The role of transporters in toxicity and disease

Drug Metabolism and Disposition

Volumn 42, Issue 4, 2014, Pages 541-545

  Schuetz, John D ^a   Swaan, Peter W ^b   Tweedie, Donald J ^c  

^a ST JUDE CHILDREN S RESEARCH HOSPITAL   (United States)

^b UNIVERSITY OF MARYLAND   (United States)

^c BOEHRINGER INGELHEIM PHARMACEUTICALS INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6BETA HYDROXYHYDROCORTISONE; ABC TRANSPORTER; BILE ACID; BILE SALT EXPORT PUMP; BREAST CANCER RESISTANCE PROTEIN; DRUG METABOLITE; GLUCURONOSYLTRANSFERASE 1A1; MULTIDRUG RESISTANCE ASSOCIATED PROTEIN 2; MULTIDRUG RESISTANCE ASSOCIATED PROTEIN 3; MULTIDRUG RESISTANCE ASSOCIATED PROTEIN 4; ORGANIC ANION TRANSPORTER 3; PROTON COUPLED FOLATE TRANSPORTER; REDUCED FOLATE CARRIER;

ANTINEOPLASTIC ACTIVITY; BILIRUBIN METABOLISM; HUMAN; KIDNEY TUBULE EXCRETION; LIPID TRANSPORT; NOTE; PRIORITY JOURNAL; PROTEIN FUNCTION; TOXIC HEPATITIS;

ANIMALS; CARRIER PROTEINS; DISEASE; DRUG INTERACTIONS; DRUG-RELATED SIDE EFFECTS AND ADVERSE REACTIONS; HUMANS; NEOPLASMS; PHARMACEUTICAL PREPARATIONS; XENOBIOTICS;

EID: 84896124417     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.114.057539     Document Type: Note

References (55)

1. Aller SG, Yu J, Ward A, Weng Y, Chittaboina S, Zhuo R, Harrell PM, Trinh YT, Zhang Q, and Urbatsch IL, et al. (2009) Structure of P-glycoprotein reveals a molecular basis for poly-specific drug binding. Science 323:1718-1722.
2. Brouwer KL, Keppler D, Hoffmaster KA, Bow DA, Cheng Y, Lai Y, Palm JE, Stieger B, and Evers R; International Transporter Consortium (2013) In vitro methods to support transporter evaluation in drug discovery and development. Clin Pharmacol Ther 94:95-112.
3. Callaghan R, Luk F, and Bebawy M (2014) Inhibition of the multidrug resistance P-glycoprotein; time for a change of strategy? Drug Metab Dispos 42:623-631.
4. Canet MJ, Hardwick RN, Lake AD, Dzierlenga AL, Clarke JD, and Cherrington NJ (2014) Modeling human nonalcoholic steatohepatitis-associated changes in drug transporter expression using experimental rodent models. Drug Metab Dispos 42:586-595.
5. Center for Drug Evaluation and Research (CDER) (2012) Guidance for Industry: Drug Interaction Studies-Study Design, Data Analysis, Implications for Dosing, and Labeling Recommendations [Draft Guidance], U.S. Department of Health and Human Services, Food and Drug Administration, Rockville, MD. http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/ Guidances/ucm292362.pdf.
6. Chu X, Korzekwa K, Elsby R, Fenner K, Galetin A, Lai Y, Matsson P, Moss A, Nagar S, and Rosania GR, et al.; International Transporter Consortium (2013) Intracellular drug concentrations and transporters: measurement, modeling, and implications for the liver. Clin Pharmacol Ther 94:126-141.
7. Committee for Human Medicinal Products (CHMP) (2012) Guideline on the Investigation of Drug Interactions [Final], European Medicines Agency, London. http://www.ema.europa.eu/docs/en-GB/document-library/Scientific-guideline/2012/ 07/WC500129606.pdf.
8. Cressman A, McDonald C, Silver K, Kain K, and Piquette-Miller M (2014) Malaria infection alters the expression of hepatobiliary and placental drug transporters in pregnant mice. Drug Metab Dispos 42:603-610.
9. Cuperus FJC, Claudel T, Gautherot J, Halilbasic E, and Trauner M (2014) The role of canalicular ABC transporters in cholestasis. Drug Metab Dispos 42:546-560.
10. Dawson PA, Haywood J, Craddock AL, Wilson M, Tietjen M, Kluckman K, Maeda N, and Parks JS (2003) Targeted deletion of the ileal bile acid transporter eliminates enterohepatic cycling of bile acids in mice. J Biol Chem 278:33920-33927. (Pubitemid 37553226)
11. Dellicour S, Tatem AJ, Guerra CA, Snow RW, and ter Kuile FO (2010) Quantifying the number of pregnancies at risk of malaria in 2007: a demographic study. PLoS Med 7:e1000221.
12. Deo AK, Prasad B, Balogh L, Lai Y, and Unadkat JD (2012) Interindividual variability in hepatic expression of the multidrug resistance-associated protein 2 (MRP2/ABCC2): quantification by liquid chromatography/tandem mass spectrometry. Drug Metab Dispos 40:852-855.
13. Dubin IN and Johnson FB (1954) Chronic idiopathic jaundice with unidentified pigment in liver cells; a new clinicopathologic entity with a report of 12 cases. Medicine (Baltimore) 33: 155-197.
14. Fenner KS, Troutman MD, Kempshall S, Cook JA, Ware JA, Smith DA, and Lee CA (2009) Drug-drug interactions mediated through P-glycoprotein: clinical relevance and in vitro-in vivo correlation using digoxin as a probe drug. Clin Pharmacol Ther 85:173-181.
15. Giacomini KM, Balimane PV, Cho SK, Eadon M, Edeki T, Hillgren KM, Huang SM, Sugiyama Y, Weitz D, and Wen Y, et al.; International Transporter Consortium (2013) International Transporter Consortium commentary on clinically important transporter polymorphisms. Clin Pharmacol Ther 94:23-26.
16. Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, and Hillgren KM, et al.; International Transporter Consortium (2010) Membrane transporters in drug development. Nat Rev Drug Discov 9:215-236.
17. Gottesman MM, Fojo T, and Bates SE (2002) Multidrug resistance in cancer: role of ATPdependent transporters. Nat Rev Cancer 2:48-58. (Pubitemid 37328807)
18. Link E, Parish S, Armitage J, Bowman L, Heath S, Matsuda F, Gut I, Lathrop M, Collins R, and Collins R; SEARCH Collaborative Group (2008) SLCO1B1 variants and statin-induced myopathy - a genomewide study. N Engl J Med 359:789-799.
19. Hegedus C, Ozvegy-Laczka C, Apáti A, Magócsi M, Német K, Orfi L, Kéri G, Katona M, Takáts Z, and Váradi A, et al. (2009a) Interaction of nilotinib, dasatinib and bosutinib with ABCB1 and ABCG2: implications for altered anti-cancer effects and pharmacological properties. Br J Pharmacol 158:1153-1164.
20. Hegedus C, Szakács G, Homolya L, Orbán TI, Telbisz A, Jani M, and Sarkadi B (2009b) Ins and outs of the ABCG2 multidrug transporter: an update on in vitro functional assays. Adv Drug Deliv Rev 61:47-56.
21. Ho RH and Kim RB (2005) Transporters and drug therapy: implications for drug disposition and disease. Clin Pharmacol Ther 78:260-277. (Pubitemid 41254111)
22. Imamura Y, Tsuruya Y, Damme K, Heer D, Kumagai Y, Maeda K, Murayama N, Okudaira N, Kurihara A, and Izumi T, et al. (2014) 6b-hydroxycortisol is an endogenous probe for evaluation of drug-drug interactions involving a multi-specific renal organic anion transporter, OAT3/SLC22A8, in healthy subjects. Drug Metab Dispos 42:685-694.
23. International Committee on Harmonization (ICH) (2010) Guidance for Industry: M3(R2) Nonclinical Safety Studies for the Conduct of Human Clinical Trials and Marketing Authorization for Pharmaceuticals. Revision 1. Center for Biologics Evaluation and Research (CBER), Center for Drug Evaluation and Research (CDER), U.S. Food and Drug Administration, Rockville, MD. http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/ Guidances/ucm073246.pdf.
24. Juliano RL and Ling V (1976) A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants. Biochim Biophys Acta 455:152-162.
25. Kadakol A, Ghosh SS, Sappal BS, Sharma G, Chowdhury JR, and Chowdhury NR (2000) Genetic lesions of bilirubin uridine-diphosphoglucuronate glucuronosyltransferase (UGT1A1) causing Crigler-Najjar and Gilbert syndromes: correlation of genotype to phenotype. Hum Mutat 16:297-306.
26. Kaplowitz N (2005) Idiosyncratic drug hepatotoxicity. Nat Rev Drug Discov 4:489-499.
27. Keitel V, Burdelski M, Warskulat U, Kühlkamp T, Keppler D, Häussinger D, and Kubitz R (2005) Expression and localization of hepatobiliary transport proteins in progressive familial intrahepatic cholestasis. Hepatology 41:1160-1172. (Pubitemid 40593925)
28. Keppler D (2014) The roles of MRP2, MRP3, and OATP1B1 and OATP1B3 in conjugated hyperbilirubinemia. Drug Metab Dispos 42:561-565.
29. Kock K, Ferslew BC, Netterberg I, Yang K, Urban TJ, Swaan PW, Stewart PW, and Brouwer K (2014) Risk factors for development of cholestatic drug-induced liver injury: inhibition of hepatic basolateral bile acid transporters MRP3 and MRP4. Drug Metab Dispos 42:665-674.
30. König J, Nies AT, Cui Y, Leier I, and Keppler D (1999) Conjugate export pumps of the multidrug resistance protein (MRP) family: localization, substrate specificity, and MRP2-mediated drug resistance. Biochim Biophys Acta 1461:377-394.
31. Li Y, Zhou J, Ramsden D, Taub ME, O'Brien D, Xu J, Busacca CA, Gonnella N, and Tweedie DJ (2014) Enzyme-transporter interplay in the formation and clearance of abundant metabolites of faldaprevir found in excreta but not in circulation. Drug Metab Dispos 42:384-393.
32. Matherly LH, Wilson MR, and Hou Z (2014) The major facilitative folate transporters SLC19A1 and SLC46A1: biology and role in antifolate chemotherapy of cancer. Drug Metab Dispos 42: 632-649.
33. McBride BF, Yang T, Liu K, Urban TJ, Giacomini KM, Kim RB, and Roden DM (2009) The organic cation transporter, OCTN1, expressed in the human heart, potentiates antagonism of the HERG potassium channel. J Cardiovasc Pharmacol 54:63-71.
34. Mennone A, Soroka CJ, Cai SY, Harry K, Adachi M, Hagey L, Schuetz JD, and Boyer JL (2006) Mrp4-/- mice have an impaired cytoprotective response in obstructive cholestasis. Hepatology 43:1013-1021. (Pubitemid 43724626)
35. Mennone A, Soroka CJ, Harry KM, and Boyer JL (2010) Role of breast cancer resistance protein in the adaptive response to cholestasis. Drug Metab Dispos 38:1673-1678.
36. Ménochet K, Kenworthy KE, Houston JB, and Galetin A (2012) Use of mechanistic modeling to assess interindividual variability and interspecies differences in active uptake in human and rat hepatocytes. Drug Metab Dispos 40:1744-1756.
37. Merrell MD, Nyagode BA, Clarke J, Cherrington N, and Morgan ET (2014) Selective and cytokine-dependent regulation of hepatic transporters and bile acid homeostasis during infectious colitis in mice. Drug Metab Dispos 42:596-602.
38. Pastor CM, Mullhaupt B, and Stieger B (2014) The role of organic anion transporters in diagnosing liver diseases by magnetic resonance imaging. Drug Metab Dispos 42:675-684.
39. Paulusma CC, de Waart DR, Kunne C, Mok KS, and Elferink RP (2009) Activity of the bile salt export pump (ABCB11) is critically dependent on canalicular membrane cholesterol content. J Biol Chem 284:9947-9954.
40. Poirier A, Funk C, Scherrmann JM, and Lavé T (2009) Mechanistic modeling of hepatic transport from cells to whole body: application to napsagatran and fexofenadine. Mol Pharm 6:1716-1733.
41. Rodrigues A, Lai Y, Cvijic M, Elkin L, Zvyaga T, and Soars M (2014) Drug-induced perturbations of the bile acid pool, cholestasis, and hepatotoxicity: mechanistic considerations beyond the direct inhibition of the bile salt export pump. Drug Metab Dispos 42:566-574.
42. Sasongko L, Link JM, Muzi M, Mankoff DA, Yang X, Collier AC, Shoner SC, and Unadkat JD (2005) Imaging P-glycoprotein transport activity at the human blood-brain barrier with positron emission tomography. Clin Pharmacol Ther 77:503-514. (Pubitemid 40824964)
43. Schuetz EG, Strom S, Yasuda K, Lecureur V, Assem M, Brimer C, Lamba J, Kim RB, Ramachandran V, and Komoroski BJ, et al. (2001) Disrupted bile acid homeostasis reveals an unexpected interaction among nuclear hormone receptors, transporters, and cytochrome P450. J Biol Chem 276 :39411-39418.
44. Shitara Y, Horie T, and Sugiyama Y (2006) Transporters as a determinant of drug clearance and tissue distribution. Eur J Pharm Sci 27:425-446. (Pubitemid 43363338)
45. Sprowl J and Sparreboom A (2014) Uptake carriers and oncology drug safety. Drug Metab Dispos 42:611-622.
46. Strautnieks SS, Bull LN, Knisely AS, Kocoshis SA, Dahl N, Arnell H, Sokal E, Dahan K, Childs S, and Ling V, et al. (1998) A gene encoding a liver-specific ABC transporter is mutated in progressive familial intrahepatic cholestasis. Nat Genet 20:233-238. (Pubitemid 28507666)
47. Sweet DH (2005) Organic anion transporter (Slc22a) family members as mediators of toxicity. Toxicol Appl Pharmacol 204:198-215.
48. Telbisz A, Hegedus C, Varadi A, Sarkadi B, and Ozvegy-Laczka C (2014) Regulation of the function of the human ABCG2 multidrug transporter by cholesterol and bile acids: effects of mutations in potential substrate- and steroid-binding sites. Drug Metab Dispos 42:575-585.
49. van de Steeg E, van Esch A, Wagenaar E, Kenworthy KE, and Schinkel AH (2013) Influence of human OATP1B1, OATP1B3, and OATP1A2 on the pharmacokinetics of methotrexate and paclitaxel in humanized transgenic mice. Clin Cancer Res 19:821-832.
50. VanWert AL, Gionfriddo MR, and Sweet DH (2010) Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos 31:1-71.
51. Yu H and Tweedie D (2013) A perspective on the contribution of metabolites to drug-drug interaction potential: the need to consider both circulating levels and inhibition potency. Drug Metab Dispos 41:536-540.
52. Zamek-Gliszczynski MJ, Xiaoyan Chu X, Polli JW, and Paine MF (2014) Understanding the transport properties of metabolites: case studies and considerations for drug development. Drug Metab Dispos 42:650-664.
53. Zelcer N, Reid G, Wielinga P, Kuil A, van der Heijden I, Schuetz JD, and Borst P (2003a) Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4). Biochem J 371:361-367. (Pubitemid 36547618)
54. Zelcer N, Saeki T, Bot I, Kuil A, and Borst P (2003b) Transport of bile acids in multidrug-resistance-protein 3-overexpressing cells co-transfected with the ileal Na+-dependent bile-acid transporter. Biochem J 369:23-30. (Pubitemid 36174121)
55. Zhao R, Matherly LH, and Goldman ID (2009) Membrane transporters and folate homeostasis: intestinal absorption and transport into systemic compartments and tissues. Expert Rev Mol Med 11:e4.