Transporter biology in drug approval: Regulatory aspects

Molecular Aspects of Medicine

Volumn 34, Issue 2-3, 2013, Pages 711-718

  Maeda, Kazuya ^a   Sugiyama, Yuichi ^b  

^a UNIVERSITY OF TOKYO   (Japan)

^b RIKEN   (Japan)

Author keywords

(SLC22A6); Drug interaction number (DIN); Dynamic model; False negative predictions; MATE2 K (SLC47A2); Multidrug and toxin extrusion (MATE)1 (SLC47A1); Multidrug resistance 1 (MDR1, P glycoprotein (P gp)); OAT3 (SLC22A8); OATP1B3 (SLCO1B3); Organic anion transporter (OAT)1; Organic anion transporting polypeptide (OATP)1B1 (SLCO1B1); Organic cation transporter (OCT)2 (SLC22A2); Static model; Transporter mediated drug drug interaction

Indexed keywords

ADEFOVIR; BREAST CANCER RESISTANCE PROTEIN; CAPTOPRIL; CARRIER PROTEINS AND BINDING PROTEINS; CEFALEXIN; CEPHALOSPORIN DERIVATIVE; CIMETIDINE; CLARITHROMYCIN; CYCLOSPORIN A; DIGOXIN; DOFETILIDE; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; INDINAVIR; METFORMIN; MULTIDRUG AND TOXIN EXTRUSION 1; MULTIDRUG AND TOXIN EXTRUSION 2 K; MULTIDRUG RESISTANCE PROTEIN; ORGANIC ANION TRANSPORTER 1; ORGANIC ANION TRANSPORTER 1B1; ORGANIC ANION TRANSPORTER 1B3; ORGANIC ANION TRANSPORTER 2; ORGANIC ANION TRANSPORTER 3; PINDOLOL; PRAVASTATIN; PROBENECID; PYRIMETHAMINE; RIFAMYCIN; TALINOLOL; TENOFOVIR; UNCLASSIFIED DRUG; UNINDEXED DRUG;

AREA UNDER THE CURVE; CONCENTRATION RESPONSE; DRUG ANTAGONISM; DRUG APPROVAL; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG LEGISLATION; DRUG MECHANISM; DRUG POTENCY; DRUG POTENTIATION; DRUG TISSUE LEVEL; ENZYME SPECIFICITY; FALSE NEGATIVE PREDICTION; FALSE POSITIVE PREDICTION; FOOD AND DRUG ADMINISTRATION; HUMAN; IC 50; KIDNEY; LIVER; MOLECULAR BIOLOGY; PREDICTION; QUANTITATIVE ANALYSIS; RECEIVER OPERATING CHARACTERISTIC; REVIEW; RISK ASSESSMENT; SMALL INTESTINE;

DRUG APPROVAL; DRUG INTERACTIONS; HUMANS; MEMBRANE TRANSPORT PROTEINS; MODELS, BIOLOGICAL; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS; RISK MANAGEMENT;

EID: 84875161979     PISSN: 00982997     EISSN: 18729452     Source Type: Journal    
DOI: 10.1016/j.mam.2012.10.012     Document Type: Review

References (39)

1. 2]/IC50 criteria in the P-gp decision tree. J. Clin. Pharmacol.
2. J.T. Backman, C. Kyrklund, M. Neuvonen, and P.J. Neuvonen Gemfibrozil greatly increases plasma concentrations of cerivastatin Clin. Pharmacol. Ther. 72 6 2002 685 691
3. I. Cascorbi P-glycoprotein: tissue distribution, substrates, and functional consequences of genetic variations Handb. Exp. Pharmacol. 201 2011 261 283
4. 2]/IC50, that allow for the exclusion of drug candidates from clinical digoxin interaction studies Mol. Pharm. 7 2 2010 398 411
5. European Medicines Agency (EMA), 2012, Guideline on the Investigation of Drug Interactions. < http://www.ema.europa.eu/docs/en-GB/document-library/ Scientific-guideline/2012/07/WC500129606.pdf >.
6. C. Fahrmayr, M.F. Fromm, and J. Konig Hepatic OATP and OCT uptake transporters: their role for drug-drug interactions and pharmacogenetic aspects Drug Metab. Rev. 42 3 2010 380 401
7. US Food and Drug Administration (FDA), 2012. Guidance for Industry Drug Interaction Studies - Study Design, Data Analysis, Implications for Dosing, and Labeling Recommendations. < http://www.fda.gov/downloads/Drugs/ GuidanceComplianceRegulatoryInformation/Guidances/UCM292362.pdf >.
8. 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 2 2009 173 181
9. K.M. Giacomini, S.M. Huang, D.J. Tweedie, L.Z. Benet, K.L. Brouwer, X. Chu, A. Dahlin, R. Evers, V. Fischer, K.M. Hillgren, K.A. Hoffmaster, T. Ishikawa, D. Keppler, R.B. Kim, C.A. Lee, M. Niemi, J.W. Polli, Y. Sugiyama, P.W. Swaan, J.A. Ware, S.H. Wright, S.W. Yee, M.J. Zamek-Gliszczynski, and L. Zhang Membrane transporters in drug development Nat. Rev. Drug Discov. 9 3 2010 215 236
10. K.M. Giacomini, and Y. Sugiyama Membrane transporters and drug response L.L. Brunton, B.A. Cahbner, B.C. Knollmann, Goodman and Gilman's The Pharmacological Basis of Therapeutics 12th ed. 2011 McGraw-Hill New York 89 121
11. K. Grime, P.J. Webborn, and R.J. Riley Functional consequences of active hepatic uptake on cytochrome P450 inhibition in rat and human hepatocytes Drug Metab. Dispos. 36 8 2008 1670 1678
12. M. Hirano, K. Maeda, Y. Shitara, and Y. Sugiyama Drug-drug interaction between pitavastatin and various drugs via OATP1B1 Drug Metab. Dispos. 34 7 2006 1229 1236
13. S.M. Huang, and M. Rowland The role of physiologically based pharmacokinetic modeling in regulatory review Clin. Pharmacol. Ther. 91 3 2012 542 549
14. K. Ito, T. Iwatsubo, S. Kanamitsu, K. Ueda, H. Suzuki, and Y. Sugiyama Prediction of pharmacokinetic alterations caused by drug-drug interactions: metabolic interaction in the liver Pharmacol. Rev. 50 3 1998 387 412
15. S. Ito, H. Kusuhara, M. Yokochi, J. Toyoshima, K. Inoue, H. Yuasa, and Y. Sugiyama Competitive inhibition of the luminal efflux by multidrug and toxin extrusions, but not basolateral uptake by organic cation transporter 2, is the likely mechanism underlying the pharmacokinetic drug-drug interactions caused by cimetidine in the kidney J. Pharmacol. Exp. Ther. 340 2 2012 393 403
16. H. Koepsell, K. Lips, and C. Volk Polyspecific organic cation transporters: structure, function, physiological roles, and biopharmaceutical implications Pharm. Res. 24 7 2007 1227 1251
17. H. Kusuhara, S. Ito, Y. Kumagai, M. Jiang, T. Shiroshita, Y. Moriyama, K. Inoue, H. Yuasa, and Y. Sugiyama Effects of a MATE protein inhibitor, pyrimethamine, on the renal elimination of metformin at oral microdose and at therapeutic dose in healthy subjects Clin. Pharmacol. Ther. 89 6 2011 837 844
18. K. Maeda, and Y. Sugiyama In vitro-in vivo scale-up of drug transport activities G. You, M.E. Morris, Drug Transporters 2007 John Wiley & Sons. Inc. New Jersey 557 588
19. S. Matsushima, K. Maeda, K. Inoue, K.Y. Ohta, H. Yuasa, T. Kondo, H. Nakayama, S. Horita, H. Kusuhara, and Y. Sugiyama The inhibition of human multidrug and toxin extrusion 1 is involved in the drug-drug interaction caused by cimetidine Drug Metab. Dispos. 37 3 2009 555 559
20. S. Matsushima, K. Maeda, N. Ishiguro, T. Igarashi, and Y. Sugiyama Investigation of the inhibitory effects of various drugs on the hepatic uptake of fexofenadine in humans Drug Metab. Dispos. 36 4 2008 663 669
21. H.E. Meyer zu Schwabedissen, and H.K. Kroemer In vitro and in vivo evidence for the importance of breast cancer resistance protein transporters (BCRP/MXR/ABCP/ABCG2) Handb. Exp. Pharmacol. 201 2011 325 371
22. Ministry of Health, Labour and Welfare (MHLW), 2001, Guideline on the Investigation of Drug Interactions. < http://wwwhourei.mhlw.go.jp/cgi-bin/t- docframe2.cgi?MODE=tsuchi&DMODE=SEARCH&SMODE=NORMAL&KEYWORD= %92%b0%8a%c7&EFSNO=4125&FILE=FIRST&POS=0&HITSU=1 > (written in Japanese).
23. J. Noe, R. Portmann, M.E. Brun, and C. Funk Substrate-dependent drug-drug interactions between gemfibrozil, fluvastatin and other organic anion-transporting peptide (OATP) substrates on OATP1B1, OATP2B1, and OATP1B3 Drug Metab. Dispos. 35 8 2007 1308 1314
24. B.W. Ogilvie, D. Zhang, W. Li, A.D. Rodrigues, A.E. Gipson, J. Holsapple, P. Toren, and A. Parkinson Glucuronidation converts gemfibrozil to a potent, metabolism-dependent inhibitor of CYP2C8: implications for drug-drug interactions Drug Metab. Dispos. 34 1 2006 191 197
25. A.N. Rizwan, and G. Burckhardt Organic anion transporters of the SLC22 family: biopharmaceutical, physiological, and pathological roles Pharm. Res. 24 3 2007 450 470
26. Y. Shitara, M. Hirano, H. Sato, and Y. Sugiyama Gemfibrozil and its glucuronide inhibit the organic anion transporting polypeptide 2 (OATP2/OATP1B1:SLC21A6)-mediated hepatic uptake and CYP2C8-mediated metabolism of cerivastatin: analysis of the mechanism of the clinically relevant drug-drug interaction between cerivastatin and gemfibrozil J. Pharmacol. Exp. Ther. 311 1 2004 228 236
27. Y. Shitara, Y. Nagamatsu, S. Wada, Y. Sugiyama, and T. Horie Long-lasting inhibition of the transporter-mediated hepatic uptake of sulfobromophthalein by cyclosporin a in rats Drug Metab. Dispos. 37 6 2009 1172 1178
28. Y. Shitara, H. Sato, and Y. Sugiyama Evaluation of drug-drug interaction in the hepatobiliary and renal transport of drugs Annu. Rev. Pharmacol. Toxicol. 45 2005 689 723
29. H. Sugimoto, S. Matsumoto, M. Tachibana, S. Niwa, H. Hirabayashi, N. Amano, and T. Moriwaki Establishment of in vitro P-glycoprotein inhibition assay and its exclusion criteria to assess the risk of drug-drug interaction at the drug discovery stage J. Pharm. Sci. 100 9 2011 4013 4023
30. T. Tachibana, M. Kato, and Y. Sugiyama Prediction of nonlinear intestinal absorption of CYP3A4 and P-glycoprotein substrates from their in vitro Km values Pharm. Res. 29 3 2012 651 668
31. T. Tachibana, M. Kato, T. Watanabe, T. Mitsui, and Y. Sugiyama Method for predicting the risk of drug-drug interactions involving inhibition of intestinal CYP3A4 and P-glycoprotein Xenobiotica 39 6 2009 430 443
32. T. Takashima, S. Kitamura, Y. Wada, M. Tanaka, Y. Shigihara, H. Ishii, R. Ijuin, S. Shiomi, T. Nakae, Y. Watanabe, Y. Cui, H. Doi, M. Suzuki, K. Maeda, H. Kusuhara, Y. Sugiyama, and Y. Watanabe PET imaging-based evaluation of hepatobiliary transport in humans with (15R)-11C-TIC-Me J. Nucl. Med. 53 5 2012 741 748
33. T. Terada, and K. Inui Physiological and pharmacokinetic roles of H+/organic cation antiporters (MATE/SLC47A) Biochem. Pharmacol. 75 9 2008 1689 1696
34. M. Tsuda, T. Terada, T. Mizuno, T. Katsura, J. Shimakura, and K. Inui Targeted disruption of the multidrug and toxin extrusion 1 (mate1) gene in mice reduces renal secretion of metformin Mol. Pharmacol. 75 6 2009 1280 1286
35. M. Tsuda, T. Terada, M. Ueba, T. Sato, S. Masuda, T. Katsura, and K. Inui Involvement of human multidrug and toxin extrusion 1 in the drug interaction between cimetidine and metformin in renal epithelial cells J. Pharmacol. Exp. Ther. 329 1 2009 185 191
36. S. Watanabe, M. Tsuda, T. Terada, T. Katsura, and K. Inui Reduced renal clearance of a zwitterionic substrate cephalexin in MATE1-deficient mice J. Pharmacol. Exp. Ther. 334 2 2010 651 656
37. K. Yoshida, K. Maeda, and Y. Sugiyama Prediction of the degree of transporter-mediated drug-drug interactions involving OATP substrates based on in vitro inhibition studies Clin. Pharmacol. Ther. 91 6 2012 1053 1064
38. L. Zhang, Y.D. Zhang, J.M. Strong, K.S. Reynolds, and S.M. Huang A regulatory viewpoint on transporter-based drug interactions Xenobiotica 38 7-8 2008 709 724
39. P. Zhao, L. Zhang, J.A. Grillo, Q. Liu, J.M. Bullock, Y.J. Moon, P. Song, S.S. Brar, R. Madabushi, T.C. Wu, B.P. Booth, N.A. Rahman, K.S. Reynolds, E. Gil Berglund, L.J. Lesko, and S.M. Huang Applications of physiologically based pharmacokinetic (PBPK) modeling and simulation during regulatory review Clin. Pharmacol. Ther. 89 2 2011 259 267