In vitro techniques to study transporter-based DDI

Enzyme- and Transporter-Based Drug-Drug Interactions: Progress and Future Challenges

Volumn , Issue , 2010, Pages 237-255

  Bleasby, Kelly ^a   Chu, Xiaoyan ^a   Evers, Raymond ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 84859109960     PISSN: None     EISSN: None     Source Type: Book    
DOI: 10.1007/978-1-4419-0840-7_9     Document Type: Chapter

References (74)

1. Acharya P, O'Connor MP, Polli JW, Ayrton A, Ellens H and Bentz J (2008) Kinetic identification of membrane transporters that assist P-glycoprotein- mediated transport of digoxin and loperamide through a confluent monolayer of MDCKII-hMDR1 cells. Drug Metab Dispos 36:452-460
2. Allen JD, Van Loevezijn A, Lakhai JM, Van Der Valk M, Van Tellingen O, Reid G, Schellens JH, Koomen GJ and Schinkel AH (2002) 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 1:417-425
3. Balimane PV, Marino A and Chong S (2008) P-gp inhibition potential in cell-based models: which "calculation" method is the most accurate?. AAPS J 10:577-586
4. Borst P, Zelcer N, Van De Wetering K and Poolman B (2007) On the putative cotransport of drugs by multidrug resistance proteins. FEBS Lett 580:1085-1093
5. Byrne JA, Strautnieks SS, Mieli-Vergani G, Higgins CF, Linton KJ and Thompson RJ (2002) The human bile salt export pump: characterization of substrate specificity and identification of inhibitors. Gastroenterology 123:1649-1658
6. Cai J and Gros P (2003) Overexpression, purification and functional characterization of ATP-binding cassette transporters in the yeast Pichia Pastoris. Biochem Biophys Acta 1610:63-76
7. Chen ZS, Lee K, Walther S, Raftogianis RB, Kuwano M, Zeng H and Kruh GD (2002) Analysis of methotrexate and folate transport by multidrug resistance protein 4 (ABCC4): MRP4 is a component of the methotrexate efflux system. Cancer Res 62:3144-3150
8. Chu XY, Bleasby K, Yabut J, Cai X, Chan GH, Hafey MJ, Xu S, Bergman AJ, Braun MP, Dean DC and Evers R (2007) Transport of the dipeptidyl peptidase-4 inhibitor sitagliptin by human organic anion transporter 3, organic anion transporting polypeptide 4C1, and multidrug resistance P-glycoprotein. J Pharmacol Exp Ther 321:673-683
9. Chu XY, Huskey SE, Braun MP, Sarkadi B, Evans DC and Evers R (2004) Transport of ethinylestradiol glucuronide and ethinylestradiol sulfate by the multidrug resistance proteins MRP1, MRP2, and MRP3. J Pharmacol Exp Ther 309:156-164
10. Chu XY, Liang Y, Cai X, Cuevas-Licea K, Rippley RK, Kassahun K, Shou M, Braun MP, Doss GA, Anari MR and Evers R (2009) Metabolism and renal elimination of gaboxadol in humans: role of UDP-glucuronosyltransferases and transporters. Pharm Res 26:459-468
11. Cihlar T, Lin DC, Pritchard JB, Fuller MD, Mendel DB and Sweet DH (1999) The antiviral nucleotide analogs cidofovir and adefovir are novel substrates for human and rat renal organic anion transporter 1. Mol Pharmacol 56:570-580
12. Cole SP and Deeley RG (2006) Transport of glutathione and glutathione conjugates by MRP1. Trends Pharmacol Sci 27:438-446
13. Cui Y, König J and Keppler D (2001) Vectorial transport by double-transfected cells expressing the human uptake transporter SLC21A8 and the apical export pump ABCC2. Mol Pharmacol 60:934-943
14. El-Sheikh AA, Masereeuw R, and Russel FG. (2008) Mechanisms of renal anionic transport. Eur J Pharamcol 585:245-255
15. Evers R and Chu XY (2008) Role of the murine organic anion-transporting polypeptide 1b2 (Oatp1b2) in drug disposition and hepatotoxicity. Mol Pharmacol 74:309-311
16. Feng B, Obach RS, Burstein AH, Clark DJ, De Morais SM and Faessel HM (2008) Effect of human renal cationic transporter inhibition on the pharmacokinetics of varenicline, a new therapy for smoking cessation: an in vitro-in vivo study. Clin Pharmacol Ther 83:567-576
17. Ghibellini G, Leslie EM and Brouwer KL (2006) Methods to evaluate biliary excretion of drugs in humans: an updated review. Mol Pharm 3:198-211
18. Ghibellini G, Vasist LS, Leslie EM, Heizer WD, Kowalsky RJ, Calvo BF and Brouwer KL (2007) In vitro-in vivo correlation of hepatobiliary drug clearance in humans. Clin Pharmacol Ther 81:406-413
19. Glavinas H, Méhn D, Jani M, Oosterhuis B, Herédi- Szabó K and Krajcsi P (2008) Utilization of membrane vesicle preparations to study drug-ABC transporter interactions. Expert Opin Drug Metab Toxicol 4:721-732
20. Gorboulev V, Ulzheimer JC, Akhoundova A, Ulzheimer-Teuber I, Karbach U, Quester S, Baumann C, Lang F, Busch AE and Koepsell H (1997) Cloning and characterization of two human polyspecific organic cation transporters. DNA Cell Biol 16:871-881
21. Hagenbuch B and Meier PJ (1994) Molecular cloning, chromosomal localization, and functional characterization of a human liver Na+/bile acid cotransporter. J Clin Invest 93:1326-1331
22. Hayer-Zillgen M, Brüss M and Bönisch H (2002) Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol 136:829-836
23. Hewitt NJ, Lechón MJ, Houston JB, Hallifax D, Brown HS, Maurel P, Kenna JG, Gustavsson L, Lohmann C, Skonberg C, Guillouzo A, Tuschl G, Li AP, Le Cluyse E, Groothuis GM and Hengstler JG (2007) Primary hepatocytes: current understanding of the regulation of metabolic enzymes and transporter proteins, and pharmaceutical practice for the use of hepatocytes in metabolism, enzyme induction, transporter, clearance, and hepatotoxicity studies. Drug Metab Rev 39:159-234
24. Hirano M, Maeda K, Shitara Y and Sugiyama Y (2004) Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther 311:139-146
25. Hirano M, Maeda K, Shitara Y and Sugiyama Y (2006) Drug-drug interaction between pitavastatin and various drugs via OATP1B1. Drug Metab Dispos 34:1229-1236
26. Ishiguro N, Maeda K, Saito A, Kishimoto W, Matsushima S, Ebner T, Roth W, Igarashi T and Sugiyama Y (2008) Establishment of a set of double transfectants coexpressing organic anion transporting polypeptide 1B3 and hepatic efflux transporters for the characterization of the hepatobiliary transport of telmisartan acylglucuronide. Drug Metab Dispos 36:796-805
27. Ishikawa T, Müller M, Klünemann C, Schaub T and Keppler D (1990) ATP-dependent primary active transport of cysteinyl leukotrienes across liver canalicular membrane. Role of the ATP-dependent transport system for glutathione S-conjugates. J Biol Chem 265:19279-19286
28. Jedlitschky G, Hoffmann U and Kroemer HK (2006) Structure and function of the MRP2 (ABCC2) protein and its role in drug disposition. Expert Opin Drug Metab Toxicol 2:351-366
29. Kalvass JC and Pollack GM (2007) Kinetic considerations for the quantitative assessment of efflux activity and inhibition: implications for understanding and predicting the effects of efflux inhibition. Pharm Res 24:265-276
30. Kamiie J, Ohtsuki S, Iwase R, Ohmine K, Katsukura Y, Yanai K, Sekine Y, Uchida Y, Ito S and Terasaki T (2008) 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 25:1469-1483
31. Khetani SR and Bhatia SN (2008) Microscale culture of human liver cells for drug development. Nat Biotechnol 26:120-126
32. Kopplow K, Letschert K, König J, Walter B and Keppler D (2005) Human hepatobiliary transport of organic anions analyzed by quadruple-transfected cells. Mol Pharmacol 68:1031-1038
33. König J, Cui Y, Nies AT and Keppler D (2000) A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane. Am J Physiol Gastrointest Liver Physiol 278:G156-G164
34. Lau YY, Huang Y, Frasetto L and Benet LZ (2006) Effect of OATP1B1 transporter inhibition on the pharmacokinetics of atorvastatin in healthy volunteers. Clin Pharmacol Ther 81:194-204
35. Le Cluyse EL, Audus KL and Hochman JH (1994) Formation of extensive canalicular networks by rat hepatocytes cultured in collagen-sandwich configuration. Am J Physiol 266:C1764-C1774
36. Lee W and Kim RB (2004) Transporters and renal drug elimination. Ann Rev Pharmacol Toxicol 44:137-166
37. Li M, Anderson GD and Wang J (2006) Drug-drug interactions involving membrane transporters in the human kidney. Expert Opin Drug Metab Toxicol 2:505-532
38. Li N, Zhang Y, Hua F and Lai Y (2009) 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 37:66-73
39. Link E, Parish S, Armitage J, Bowman L, Heath S, Matsuda F, Gut I, Lathrop M and Collins R (2008) SLCO1B1 variants and statin-induced myopathy - a genome wide study. N Engl J Med 359:789-799
40. Liu X, Chism JP, Le Cluyse EL, Brouwer KR and Brouwer KL (1999a) Correlation of biliary excretion in sandwich-cultured rat hepatocytes and in vivo in rats. Drug Metab Dispos 27:637-644
41. Liu X, Le Cluyse EL, Brouwer KR, Gan LS, Lemasters JJ, Stieger B, Meier PJ and Brouwer KL (1999b) Biliary excretion in primary rat hepatocytes cultured in a collagen-sandwich configuration. Am J Physiol 277:G12-G21
42. Matsushima S, Maeda K, Inoue K, Ohta KY, Yuasa H, Kondo T, Nakayama H, Horita S, Kusuhara H and Sugiyama Y (2009) The inhibition of human multidrug and toxin extrusion 1 is involved in the drug-drug interaction caused by cimetidine. Drug Metab Dispos 37:555-559
43. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H and Sugiyama Y (2005) Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther 314:1059-1067
44. Mikkaichi T, Suzuki T, Onogawa T, Tanemoto M, Mizutamari H, Okada M, Chaki T, Masuda S, Tokui T, Eto N, Abe M, Satoh F, Unno M, Hishinuma T, Inui K, Ito S, Goto J and Abe T (2004) Isolation and characterization of a digoxin transporter and its rat homologue expressed in the kidney. Proc Natl Acad Sci USA 101:3569-3574
45. Mita S, Suzuki H, Akita H, Stieger B, Meier PJ, Hofmann AF and Sugiyama Y (2005) Vectorial transport of bile salts across MDCK cells expressing both rat Na+-taurocholate cotransporting polypeptide and rat bile salt export pump. Am J Physiol Gastrointest Liver Physiol 288:G159-G167
46. Mück W, Mai I, Fritsche L, Ochmann K, Rohde G, Unger S, Johne A, Bauer S, Budde K, Roots I, Neumayer HH and Kuhlmann J (1999) Increase in cerivastatin systemic exposure after single and multiple dosing in cyclosporine-treated kidney transplant recipients. Clin Pharmacol Ther 65:251-261
47. Neuvonen PJ, Niemi M and Backman J (2006) Drug interactions with lipid-lowering drugs: Mechanism and clinical relevance. Clin Pharmacol Ther 80:565-581
48. Nies AT, Herrmann E, Brom M and Keppler D (2008) Vectorial transport of the plant alkaloid berberine by double-transfected cells expressing the human organic cation transporter 1 (OCT1, SLC22A1) and the efflux pump MDR1 P-glycoprotein (ABCB1).. Naunyn Schmiedebergs Arch Pharmacol 376:449-461
49. Poirier A, Lave T, Portmann R, Brun ME, Senner F, Kansy M, Grimm HP and Funk C (2008) Design, data analysis, and simulation of in vitro drug transport kinetic experiments using a mechanistic in vitro model. Drug Metab Dispos 36:2434-2444
50. Rautio J, Humphreys JE, Webster LO, Balakrishnan A, Keogh JP, Kunta JR, Serabjit-Singh CJ and Polli JW (2006) In vitro P-glycoprotein inhibition assays for assessment of clinical drug interaction potential of new drug candidates: a recommendation for probe substrates. Drug Metab Dispos 34:786-792
51. Regazzi MB, Iacona I, Campana C, Raddato V, Lesi C, Perani G, Gavazzi A and Vigano M (1993) Altered disposition of pravastatin following concomitant drug therapy with cyclosporin A in transplant recipients. Transplant Proc 25:2732-2734
52. Roelofsen H, Bakker CT, Schoemaker B, Heijn M, Jansen PL and Elferink RP (1995) Redistribution of canalicular organic anion transport activity in isolated and cultured rat hepatocytes. Hepatology 21:1649-1657
53. Russel FG, Masereeuw R and Van Aubel RA (2002) Molecular aspects of renal anionic drug transport. Ann Rev Physiol 64:563-594
54. Saito H, Hirano H, Nakagawa H, Fukami T, Oosumi K, Murakami K, Kimura H, Kouchi T, Konomi M, Tao E, Tsujikawa N, Tarui S, Nagakura M, Osumi M and Ishikawa T (2006) A new strategy of high-speed screening and quantitative structure-activity relationship analysis to evaluate human ATP-binding cassette transporter ABCG2-drug interactions. J Pharmacol Exp Ther 317:1114-1124
55. Sasaki M, Suzuki H, Aoki J, Ito K, Meier PJ and Sugiyama Y (2004) Prediction of in vivo biliary clearance from the in vitro transcellular transport of organic anions across a double-transfected Madin-Darby canine kidney II monolayer expressing both rat organic anion transporting polypeptide 4 and multidrug resistance associated protein 2. Mol Pharmacol 66:450-459
56. Sasaki M, Suzuki H, Ito K, Abe T and Sugiyama Y (2002) Transcellular transport of organic anions across a double-transfected Madin-Darby canine kidney II cell monolayer expressing both human organic anion-transporting polypeptide (OATP2/SLC21A6) and Multidrug resistance-associated protein 2 (MRP2/ABCC2. J Biol Chem 277:6497-6503
57. Sato T, Masuda S, Yonezawa A, Tanihara Y, Katsura T and Inui K (2008) Transcellular transport of organic cations in double-transfected MDCK cells expressing human organic cation transporters hOCT1/hMATE1 and hOCT2/hMATE1. Biochem Pharmacol 76:894-903
58. Shitara Y, Itoh T, Sato H, Li AP and Sugiyama Y (2003a) Inhibition of transporter-mediated hepatic uptake as a mechanism for drug-drug interaction between cerivastatin and cyclosporin A. J Pharmacol Exp Ther 304:610-616
59. Shitara Y, Li AP, Kato Y, Lu C, Ito K, Itoh T and Sugiyama Y (2003b) Function of uptake transporters for taurocholate and estradiol 17beta-D-glucuronide in cryopreserved human hepatocytes. Drug Metab Pharmacokinet 18:33-41
60. Shu Y, Sheardown SA, Brown C, Owen RP, Zhang S, Castro RA, Ianculescu AG, Yue L, Lo JC, Burchard EG, Brett CM, and Giacomini KM. (2007) Effect of genetic variation in the organic cation transporter 1 (OCT1) in metformin action. J Clin Invest 117:1422-1431
61. Smit JW, Weert B, Schinkel AH and Meijer DK (1998) Heterologous expression of various P-glycoproteins in polarized epithelial cells induces directional transport of small (type 1) and bulky (type 2) cationic drugs. J Pharmacol Exp Ther 286:321-327
62. Somogyi A, Stockley C, Keal J, Rolan P and Bochner F (1987) Reduction of metformin renal tubular secretion by cimetidine in man. Br J Clin Pharmacol 23:545-551
63. Steck TL, Weinstein RS, Straus JH and Wallach DF (1970) Inside-out red cell membrane vesicles: preparation and purification. Science 168:255-257
64. Tahara H, Kusuhara H, Endou H, Koepsell H, Imaoka T, Fuse E and Sugiyama Y (2005) A species difference in the transport activities of H2 receptor antagonists by rat and human renal organic anion and cation transporters. J Pharmacol Exp Ther 315:337-345
65. Tamai I, Nozawa T, Koshida M, Nezu J, Sai Y and Tsuji A (2001) Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharm Res 18:1262-1269
66. Terada T and Inui K (2007) Physiological and pharmacokinetic roles of H+/organic cation antiporters (MATE/SLC47A. Biochem Pharmacol 75:1689-1696
67. Troutman MD and Thakker DR (2003) Novel Experimental Parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. Pharm Res 20:1210-1224
68. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ and Fattinger K (2002) Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology 36:164-172
69. Webborn PJ, Parker AJ, Denton RL and Riley RJ (2007) In vitro-in vivo extrapolation of hepatic clearance involving active uptake: theoretical and experimental aspects. Xenobiotica 37:1090-1109
70. Yamazaki M, Neway WE, Ohe T, Chen I, Rowe JF, Hochman JH, Chiba M and Lin JH (2001) In vitro substrate identification studies for p-glycoprotein-mediated transport: species difference and predictability of in vivo results. J Pharmacol Exp Ther 296:723-735
71. Zelcer N, Saeki T, Reid G, Beijnen JH and Borst P (2001) Characterization of drug transport by the human multidrug resistance protein 3 (ABCC3. J Biol Chem 276:46400-46407
72. Zeng H, Liu G, Rea PA and Kruh GD (2000) Transport of amphipathic anions by human multidrug resistance protein 3. Cancer Res 60:4779-4784
73. Zhang L, Dresser MJ, Gray AT, Yost SC, Terashita S and Giacomini KM (1997) Cloning and functional expression of a human liver organic cation transporter. Mol Pharmacol 51:913-921
74. Zhou SF, Wang LL, Di YM, Xue CC, Duan W, Li CG and Li Y (2008) Substrates and inhibitors of human multidrug resistance associated proteins and the implications in drug development. Curr Med Chem 15:1981-2039