacol. Ther. 2010, 88:339-342.
144. Nozawa T., Nakajima M., Tamai I., Noda K., Nezu J., Sai Y., Tsuji A., Yokoi T. Genetic polymorphisms of human organic anion transporters OATP-C (SLC21A6) and OATP-B (SLC21A9): allele frequencies in the Japanese population and functional analysis. J. Pharmacol. Exp. Ther. 2002, 302:804-813.
145. Dresser G.K., Bailey D.G., Leake B.F., Schwarz U.I., Dawson P.A., Freeman D.J., Kim R.B. Fruit juices inhibit organic anion transporting polypeptide-mediated drug uptake to decrease the oral availability of fexofenadine. Clin. Pharmacol. Ther. 2002, 71:11-20.
146. Perloff M.D., von Moltke L.L., Greenblatt D.J. Fexofenadine transport in Caco-2 cells: inhibition with verapamil and ritonavir. J. Clin. Pharmacol. 2002, 42:1269-1274.
147. Dresser G.K., Kim R.B., Bailey D.G. Effect of grapefruit juice volume on the reduction of fexofenadine bioavailability: possible role of organic anion transporting polypeptides. Clin. Pharmacol. Ther. 2005, 77:170-177.
148. Bailey D.G. Fruit juice inhibition of uptake transport: a new type of food-drug interaction. Br. J. Clin. Pharmacol. 2010, 70:645-655.
149. Imanaga J., Kotegawa T., Imai H., Tsutsumi K., Yoshizato T., Ohyama T., Shirasaka Y., Tamai I., Tateishi T., Ohashi K. The effects of the SLCO2B1 c.1457C>T polymorphism and apple juice on the pharmacokinetics of fexofenadine and midazolam in humans. Pharmacogenet Genomics 2011, 21:84-93.
150. Schwarz U.I., Seemann D., Oertel R., Miehlke S., Kuhlisch E., Fromm M.F., Kim R.B., Bailey D.G., Kirch W. Grapefruit juice ingestion significantly reduces talinolol bioavailability. Clin. Pharmacol. Ther. 2005, 77:291-301.
151. Lilja J.J., Backman J.T., Laitila J., Luurila H., Neuvonen P.J. Itraconazole increases but grapefruit juice greatly decreases plasma concentrations of celiprolol. Clin. Pharmacol. Ther. 2003, 73:192-198.
152. Lilja J.J., Juntti-Patinen L., Neuvonen P.J. Orange juice substantially reduces the bioavailability of the beta-adrenergic-blocking agent celiprolol. Clin. Pharmacol. Ther. 2004, 75:184-190.
153. Lilja J.J., Raaska K., Neuvonen P.J. Effects of orange juice on the pharmacokinetics of atenolol. Eur. J. Clin. Pharmacol. 2005, 61:337-340.
154. Neuhofel A.L., Wilton J.H., Victory J.M., Hejmanowsk L.G., Amsden G.W. Lack of bioequivalence of ciprofloxacin when administered with calcium-fortified orange juice: a new twist on an old interaction. J. Clin. Pharmacol. 2002, 42:461-466.
155. Roth M., Timmermann B.N., Hagenbuch B. Interactions of green tea catechins with organic anion-transporting polypeptides. Drug Metab. Dispos. 2011, 39:920-926.
156. Picard N., Levoir L., Lamoureux F., Yee S.W., Giacomini K.M., Marquet P. Interaction of sirolimus and everolimus with hepatic and intestinal organic anion-transporting polypeptide transporters. Xenobiotica 2011, 41:752-757.
157. Lee W., Glaeser H., Smith L.H., Roberts R.L., Moeckel G.W., Gervasini G., Leake B.F., Kim R.B. Polymorphisms in human organic anion-transporting polypeptide 1A2 (OATP1A2): implications for altered drug disposition and central nervous system drug entry. J. Biol. Chem. 2005, 280:9610-9617.
158. Paine M.F., Shen D.D., Kunze K.L., Perkins J.D., Marsh C.L., McVicar J.P., Barr D.M., Gillies B.S., Thummel K.E. First-pass metabolism of midazolam by the human intestine. Clin. Pharmacol. Ther. 1996, 60:14-24.
159. Kolars J.C., Awni W.M., Merion R.M., Watkins P.B. First-pass metabolism of cyclosporin by the gut. Lancet 1991, 338:1488-1490.
160. Edgar B., Bailey D., Bergstrand R., Johnsson G., Regardh C.G. Acute effects of drinking grapefruit juice on the pharmacokinetics and dynamics of felodipine-and its potential clinical relevance. Eur. J. Clin. Pharmacol. 1992, 42:313-317.
161. Cummins C.L., Jacobsen W., Benet L.Z. Unmasking the dynamic interplay between intestinal P-glycoprotein and CYP3A4. J. Pharmacol. Exp. Ther. 2002, 300:1036-1045.
162. Wacher V.J., Wu C.Y., Benet L.Z. 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, 13:129-134.
163. Schuetz E.G., Beck W.T., Schuetz J.D. Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol. Pharmacol. 1996, 49:311-318.
164. Zhang Y., Benet L.Z. The gut as a barrier to drug absorption: combined role of cytochrome P450 3A and P-glycoprotein. Clin. Pharmacokinet. 2001, 40:159-168.
165. Ito K., Kusuhara H., Sugiyama Y. Effects of intestinal CYP3A4 and P-glycoprotein on oral drug absorption-theoretical approach. Pharm. Res. 1999, 16:225-231.
166. Hochman J.H., Chiba M., Nishime J., Yamazaki M., Lin J.H. Influence of P-glycoprotein on the transport and metabolism of indinavir in Caco-2 cells expressing cytochrome P-450 3A4. J. Pharmacol. Exp. Ther. 2000, 292:310-318.
167. Cummins C.L., Salphati L., Reid M.J., Benet L.Z. In vivo modulation of intestinal CYP3A metabolism by P-glycoprotein: studies using the rat single-pass intestinal perfusion model. J. Pharmacol. Exp. Ther. 2003, 305:306-314.
168. Benet L.Z., Cummins C.L., Wu C.Y. Transporter-enzyme interactions: implications for predicting drug-drug interactions from in vitro data. Curr. Drug Metab. 2003, 4:393-398.
169. Amidon G.L., Lennernas H., Shah V.P., Crison J.R. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 1995, 12:413-420.
170. Wu C.Y., Benet L.Z. Disposition of tacrolimus in isolated perfused rat liver: influence of troleandomycin, cyclosporine, and GG918. Drug Metab. Dispos. 2003, 31:1292-1295.
171. Lam J.L., Benet L.Z. 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, 32:1311-1316.
172. Lau Y.Y., Wu C.Y., Okochi H., Benet L.Z. Ex situ inhibition of hepatic uptake and efflux significantly changes metabolism: hepatic enzyme-transporter interplay. J. Pharmacol. Exp. Ther. 2004, 308:1040-1045.
173. Lau Y.Y., Okochi H., Huang Y., Benet L.Z. Multiple transporters affect the disposition of atorvastatin and its two active hydroxy metabolites: application of in vitro and ex situ systems. J. Pharmacol. Exp. Ther. 2006, 316:762-771.
174. Takagi T., Ramachandran C., Bermejo M., Yamashita S., Yu L.X., Amidon G.L. A provisional biopharmaceutical classification of the top 200 oral drug products in the United States, Great Britain, Spain, and Japan. Mol. Pharm. 2006, 3:631-643.
175. Wright E.M., Martin M.G., Turk E. Intestinal absorption in health and disease-sugars. Best Pract. Res. Clin. Gastroenterol. 2003, 17:943-956.
176. Kanai Y., Endou H. Functional properties of multispecific amino acid transporters and their implications to transporter-mediated toxicity. J. Toxicol. Sci. 2003, 28:1-17.
177. Polli J.E., Abrahamsson B.S., Yu L.X., Amidon G.L., Baldoni J.M., Cook J.A., Fackler P., Hartauer K., Johnston G., Krill S.L., Lipper R.A., Malick W.A., Shah V.P., Sun D., Winkle H.N., Wu Y., Zhang H. Summary workshop report: bioequivalence, biopharmaceutics classification system, and beyond. AAPS J. 2008, 10:373-379.
178. Benet L.Z., Amidon G.L., Barends D.M., Lennernas H., Polli J.E., Shah V.P., Stavchansky S.A., Yu L.X. The use of BDDCS in classifying the permeability of marketed drugs. Pharm. Res. 2008, 25:483-488.
179. Chen M.L., Yu L. The use of drug metabolism for prediction of intestinal permeability (dagger). Mol. Pharm. 2009, 6:74-81.
180. Tolle-Sander S., Rautio J., Wring S., Polli J.W., Polli J.E. Midazolam exhibits characteristics of a highly permeable P-glycoprotein substrate. Pharm. Res. 2003, 20:757-764.
181. FDA Guidance for industry: waiver of in vivo bioavailability and bioequivalence studies for immediate-release solid oral dosage forms based on a Biopharmaceutics Classification System 2000, 13. F.a.D.A. U.S. Department of Health and Human Services, Rockville, MD. Center for Drug Evaluation, Research (CDER) (Ed.).
182. Cao X., Yu L.X., Barbaciru C., Landowski C.P., Shin H.C., Gibbs S., Miller H.A., Amidon G.L., Sun D. Permeability dominates in vivo intestinal absorption of P-gp substrate with high solubility and high permeability. Mol. Pharm. 2005, 2:329-340.
183. Benet L.Z., Broccatelli F., Oprea T.I. BDDCS applied to over 900 drugs. AAPS J. 2011, 13:519-547.
184. Gomez D.Y., Wacher V.J., Tomlanovich S.J., Hebert M.F., Benet L.Z. The effects of ketoconazole on the intestinal metabolism and bioavailability of cyclosporine. Clin. Pharmacol. Ther. 1995, 58:15-19.
185. Dahan A., Amidon G.L. Segmental dependent transport of low permeability compounds along the small intestine due to P-glycoprotein: the role of efflux transport in the oral absorption of BCS class III drugs. Mol. Pharm. 2009, 6:19-28.
186. Balimane P.V., Chong S., Morrison R.A. Current methodologies used for evaluation of intestinal permeability and absorption. J Pharmacol Toxicol Methods 2000, 44:301-312.
187. Tian S., Li Y., Wang J., Zhang J., Hou T. ADME evaluation in drug discovery. 9. Prediction of oral bioavailability in humans based on molecular properties and structural fingerprints. Mol. Pharm. 2011, 8:841-851.
188. Dressman J.B., Thelen K., Jantratid E. Towards quantitative prediction of oral drug absorption. Clin. Pharmacokinet. 2008, 47:655-667.
189. Wilson T.H., Wiseman G. The use of sacs of everted small intestine for the study of the transference of substances from the mucosal to the serosal surface. J. Physiol. 1954, 123:116-125.
190. Liu W., Okochi H., Benet L.Z., Zhai S.D. Sotalol permeability in cultured-cell, rat Intestine, and PAMPA system. Pharm. Res. 2012, 29:1768-1774.
191. Donowitz M., Singh S., Singh P., Salahuddin F.F., Chen Y., Chakraborty M., Murtazina R., Gucek M., Cole R.N., Zachos N.C., Kovbasnjuk O., Broere N., Smalley-Freed W.G., Reynolds A.B., Hubbard A.L., Seidler U., Weinman E., de Jonge H.R., Hogema B.M., Li X. Alterations in the proteome of the NHERF1 knockout mouse jejunal brush border membrane vesicles. Physiol. Genomics 2010, 42A:200-210.
192. Grass G.M., Sweetana S.A. In vitro measurement of gastrointestinal tissue permeability using a new diffusion cell. Pharm. Res. 1988, 5:372-376.
193. Lennernas H. Animal data: the contributions of the Ussing Chamber and perfusion systems to predicting human oral drug delivery in vivo. Adv Drug Deliv Rev 2007, 59:1103-1120.
194. Doluisio J.T., Billups N.F., Dittert L.W., Sugita E.T., Swintosky J.V. Drug absorption. I. An in situ rat gut technique yielding realistic absorption rates. J. Pharm. Sci. 1969, 58:1196-1200.
195. Zakeri-Milani P., Valizadeh H., Tajerzadeh H., Azarmi Y., Islambolchilar Z., Barzegar S., Barzegar-Jalali M. Predicting human intestinal permeability using single-pass intestinal perfusion in rat. J. Pharm. Pharm. Sci. 2007, 10:368-379.
196. Lane J.S., Whang E.E., Rigberg D.A., Hines O.J., Kwan D., Zinner M.J., McFadden D.W., Diamond J., Ashley S.W. Paracellular glucose transport plays a minor role in the unanesthetized dog. Am. J. Physiol. 1999, 276:G789-G794.
197. Balimane P.V., Chong S. Evaluation of permeability and P-glycoprotein interations: industry outlook. Biopharmaceutics Applications in Drug Development 2008, 101-132. Springer. K. Rajesh, Y. Lawrence (Eds.).
198. Balimane P.V., Chong S. Cell culture-based models for intestinal permeability: a critique. Drug Discov. Today 2005, 10:335-343.
199. Scheidweiler K.B., Ladenheim B., Barnes A.J., Cadet J.L., Huestis M.A. (+/-)-3,4-Methylenedioxymethamphetamine and metabolite disposition in plasma and striatum of wild-type and multidrug resistance protein 1a knock-out mice. J. Anal. Toxicol. 2011, 35:470-480.
200. Beumer J.H., Franke N.E., Tolboom R., Buckle T., Rosing H., Lopez-Lazaro L., Schellens J.H., Beijnen J.H., van Tellingen O. Disposition and toxicity of trabectedin (ET-743) in wild-type and mdr1 gene (P-gp) knock-out mice. Invest. New Drugs 2010, 28:145-155.
201. Cang J., Zhang J., Wang C., Liu Q., Meng Q., Wang D., Sugiyama Y., Tsuji A., Kaku T., Liu K. Pharmacokinetics and mechanism of intestinal absorption of JBP485 in rats. Drug Metab. Pharmacokinet. 2010, 25:500-507.
202. Hirouchi M., Kusuhara H., Onuki R., Ogilvie B.W., Parkinson A., Sugiyama Y. Construction of triple-transfected cells [organic anion-transporting polypeptide (OATP) 1B1/multidrug resistance-associated protein (MRP) 2/MRP3 and OATP1B1/MRP2/MRP4] for analysis of the sinusoidal function of MRP3 and MRP4. Drug Metab. Dispos. 2009, 37:2103-2111.
203. Cummins C.L., Jacobsen W., Christians U., Benet L.Z. CYP3A4-transfected Caco-2 cells as a tool for understanding biochemical absorption barriers: studies with sirolimus and midazolam. J. Pharmacol. Exp. Ther. 2004, 308:143-155.
204. Laitinem L. Caco-2 Cell Cultures in the Assessment of Intestinal Absorption: Effects of Some Co-administered Drugs and Natural Compounds in Biological Matrices 2006, Division of Biopharmaceutics and Pharmacokinetics, University of Helsinki, Helsinki.
205. Paixao P., Gouveia L.F., Morais J.A. Prediction of the in vitro permeability determined in Caco-2 cells by using artificial neural networks. Eur. J. Pharm. Sci. 2010, 41:107-117.
206. Broccatelli F., Cruciani G., Benet L.Z., Oprea T.I. BDDCS class prediction for new molecular entities. Mol. Pharm. 2012, 9:570-580.
207. Ding R., Tayrouz Y., Riedel K.D., Burhenne J., Weiss J., Mikus G., Haefeli W.E. Substantial pharmacokinetic interaction between digoxin and ritonavir in healthy volunteers. Clin. Pharmacol. Ther. 2004, 76:73-84.
208. Vallakati A., Chandra P.A., Pednekar M., Frankel R., Shani J. Dronedarone-induced digoxin toxicity: new drug, new interactions. Am. J. Ther. 2011, 10.1097/MJT.0b013e31821106c9.
209. Jerling M. Clinical pharmacokinetics of ranolazine. Clin. Pharmacokinet. 2006, 45:469-491.
210. Sababi M., Borga O., Hultkvist-Bengtsson U. The role of P-glycoprotein in limiting intestinal regional absorption of digoxin in rats. Eur. J. Pharm. Sci. 2001, 14:21-27.
211. Bigger J.T., Leahey E.B. Quinidine and digoxin. An important interaction. Drugs 1982, 24:229-239.
212. Fromm M.F., Kim R.B., Stein C.M., Wilkinson G.R., Roden D.M. Inhibition of P-glycoprotein-mediated drug transport: a unifying mechanism to explain the interaction between digoxin and quinidine [see comments]. Circulation 1999, 99:552-557.
213. Stephens R.H., O'Neill C.A., Bennett J., Humphrey M., Henry B., Rowland M., Warhurst G. Resolution of P-glycoprotein and non-P-glycoprotein effects on drug permeability using intestinal tissues from mdr1a (-/-) mice. Br. J. Pharmacol. 2002, 135:2038-2046.
214. Verstuyft C., Strabach S., El-Morabet H., Kerb R., Brinkmann U., Dubert L., Jaillon P., Funck-Brentano C., Trugnan G., Becquemont L. Dipyridamole enhances digoxin bioavailability via P-glycoprotein inhibition. Clin. Pharmacol. Ther. 2003, 73:51-60.
215. Hughes J., Crowe A. Inhibition of P-glycoprotein-mediated efflux of digoxin and its metabolites by macrolide antibiotics. J. Pharmacol. Sci. 2010, 113:315-324.
216. Rengelshausen J., Goggelmann C., Burhenne J., Riedel K.D., Ludwig J., Weiss J., Mikus G., Walter-Sack I., Haefeli W.E. Contribution of increased oral bioavailability and reduced nonglomerular renal clearance of digoxin to the digoxin-clarithromycin interaction. Br. J. Clin. Pharmacol. 2003, 56:32-38.
217. Boyd R.A., Stern R.H., Stewart B.H., Wu X., Reyner E.L., Zegarac E.A., Randinitis E.J., Whitfield L. Atorvastatin coadministration may increase digoxin concentrations by inhibition of intestinal P-glycoprotein-mediated secretion. J. Clin. Pharmacol. 2000, 40:91-98.
218. Westphal K., Weinbrenner A., Giessmann T., Stuhr M., Franke G., Zschiesche M., Oertel R., Terhaag B., Kroemer H.K., Siegmund W. Oral bioavailability of digoxin is enhanced by talinolol: evidence for involvement of intestinal P-glycoprotein. Clin. Pharmacol. Ther. 2000, 68:6-12.
219. Durr D., Stieger B., Kullak-Ublick G.A., Rentsch K.M., Steinert H.C., Meier P.J., Fattinger K. St John's Wort induces intestinal P-glycoprotein/MDR1 and intestinal and hepatic CYP3A4. Clin. Pharmacol. Ther. 2000, 68:598-604.
220. Laffont C.M., Toutain P.L., Alvinerie M., Bousquet-Melou A. Intestinal secretion is a major route for parent ivermectin elimination in the rat. Drug Metab Dispos 2002, 30:626-630.
221. Bardelmeijer H.A., Beijnen J.H., Brouwer K.R., Rosing H., Nooijen W.J., Schellens J.H., van Tellingen O. Increased oral bioavailability of paclitaxel by GF120918 in mice through selective modulation of P-glycoprotein. Clin. Cancer Res. 2000, 6:4416-4421.
222. Edwards D.J., Fitzsimmons M.E., Schuetz E.G., Yasuda K., Ducharme M.P., Warbasse L.H., Woster P.M., Schuetz J.D., Watkins P. 6',7'-Dihydroxybergamottin in grapefruit juice and Seville orange juice: effects on cyclosporine disposition, enterocyte CYP3A4, and P-glycoprotein. Clin. Pharmacol. Ther. 1999, 65:237-244.
223. Gramatte T., Oertel R. Intestinal secretion of intravenous talinolol is inhibited by luminal R-verapamil. Clin. Pharmacol. Ther. 1999, 66:239-245.
224. van Zuylen L., Verweij J., Nooter K., Brouwer E., Stoter G., Sparreboom A. Role of intestinal P-glycoprotein in the plasma and fecal disposition of docetaxel in humans. Clin. Cancer Res. 2000, 6:2598-2603.
225. Meerum Terwogt J.M., Malingre M.M., Beijnen J.H., ten Bokkel Huinink W.W., Rosing H., Koopman F.J., van Tellingen O., Swart M., Schellens J.H. Coadministration of oral cyclosporin A enables oral therapy with paclitaxel. Clin. Cancer Res. 1999, 5:3379-3384.
226. Dresser G.K., Schwarz U.I., Wilkinson G.R., Kim R.B. Coordinate induction of both cytochrome P4503A and MDR1 by St John's wort in healthy subjects. Clin. Pharmacol. Ther. 2003, 73:41-50.
227. Su Y., Hu P., Lee S.H., Sinko P.J. Using novobiocin as a specific inhibitor of breast cancer resistant protein to assess the role of transporter in the absorption and disposition of topotecan. J. Pharm. Pharm. Sci. 2007, 10:519-536.