In vitro-in vivo extrapolation method to predict human renal clearance of drugs

Journal of Pharmaceutical Sciences

Volumn 103, Issue 3, 2014, Pages 994-1001

  Kunze, Annett ^a,b   Huwyler, Jörg ^b   Poller, Birk ^a   Gutmann, Heike ^a   Camenisch, Gian ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

^b UNIVERSITY OF BASEL   (Switzerland)

Author keywords

clearance prediction; drug transport; in vitro models; in vitro in vivo correlations (IVIVC); membrane transport; permeability; pharmacokinetics; renal clearance; renal reabsorption

Indexed keywords

AMANTADINE; ATENOLOL; ATORVASTATIN; CHLOROQUINE; CIMETIDINE; CREATININE; CYCLOSPORIN A; DESIPRAMINE; DIGOXIN; DRUG; FEXOFENADINE; IMIPRAMINE; KETOCONAZOLE; METFORMIN; METHOTREXATE; PRAVASTATIN; PROPRANOLOL; QUINIDINE; QUININE; TETRACYCLINE; VALSARTAN; VERAPAMIL;

ARTICLE; CONTROLLED STUDY; DRUG CLEARANCE; DRUG DISPOSITION; DRUG ELIMINATION; DRUG TRANSPORT; GLOMERULUS FILTRATION; HUMAN; HUMAN CELL; KIDNEY CLEARANCE; KIDNEY PROXIMAL TUBULE; KIDNEY TUBULE ABSORPTION; LLC PK1 CELL; SECRETION (PROCESS); ABSORPTION; ALGORITHM; ANIMAL; BIOLOGICAL MODEL; BLOOD; CELL MEMBRANE PERMEABILITY; COMPARATIVE STUDY; GLOMERULUS FILTRATION RATE; KIDNEY; KIDNEY TUBULE; LLC PK1 CELL LINE; METABOLIC CLEARANCE RATE; METABOLISM; PERMEABILITY; PHARMACOKINETICS; REPRODUCIBILITY; SWINE; TRANSPORT AT THE CELLULAR LEVEL;

ABSORPTION; ALGORITHMS; ANIMALS; BIOLOGICAL TRANSPORT; CELL MEMBRANE PERMEABILITY; GLOMERULAR FILTRATION RATE; HUMANS; KIDNEY; KIDNEY TUBULES; LLC-PK1 CELLS; METABOLIC CLEARANCE RATE; MODELS, BIOLOGICAL; PERMEABILITY; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS; REPRODUCIBILITY OF RESULTS; SWINE;

EID: 84894470435     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23851     Document Type: Article

References (26)

1. Morrissey KM, Stocker SL, Wittwer MB, Xu L, Giacomini KM,. 2013. Renal transporters in drug development. Annu Rev Pharmacol Toxicol 53: 503-529.
2. Li M, Anderson GD, Wang J,. 2006. Drug-drug interactions involving membrane transporters in the human kidney. Expert Opin Drug Metab Toxicol 2 (4): 505-532.
3. Feng B, LaPerle JL, Chang G, Varma MV,. 2010. Renal clearance in drug discovery and development: Molecular descriptors, drug transporters and disease state. Expert Opin Drug Metab Toxicol 6 (8): 939-952.
4. Masereeuw R, Russel FG,. 2001. Mechanisms and clinical implications of renal drug excretion. Drug Metab Rev 33 (3-4): 299-351.
5. Masago M, Takaai M, Sakata J, Horie A, Ito T, Ishida K, Taguchi M, Hashimoto Y,. 2010. Membrane transport mechanisms of quinidine and procainamide in renal LLC-PK1 and intestinal LS180 cells. Biol Pharm Bull 33 (8): 1407-1412.
6. Takaai M, Suzuki H, Ishida K, Tahara K, Hashimoto Y,. 2007. Pharmacokinetic analysis of transcellular transport of levofloxacin across LLC-PK1 and Caco-2 cell monolayers. Biol Pharm Bull 30 (11): 2167-2172.
7. Urakami Y, Kimura N, Okuda M, Masuda S, Katsura T, Inui K,. 2005. Transcellular transport of creatinine in renal tubular epithelial cell line LLC-PK1. Drug Metab Pharmacokinet 20 (3): 200-205.
8. Saito H, Yamamoto M, Inui K, Hori R,. 1992. Transcellular transport of organic cation across monolayers of kidney epithelial cell line LLC-PK. Am J Physiol 262 (1 Pt 1): C59-C66.
9. Kuteykin-Teplyakov K, Luna-Tortos C, Ambroziak K, Loscher W,. 2010. Differences in the expression of endogenous efflux transporters in MDR1-transfected versus wildtype cell lines affect P-glycoprotein mediated drug transport. Br J Pharmacol 160 (6): 1453-1463.
10. Takada T, Suzuki H, Sugiyama Y,. 2005. Characterization of polarized expression of point- or deletion-mutated human BCRP/ABCG2 in LLC-PK1 cells. Pharm Res 22 (3): 458-464.
11. Benet LZ, Broccatelli F, Oprea TI,. 2011. BDDCS applied to over 900 drugs. AAPS J 13 (4): 519-547.
12. Umehara K, Camenisch G,. 2012. Novel in vitro-in vivo extrapolation (IVIVE) method to predict hepatic organ clearance in rat. Pharm Res 29 (2): 603-617.
13. Camenisch G, Umehara K,. 2012. Predicting human hepatic clearance from in vitro drug metabolism and transport data: A scientific and pharmaceutical perspective for assessing drug-drug interactions. Biopharm Drug Dispos 33 (4): 179-194.
14. Brown CD, Sayer R, Windass AS, Haslam IS, De Broe ME, D'Haese PC, Verhulst A,. 2008. Characterisation of human tubular cell monolayers as a model of proximal tubular xenobiotic handling. Toxicol Appl Pharmacol 233 (3): 428-438.
15. Lote CJ,. 2012. Essential anatomy of the kidney. Principles of renal physiology, 5 ed. New York: Springer Science+Business Media. pp. 21-32.
16. Okudaira N, Sugiyama Y,. 1996. Use of an isolated perfused kidney to assess renal clearance of drugs: Information obtained in steady-state and non-steady-state experimental systems. Pharm Biotechnol 8: 211-238.
17. Fagerholm U,. 2007. Prediction of human pharmacokinetics-gastrointestinal absorption. J Pharm Pharmacol 59 (7): 905-916.
18. Kusuhara H, Sugiyama Y,. 2009. In vitro-in vivo extrapolation of transporter-mediated clearance in the liver and kidney. Drug Metab Pharmacokinet 24 (1): 37-52.
19. DeWoskin RS, Thompson CM,. 2008. Renal clearance parameters for PBPK model analysis of early lifestage differences in the disposition of environmental toxicants. Regul Toxicol Pharmacol 51 (1): 66-86.
20. Shitara Y, Sato H, Sugiyama Y,. 2005. Evaluation of drug-drug interaction in the hepatobiliary and renal transport of drugs. Annu Rev Pharmacol Toxicol 45: 689-723.
21. Obach RS, Baxter JG, Liston TE, Silber BM, Jones BC, MacIntyre F, Rance DJ, Wastall P,. 1997. The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data. J Pharmacol Exp Therapeut 283 (1): 46-58.
22. Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, Hillgren KM, Hoffmaster KA, Ishikawa T, Keppler D, Kim RB, Lee CA, Niemi M, Polli JW, Sugiyama Y, Swaan PW, Ware JA, Wright SH, Yee SW, Zamek-Gliszczynski MJ, Zhang L,. 2010. Membrane transporters in drug development. Nat Rev Drug Discov 9 (3): 215-236.
23. Hori R, Okamura M, Takayama A, Hirozane K, Takano M,. 1993. Transport of organic anion in the OK kidney epithelial cell line. Am J Physiol 264 (6 Pt 2): F975-F980.
24. Varma MV, Feng B, Obach RS, Troutman MD, Chupka J, Miller HR, El-Kattan A,. 2009. Physicochemical determinants of human renal clearance. J Med Chem 52 (15): 4844-4852.
25. Neuhoff S, Gaohua L, Howard Burt, Masoud Jamei, Linzhong Li, Geoffrey T. Tucker, Armin Rostami-Hodjeagan,. 2013. Accounting for transporters in renal clearance: Towards a mechanistic kidney model (Mech KiM). In Transporters in drug development;, Yuichi Sugiyama BS, Ed. New York: Springer Science+Business Media. pp. 155-177.
26. Watanabe T, Kusuhara H, Debori Y, Maeda K, Kondo T, Nakayama H, Horita S, Ogilvie BW, Parkinson A, Hu Z, Sugiyama Y,. 2011. Prediction of the overall renal tubular secretion and hepatic clearance of anionic drugs and a renal drug-drug interaction involving organic anion transporter 3 in humans by in vitro uptake experiments. Drug Metab Dispos 39 (6): 1031-1038.