Prediction of hepatic plasma clearance in vivo from gel-entrapped rat and human hepatocytes

Canadian Journal of Physiology and Pharmacology

Volumn 91, Issue 2, 2013, Pages 178-186

  Yin, Jian ^a   Qiu, Hongxia ^b   Dai, Jing ^a   Lu, Yanhua ^a   Zhao, Rong ^b   Chen, Li ^b   Meng, Qin ^a  

^a ZHEJIANG UNIVERSITY   (China)

^b Roche RandD Center China Ltd   (China)

Author keywords

Gel entrapment; Hepatic plasma clearance; Human hepatocytes; Prediction; Rat hepatocytes

Indexed keywords

7 ETHOXYCOUMARIN; AMITRIPTYLINE; CIMETIDINE; CLOZAPINE; CYCLOSPORIN A; DESIPRAMINE; DEXAMETHASONE; DILTIAZEM; IBUPROFEN; IMIPRAMINE; METHOXSALEN; OMEPRAZOLE; PARACETAMOL; PREDNISONE; QUINIDINE; RIFAMPICIN; TESTOSTERONE; TOLBUTAMIDE; VERAPAMIL; WARFARIN;

ANIMAL CELL; ARTICLE; DRUG BINDING; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; LIVER CELL; MATHEMATICAL MODEL; NONHUMAN; PLASMA CLEARANCE; PRIORITY JOURNAL; RAT;

AGED; ANIMALS; CELLS, CULTURED; CULTURE MEDIA; FEMALE; GELS; HEPATOCYTES; HUMANS; MALE; METABOLIC CLEARANCE RATE; MIDDLE AGED; MODELS, BIOLOGICAL; PHARMACEUTICAL PREPARATIONS; PREDICTIVE VALUE OF TESTS; PRIMARY CELL CULTURE; RATS; SPECIES SPECIFICITY;

EID: 84874595257     PISSN: 00084212     EISSN: 12057541     Source Type: Journal    
DOI: 10.1139/cjpp-2012-0334     Document Type: Article

References (60)

1. Abe, K., Bridges, A.S., and Brouwer, K.L. 2009. Use of sandwich-cultured human hepatocytes to predict biliary clearance of angiotensin II receptor blockers and HMG-CoA reductase inhibitors. Drug Metab. Dispos. 37(3): 447-452. doi: 10.1124/dmd.108.023465. PMID:19074974.
2. Akabane, T., Gerst, N., Masters, J.N., and Tamura, K. 2012. A quantitative approach to hepatic clearance prediction of metabolism by aldehyde oxidase using custom pooled hepatocytes. Xenobiotica. doi:10.3109/00498254.2012. 670736. PMID:22448773.
3. Axelsson, H., Granhall, C., Floby, E., Jaksch, Y., Svedling, M., and Sohlenius-Sternbeck, A.K. 2003. Rates of metabolism of chlorzoxazone, dextromethorphan, 7-ethoxycoumarin, imipramine, quinidine, testosterone and verapamil by fresh and cryopreserved rat liver slices, and some comparisons with microsomes. Toxicol. In Vitro, 17(4): 481-488. doi:10.1016/S0887-2333(03)00049-3. PMID:12849732.
4. Bayliss, M.K., Bell, J.A., Jenner, W.N., and Wilson, K. 1990. Prediction of intrinsic clearance of loxtidine from kinetic studies in rat, dog and human hepatocytes. Biochem. Soc. Trans. 18(6): 1198-1199. doi:10.1042/bst0181198. PMID: 1982435.
5. Bernareggi, A., and Rowland, M. 1991. Physiologic modeling of cyclosporin kinetics in rat and man. J. Pharmacokinet. Biopharm. 19(1): 21-50. doi:10.1007/ BF01062191. PMID:2023108.
6. Bjorkman, S. 2005. Prediction of drug disposition in infants and children by means of physiologically based pharmacokinetic (PBPK) modelling: theophylline and midazolam as model drugs. Br. J. Clin. Pharmacol. 59(6): 691-704. doi:10.1111/j.1365-2125.2004.02225.x. PMID:15948934.
7. Blanchard, N., Richert, L., Notter, B., Delobel, F., David, P., Coassolo, P., et al. 2004. Impact of serum on clearance predictions obtained from suspensions and primary cultures of rat hepatocytes. Eur. J. Pharm. Sci. 23(2): 189-199. doi:10.1016/j.ejps.2004.07.007. PMID:15451007.
8. Brightman, F.A., Leahy, D.E., Searle, G.E., and Thomas, S. 2006. Application of a generic physiologically based pharmacokinetic model to the estimation of xenobiotic levels in rat plasma. Drug Metab. Dispos. 34(1): 84-93. doi:10.1124/ dmd.105.004804. PMID: 16221757.
9. Carlile, D.J., Stevens, A.J., Ashforth, E.I., Waghela, D., and Houston, J.B. 1998. In vivo clearance of ethoxycoumarin and its prediction from in vitro systems. Use of drug depletion and metabolite formation methods in hepatic microsomes and isolated hepatocytes. Drug Metab. Dispos. 26(3): 216-221. doi:10. 1124/dmd.33.1.115. PMID:9492383.
10. Chao, P., Barminko, J., Novik, E., Han, Y., Maguire, T., and Cheng, K.C. 2009. Prediction of human hepatic clearance using an in vitro plated hepatocyte clearance model. Drug Metab. Lett. 3(4): 296-307. doi:10.2174/ 187231209790218073. PMID:20041832.
11. Chiba, M., Ishii, Y., and Sugiyama, Y. 2009. Prediction of hepatic clearance in human from in vitro data for successful drug development. AAPS J. 11(2): 262-276. doi:10.1208/s12248-009-9103-6. PMID:19408130.
12. Cox, J.W., Cox, S.R., VanGiessen, G., and Ruwart, M.J. 1985. Ibuprofen stereoisomer hepatic clearance and distribution in normal and fatty in situ perfused rat liver. J. Pharmacol. Exp. Ther. 232(3): 636-643. doi:10.2174/187231209790218073. PMID:3973821.
13. Cross, D.M., and Bayliss, M.K. 2000. A commentary on the use of hepatocytes in drug metabolism studies during drug discovery and development. Drug Metab. Rev. 32(2): 219-240. doi:10.1081/DMR-100100574. PMID:10774777.
14. Davies, B., and Morris, T. 1993. Physiological parameters in laboratory animals and humans. Pharm. Res. 10(7): 1093-1095. doi:10.1023/A:1018943613122. PMID:8378254.
15. De Kanter, R., Monshouwer, M., Draaisma, A.L., De Jager, M.H., de Graaf, I.A., Proost, J.H., et al. 2004. Prediction of whole-body metabolic clearance of drugs through the combined use of slices from rat liver, lung, kidney, small intestine and colon. Xenobiotica, 34(3): 229-241. doi:10.1080/ 004982502000196758. PMID:15204696.
16. Earp, J.C., Pyszczynski, N.A., Molano, D.S., and Jusko, W.J. 2008. Pharmacokinetics of dexamethasone in a rat model of rheumatoid arthritis. Biopharm. Drug Dispos. 29(6): 366-372. doi:10.1002/bdd.626. PMID:18613033.
17. Egfjord, M., Daugaard, H., and Olgaard, K. 1990. Clearance of prednisone in isolated perfused livers of normal and uremic rats. Effects of acute and chronic cyclosporin A administration. Drug Metab. Dispos. 18(2): 231-237. PMID:1971579.
18. Eichelbaum, M., Mikus, G., and Vogelgesang, B. 1984. Pharmacokinetics of (+)-, (-)-and (+/-)-verapamil after intravenous administration. Br. J. Clin. Pharmacol. 17(4): 453-458. doi:10.1111/j.1365-2125.1984.tb02371.x. PMID:6721991.
19. Farrell, G., and Koltai, A. 1988. Hepatic testosterone metabolism in male rats with portal bypass. Gastroenterology, 95(2): 425-433. PMID:3391370.
20. Foster, J.A., Houston, J.B., and Hallifax, D. 2011. Comparison of intrinsic clearances in human liver microsomes and suspended hepatocytes from the same donor livers: clearance-dependent relationship and implications for prediction of in vivo clearance. Xenobiotica, 41(2): 124-136. doi:10.3109/00498254. 2010.530700. PMID:21058916.
21. Glew, W.B. 1979. Determination of 8-methoxypsoralen in serum, aqueous, and lens: relation to long-wave ultraviolet phototoxicity in experimental and clinical photochemotherapy. Trans. Am. Ophthalmol. Soc. 77: 464-514. PMID:397661.
22. Guo, Y., Wang, H., and Zhang, C. 2007. Establishment of rat precision-cut fibrotic liver slice technique and its application in verapamil metabolism. Clin. Exp. Pharmacol. Physiol. 34(5-6): 406-413. doi:10.1111/j.1440-1681.2007.04582.x. PMID:17439408.
23. Hanada, K., Ikemi, Y., Kukita, K., Mihara, K., and Ogata, H. 2008. Stereoselective first-pass metabolism of verapamil in the small intestine and liver in rats. Drug Metab. Dispos. 36(10): 2037-2042. doi:10.1124/dmd.107.020339. PMID: 18617604.
24. Houston, J.B. 1994. Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance. Biochem. Pharmacol. 47(9): 1469-1479. PMID:8185657.
25. Houston, J.B., and Carlile, D.J. 1997. Prediction of hepatic clearance from microsomes, hepatocytes, and liver slices. Drug Metab. Rev. 29(4): 891-922. doi:10. 3109/03602539709002237. PMID:9421679.
26. Houston, J.B., Rowland-Yeo, K., and Zanelli, U. 2012. Evaluation of the novel in vitro systems for hepatic drug clearance and assessment of their predictive utility. Toxicol. In Vitro. doi:10.1016/j.tiv.2011.12.016. PMID:22244922.
27. Ito, K., and Houston, J.B. 2004. Comparison of the use of liver models for predicting drug clearance using in vitro kinetic data from hepatic microsomes and isolated hepatocytes. Pharm. Res. 21(5): 785-792. doi:10.1023/B:PHAM. 0000026429.12114.7d. PMID:15180335.
28. Ito, K., and Houston, J.B. 2005. Prediction of human drug clearance from in vitro and preclinical data using physiologically based and empirical approaches. Pharm. Res. 22(1): 103-112. doi:10.1007/s11095-004-9015-1. PMID:15771236.
29. Ji, L., Masuda, S., Saito, H., and Inui, K. 2002. Down-regulation of rat organic cation transporter rOCT2 by 5/6 nephrectomy. Kidney Int. 62(2): 514-524. doi:10.1046/j.1523-1755.2002.00464.x. PMID:12110012.
30. Jones, H.M., and Houston, J.B. 2004. Substrate depletion approach for determining in vitro metabolic clearance: time dependencies in hepatocyte and microsomal incubations. Drug Metab. Dispos. 32(9): 973-982. doi:10.1124/dmd. 104.000125. PMID:15319339.
31. Jouin, D., Blanchard, N., Alexandre, E., Delobel, F., David-Pierson, P., Lave, T., et al. 2006. Cryopreserved human hepatocytes in suspension are a convenient high throughput tool for the prediction of metabolic clearance. Eur. J. Pharm. Biopharm. 63(3): 347-355. doi:10.1016/j.ejpb.2006.01.014. PMID: 16621491.
32. Keyler, D.E., Le Couteur, D.G., Pond, S.M., St Peter, J.V., and Pentel, P.R. 1995. Effects of specific antibody Fab fragments on desipramine pharmacokinetics in the rat in vivo and in the isolated, perfused liver. J. Pharmacol. Exp. Ther. 272(3): 1117-1123. PMID:7891324.
33. Kidambi, S., Yarmush, R.S., Novik, E., Chao, P., Yarmush, M.L., and Nahmias, Y. 2009. Oxygen-mediated enhancement of primary hepatocyte metabolism, functional polarization, gene expression, and drug clearance. Proc. Natl. Acad. Sci. U.S.A. 106(37): 15714-15719. doi:10.1073/pnas.0906820106. PMID: 19720996.
34. Lave, T., Chapman, K., Goldsmith, P., and Rowland, M. 2009. Human clearance prediction: shifting the paradigm. Expert Opin. Drug Metab. Toxicol. 5(9): 1039-1048. doi:10.1517/17425250903099649. PMID:19611405.
35. LeCluyse, E.L., Alexandre, E., Hamilton, G.A., Viollon-Abadie, C., Coon, D.J., Jolley, S., et al. 2005. Isolation and culture of primary human hepatocytes. Methods Mol. Biol. 290: 207-229. doi:10.1385/1-59259-838-2:207. PMID: 15361665.
36. Lee, D.Y., Lee, I., and Lee, M.G. 2007. Pharmacokinetics of omeprazole after intravenous and oral administration to rats with liver cirrhosis induced by dimethylnitrosamine. Int. J. Pharm. 330(1-2): 37-44. doi:10.1016/j.ijpharm. 2006.08.037. PMID:16997515.
37. Liu, X., Chism, J.P., LeCluyse, E.L., Brouwer, K.R., and Brouwer, K.L. 1999. Correlation of biliary excretion in sandwich-cultured rat hepatocytes and in vivo in rats. Drug Metab. Dispos. 27(6): 637-644. PMID:10348791.
38. Mansor, S.M., Ward, S.A., Edwards, G., Hoaksey, P.E., and Breckenridge, A.M. 1990. The effect of malaria infection on the disposition of quinine and quinidine in the rat isolated perfused liver preparation. J. Pharm. Pharmacol. 42(6): 428-432. doi:10.1111/j.2042-7158.1990.tb06584.x. PMID:1979624.
39. Mays, D.C., Hecht, S.G., Unger, S.E., Pacula, C.M., Climie, J.M., Sharp, D.E., et al. 1987. Disposition of 8-methoxypsoralen in the rat. Induction of metabolism in vivo and in vitro and identification of urinary metabolites by thermospray mass spectrometry. Drug Metab. Dispos. 15(3): 318-328. PMID:2886306.
40. McGinnity, D.F., Soars, M.G., Urbanowicz, R.A., and Riley, R.J. 2004. Evaluation of fresh and cryopreserved hepatocytes as in vitro drug metabolism tools for the prediction of metabolic clearance. Drug Metab. Dispos. 32(11): 1247-1253. doi:10.1124/dmd.104.000026. PMID:15286053.
41. Naritomi, Y., Terashita, S., Kimura, S., Suzuki, A., Kagayama, A., and Sugiyama, Y. 2001. Prediction of human hepatic clearance from in vivo animal experiments and in vitro metabolic studies with liver microsomes from animals and humans. Drug Metab. Dispos. 29(10): 1316-1324. PMID:11560875.
42. Obach, R.S. 1996. The importance of nonspecific binding in in vitro matrices, its impact on enzyme kinetic studies of drug metabolism reactions, and implications for in vitro-in vivo correlations. Drug Metab. Dispos. 24(10): 1047-1049. PMID:8894503.
43. Obach, R.S. 1999. Prediction of human clearance of twenty-nine drugs from hepatic microsomal intrinsic clearance data: An examination of in vitro half-life approach and nonspecific binding to microsomes. Drug Metab. Dispos. 27(11): 1350-1359. PMID:10534321.
44. Ohshima, N., Kotaki, H., Sawada, Y., and Iga, T. 1994. Tissue distribution and metabolism of amitriptyline after repeated administration in rats. Drug Metab. Dispos. 22(1): 21-25. PMID:8149884.
45. O'Reilly, R.A. 1972. Sodium warfarin. Pharmacology, 8(1): 181-190. PMID: 4644647.
46. Poulin, P., Kenny, J.R., Hop, C.E., and Haddad, S. 2012. In vitro-in vivo extrapolation of clearance: modeling hepatic metabolic clearance of highly bound drugs and comparative assessment with existing calculation methods. J. Pharm. Sci. 101(2): 838-851. doi:10.1002/jps.22792. PMID:22009717.
47. Qiu, H.X., Su, G.G., and Tang, X. 2006. [Tissue-like cultures of rat hepatocytes in study of phase I and phase II drug metabolism]. Zhejiang Da Xue Xue Bao Yi Xue Ban, 35(5): 541-546. PMID:17063549.
48. Rowland Yeo, K., Howgate, E.M., Tucker, G.T., and Rostami-Hodjegan, A. 2004. Predicting the clearance of CYP2C9 substrates. Drug Metab. Dispos. 32(12): 1522; author reply 1523. doi:10.1124/dmd.104.001792. PMID:15550723.
49. Shen, C., Zhang, G., Qiu, H., and Meng, Q. 2006. Acetaminophen-induced hepatotoxicity of gel-entrapped rat hepatocytes in hollow fibers. Chem. Biol. Interact. 162(1): 53-61. doi:10.1016/j.cbi.2006.05.005. PMID:16797510.
50. Shen, C., Meng, Q., and Zhang, G. 2012. Species-specific toxicity of troglitazone on rats and human by gel-entrapped hepatocytes. Toxicol. Appl. Pharmacol. 258(1): 19-25. doi:10.1016/j.taap.2011.10.020. PMID:22085495.
51. Shim, C.-K., and Lee, J.-U. 1985. Comparative study of rifarnpicin pharmacokinetics administered orally and intravenously in the fasted and non-fasted Rats. Arch. Pharm. Res. 8(3): 177-186. doi:10.1007/BF02857043.
52. Sohlenius-Sternbeck, A.K., Afzelius, L., Prusis, P., Neelissen, J., Hoogstraate, J., Johansson, J., et al. 2010. Evaluation of the human prediction of clearance from hepatocyte and microsome intrinsic clearance for 52 drug compounds. Xenobiotica, 40(9): 637-649. doi:10.3109/00498254.2010.500407. PMID: 20624033.
53. Studenberg, S.D., and Brouwer, K.L. 1991. Phenacetin and acetaminophen metabolism in the isolated perfused rat liver. Precursor concentration influences the selection of kinetic parameters to assess hypoxic impairment. Drug Metab. Dispos. 19(2): 423-429. PMID:1676648.
54. Treijtel, N., Barendregt, A., Freidig, A.P., Blaauboer, B.J. van, and Eijkeren, J.C. 2004. Modeling the in vitro intrinsic clearance of the slowly metabolized compound tolbutamide determined in sandwich-cultured rat hepatocytes. Drug Metab. Dispos. 32(8): 884-891. doi:10.1124/dmd.32.8.884. PMID: 15258115.
55. Umehara, K., and Camenisch, G. 2012. Novel in vitro-in vivo extrapolation (IVIVE) method to predict hepatic organ clearance in rat. Pharm. Res. 29(2): 603-617. doi:10.1007/s11095-011-0607-2. PMID:22011931.
56. Wattanachai, N., Tassaneeyakul, W., Rowland, A., Elliot, D.J., Bowalgaha, K., Knights, K.M., et al. 2012. Effect of albumin on human liver microsomal and recombinant CYP1A2 activities: impact on in vitro-in vivo extrapolation of drug clearance. Drug Metab. Dispos. 40(5): 982-989. doi:10.1124/dmd.111. 044057. PMID:22331994.
57. Wong, H., Lewin-Koh, S.C., Theil, F.P., and Hop, C.E. 2012. Influence of the compound selection process on the performance of human clearance prediction methods. J. Pharm. Sci. 101(2): 509-515. doi:10.1002/jps.22786. PMID: 1976152.
58. Wu, D.Q., Zhang, G.L., Shen, C., Zhao, Q., Li, H., and Meng, Q. 2005. Evaluation of diffusion in gel entrapment cell culture within hollow fibers. World J. Gastroenterol. 11(11): 1599-1604. PMID:15786534.
59. Yin, J., Meng, Q., Zhang, G., and Sun, Y. 2009. Differential methotrexate hepatotoxicity on rat hepatocytes in 2-D monolayer culture and 3-D gel entrapment culture. Chem. Biol. Interact. 180(3): 368-375. doi:10.1016/j.cbi.2009.04.004. PMID:19394316.
60. Yin, J., Meng, Q., and Dong, X. 2011. Auto-inhibition of verapamil metabolism in rat hepatocytes of gel entrapment culture. Biomed. Pharmacother. 65(5): 328-333. doi:10.1016/j.biopha.2011.04.011. PMID:21775094.