Assessment of hepatotoxicity potential of drug candidate molecules including kinase inhibitors by hepatocyte imaging assay technology and bile flux imaging assay technology

Methods in Molecular Biology

Volumn 795, Issue , 2012, Pages 83-107

  Xu, Jinghai J ^a   Dunn, Margaret C ^b   Smith, Arthur R ^b   Tien, Eric S ^b  

^a MERCK RESEARCH LABORATORIES   (United States)

^b PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

Author keywords

Cellular imaging; Discovery toxicology; Drug safety evaluation; Hepatocellular damage; High content screening and analysis; Mechanism based drug profiling; Primary cell culture; Toxicity test; Translational toxicology

Indexed keywords

COLLAGEN; ENZYME INHIBITOR; LAMININ; MATRIGEL; PHOSPHOTRANSFERASE; PROTEOGLYCAN;

ARTICLE; BILE; BIOASSAY; CELL CULTURE; CRYOPRESERVATION; DRUG ANTAGONISM; DRUG COMBINATION; DRUG EFFECT; ENZYMOLOGY; FLUORESCENCE MICROSCOPY; HUMAN; IMAGE PROCESSING; LIVER CELL; METABOLISM; METHODOLOGY; MOLECULAR IMAGING; STAINING; TOXICITY TESTING;

BILE; BIOLOGICAL ASSAY; CELLS, CULTURED; COLLAGEN; CRYOPRESERVATION; DRUG COMBINATIONS; ENZYME INHIBITORS; HEPATOCYTES; HUMANS; IMAGE PROCESSING, COMPUTER-ASSISTED; LAMININ; MICROSCOPY, FLUORESCENCE; MOLECULAR IMAGING; PHOSPHOTRANSFERASES; PROTEOGLYCANS; STAINING AND LABELING; TOXICITY TESTS;

EID: 80555156167     PISSN: 10643745     EISSN: None     Source Type: Book Series    
DOI: 10.1007/978-1-61779-337-0_6     Document Type: Article

References (24)

1. Duan, W., and Wong, W. S. (2006) Targeting mitogen-activated protein kinases for asthma. Curr. Drug Targets 7, 691-698. (Pubitemid 43827265)
2. Wong, K. K. (2009) Recent Developments in Anti-Cancer Agents Targeting the Ras/Raf/MEK/ERK Pathway. Recent Patents Anticancer Drug Discov. 4, 28-35.
3. Schindler, J. F., Monahan, J. B., and Smith, W. G. (2007) p38 pathway kinases as antiinflammatory drug targets. J. Dent. Res. 86, 800-811.
4. Hendriks, B. S., Hua, F., and Chabot, J. R. (2008) Analysis of mechanistic pathway models in drug discovery: p38 pathway. Biotechnol. Prog. 24, 96-109. (Pubitemid 351231254)
5. Konecny, G. E., Pegram, M. D., Venkatesan, N., Finn, R., Yang, G., Rahmeh, M., Untch, M., Rusnak, D. W., Spehar, G., Mullin, R. J., Keith, B. R., Gilmer, T. M., Berger, M., Podratz, K. C., and Slamon, D. J. (2006) Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells. Cancer Res. 66, 1630-1639. (Pubitemid 43259947)
6. Moulder, S. L., Yakes, F. M., Muthuswamy, S. K., Bianco, R., Simpson, J. F., and Arteaga, C. L. (2001) Epidermal growth factor receptor (HER1) tyrosine kinase inhibitor ZD1839 (Iressa) inhibits HER2/neu (erbB2)-overexpressing breast cancer cells in vitro and in vivo. Cancer Res. 61, 8887-8895. (Pubitemid 34013905)
7. Dominguez, C., Powers, D. A., and Tamayo, N. (2005) p38 MAP kinase inhibitors: many are made, but few are chosen. Curr. Opin. Drug Discov. Devel. 8, 421-430. (Pubitemid 40921741)
8. Guo, F., Letrent, S. P., Munster, P. N., Britten, C. D., Gelmon, K., Tolcher, A. W., and Sharma, A. (2008) Pharmacokinetics of a HER2 tyrosine kinase inhibitor CP-724,714 in patients with advanced malignant HER2 positive solid tumors: correlations with clinical characteristics and safety. Cancer Chemother. Pharmacol. 62, 97-109. (Pubitemid 351537850)
9. Xu, J. J., Hendriks, B. S., Zhao, J., and de Graaf, D. (2008) Multiple effects of acetaminophen and p38 inhibitors: towards pathway toxicology. FEBS Lett. 582, 1276-1282.
10. Antoine, D. J., Williams, D. P., and Park, B. K. (2008) Understanding the role of reactive metabolites in drug-induced hepatotoxicity: state of the science. Expert Opin. Drug Metab. Toxicol. 4, 1415-1427.
11. Obach, R. S., Kalgutkar, A. S., Soglia, J. R., and Zhao, S. X. (2008) Can in vitro metabolism-dependent covalent binding data in liver microsomes distinguish hepatotoxic from nonhepatotoxic drugs? An analysis of 18 drugs with consideration of intrinsic clearance and daily dose. Chem. Res. Toxicol. 21, 1814-1822.
12. Zhao, S. X., Dalvie, D. K., Kelly, J. M., Soglia, J. R., Frederick, K. S., Smith, E. B., Obach, R. S., and Kalgutkar, A. S. (2007) NADPHdependent covalent binding of [3H]paroxetine to human liver microsomes and S-9 fractions: identification of an electrophilic quinone metabolite of paroxetine. Chem. Res. Toxicol. 20, 1649-1657. (Pubitemid 350275610)
13. Xu, J. J., Henstock, P. V., Dunn, M. C., Smith, A. R., Chabot, J. R., and de Graaf, D. (2008) Cellular imaging predictions of clinical druginduced liver injury. Toxicol. Sci. 105, 97-105.
14. Olson, H., Betton, G., Robinson, D., Thomas, K., Monro, A., Kolaja, G., Lilly, P., Sanders, J., Sipes, G., Bracken, W., Dorato, M., Van Deun, K., Smith, P., Berger, B., and Heller, A. (2000) Concordance of the toxicity of pharmaceuticals in humans and in animals. Regul. Toxicol. Pharmacol. 32, 56-67.
15. LeCluyse, E. L., Audus, K. L., and Hochman, J. H. (1994) Formation of extensive canalicular networks by rat hepatocytes cultured in collagen-sandwich configuration. Am. J. Physiol. 266, C1764-1774. (Pubitemid 24220826)
16. Liu, X., LeCluyse, E. L., Brouwer, K. R., Gan, L. S., Lemasters, J. J., Stieger, B., Meier, P. J., and Brouwer, K. L. (1999) Biliary excretion in primary rat hepatocytes cultured in a collagen-sandwich configuration. Am. J. Physiol. 277, G12-21. (Pubitemid 29352640)
17. Hariparsad, N., Carr, B. A., Evers, R., and Chu, X. (2008) Comparison of immortalized Fa2N-4 cells and human hepatocytes as in vitro models for cytochrome P450 induction. Drug Metab. Dispos. 36, 1046-1055. (Pubitemid 351717461)
18. Le Vee, M., Jigorel, E., Glaise, D., Gripon, P., Guguen-Guillouzo, C., and Fardel, O. (2006) Functional expression of sinusoidal and canalicular hepatic drug transporters in the differentiated human hepatoma HepaRG cell line. Eur. J. Pharm. Sci. 28, 109-117.
19. Munster, P. N., Britten, C. D., Mita, M., Gelmon, K., Minton, S. E., Moulder, S., Slamon, D. J., Guo, F., Letrent, S. P., Denis, L., and Tolcher, A. W. (2007) First study of the safety, tolerability, and pharmacokinetics of CP-724,714 in patients with advanced malignant solid HER2-expressing tumors. Clin. Cancer Res. 13, 1238-1245. (Pubitemid 46424065)
20. Feng, B., Xu, J. J., Bi, Y. A., Mireles, R., Davidson, R., Duignan, D. B., Campbell, S., Kostrubsky, V. E., Dunn, M. C., Smith, A. R., and Wang, H. F. (2009) Role of hepatic transporters in the disposition and hepatotoxicity of a HER2 tyrosine kinase inhibitor CP-724,714. Toxicol. Sci. 108, 492-500.
21. Bi, Y. A., Kazolias, D., and Duignan, D. B. (2006) Use of cryopreserved human hepatocytes in sandwich culture to measure hepatobiliary transport. Drug Metab. Dispos. 34, 1658-1665. (Pubitemid 44285409)
22. Kreamer, B. L., Staecker, J. L., Sawada, N., Sattler, G. L., Hsia, M. T., and Pitot, H. C. (1986) Use of a low-speed, iso-density percoll centrifugation method to increase the viability of isolated rat hepatocyte preparations. In Vitro Cell Dev. Biol. 22, 201-211. (Pubitemid 16075195)
23. Vinken, M., Henkens, T., Vanhaecke, T., Papeleu, P., Geerts, A., Van Rossen, E., Chipman, J. K., Meda, P., and Rogiers, V. (2006) Trichostatin a enhances gap junctional intercellular communication in primary cultures of adult rat hepatocytes. Toxicol. Sci. 91, 484-492. (Pubitemid 43827301)
24. Papeleu, P., Vanhaecke, T., and Rogiers, V. (2006) Histone deacetylase inhibition: A differentiation therapy for cultured primary hepatocytes? Curr. Enz. Inhib. 2, 91-104. (Pubitemid 44082966)