메뉴 건너뛰기




Volumn 39, Issue 9, 2011, Pages 1658-1667

In vitro characterization of the metabolic pathways and cytochrome P450 inhibition and induction potential of BMS-690514, an ErbB/vascular endothelial growth factor receptor inhibitor

Author keywords

[No Author keywords available]

Indexed keywords

1 AMINOBENZOTRIAZOLE; 4 AMINO 1 [[4 [(3 METHOXYPHENYL)AMINO]PYRROLO[2,1 F][1,2,4]TRIAZIN 5 YL]METHYL] 3 PIPERIDINOL; BMS 690514; CYTOCHROME P450; CYTOCHROME P450 1A1; CYTOCHROME P450 1A2; CYTOCHROME P450 2A6; CYTOCHROME P450 2B6; CYTOCHROME P450 2C19; CYTOCHROME P450 2C8; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; DIETHYLDITHIOCARBAMIC ACID; DRUG METABOLITE; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR KINASE INHIBITOR; GLUCURONOSYLTRANSFERASE; GLUCURONOSYLTRANSFERASE 1A1; GLUCURONOSYLTRANSFERASE 2B4; GLUCURONOSYLTRANSFERASE 2B7; KETOCONAZOLE; MONTELUKAST; ORPHENADRINE; QUINIDINE; SULFAPHENAZOLE; TRANYLCYPROMINE; TROLEANDOMYCIN; UNCLASSIFIED DRUG; VASCULOTROPIN; VASCULOTROPIN INHIBITOR;

EID: 80051967794     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.111.039776     Document Type: Article
Times cited : (11)

References (29)
  • 1
    • 59349096968 scopus 로고    scopus 로고
    • Phase I multicenter trial of BMS-690514: Safety, pharmacokinetic profile, biological effects, and early clinical evaluation in patients with advanced solid tumors and non-small cell lung cancer
    • abstr 2564
    • Bahleda R., Felip E., Herbst R.S., Hanna N.H., Laurie S.A., Shepherd F.A., Armand J.P., Sweeney C.J., Calvo-Aller E, and Soria J.C. (2008) Phase I multicenter trial of BMS-690514: safety, pharmacokinetic profile, biological effects, and early clinical evaluation in patients with advanced solid tumors and non-small cell lung cancer. J Clin Oncol 26 (15 Suppl):abstr 2564.
    • (2008) J Clin Oncol , vol.26 , Issue.15 SUPPL.
    • Bahleda, R.1    Felip, E.2    Herbst, R.S.3    Hanna, N.H.4    Laurie, S.A.5    Shepherd, F.A.6    Armand, J.P.7    Sweeney, C.J.8    Calvo-Aller, E.9    Soria, J.C.10
  • 2
    • 75449088707 scopus 로고    scopus 로고
    • Tumor regression and pharmacodynamic (PD) biomarker validation in non-small cell lung cancer (NSCLC) patients treated with the ErbB/VEGFR inhibitor BMS-690514
    • abstr 8098
    • Bahleda R., Soria J., Harbison C., Park J., E. Felip, Hanna N., Laurie S.A., Armand J., Shepherd FA, and Herbst R. (2009) Tumor regression and pharmacodynamic (PD) biomarker validation in non-small cell lung cancer (NSCLC) patients treated with the ErbB/VEGFR inhibitor BMS-690514. J Clin Oncol 27 (15 Suppl):abstr 8098.
    • (2009) J Clin Oncol , vol.27 , Issue.15 SUPPL.
    • Bahleda, R.1    Soria, J.2    Harbison, C.3    Park, J.4    Felip, E.5    Hanna, N.6    Laurie, S.A.7    Armand, J.8    Shepherd, F.A.9    Herbst, R.10
  • 3
    • 33846967445 scopus 로고    scopus 로고
    • Substrate specificity of the human UDP- Glucuronosyltransferase UGT2B4 and UGT2B7. Identification of a critical aromatic amino acid residue at position 33
    • Barre L., Fournel-Gigleux S., Finel M., Netter P., Magdalou J, and Ouzzine M. (2007) Substrate specificity of the human UDP- Glucuronosyltransferase UGT2B4 and UGT2B7. Identification of a critical aromatic amino acid residue at position 33. FEBS J 274:1256-1264.
    • (2007) FEBS J , vol.274 , pp. 1256-1264
    • Barre, L.1    Fournel-Gigleux, S.2    Finel, M.3    Netter, P.4    Magdalou, J.5    Ouzzine, M.6
  • 6
    • 30144436526 scopus 로고    scopus 로고
    • Isoform- Selective probe substrates for in vitro studies of human UDPglucuronosyltransferases
    • Court M.H. (2005) Isoform- Selective probe substrates for in vitro studies of human UDPglucuronosyltransferases. Methods Enzymol 400:104-116.
    • (2005) Methods Enzymol , vol.400 , pp. 104-116
    • Court, M.H.1
  • 7
    • 78651512226 scopus 로고    scopus 로고
    • Mechanistic studies on a P450- Mediated rearrangement of BMS- Mediated rearrangement of BMS690514: Conversion of a pyrrolotriazine to a hydroxypyridotriazine
    • Hong H., Caceres-Cortes J., Su H., Huang X., Roongta V., Bonacorsi S. Jr, Hong Y., Tian Y., Iyer R.A., Humphreys W.G., et al. (2011) Mechanistic studies on a P450- Mediated rearrangement of BMS- Mediated rearrangement of BMS690514: conversion of a pyrrolotriazine to a hydroxypyridotriazine. Chem Res Toxicol 24:125-134.
    • (2011) Chem Res Toxicol , vol.24 , pp. 125-134
    • Hong, H.1    Caceres-Cortes, J.2    Su, H.3    Huang, X.4    Roongta, V.5    Bonacorsi Jr., S.6    Hong, Y.7    Tian, Y.8    Iyer, R.A.9    Humphreys, W.G.10
  • 9
    • 80051984319 scopus 로고    scopus 로고
    • Reaction phenotyping
    • Zhang D, Zhu M, and Humphreys GW eds John Wiley & Sons, Inc., Hoboken, NJ
    • Hurst S., Williams JA, and Hansel S. (2007) Reaction phenotyping, in Drug Metabolism in Drug Design and Development (Zhang D, Zhu M, and Humphreys GW eds) pp 477-510, John Wiley & Sons, Inc., Hoboken, NJ.
    • (2007) Drug Metabolism in Drug Design and Development , pp. 477-510
    • Hurst, S.1    Williams, J.A.2    Hansel, S.3
  • 10
    • 15244342411 scopus 로고    scopus 로고
    • UDP- Glucuronosyltransferases and clinical drug- Glucuronosyltransferases and clinical drugDrug interactions
    • Kiang T.K., Ensom MH, and Chang T.K. (2005) UDP- Glucuronosyltransferases and clinical drug- Glucuronosyltransferases and clinical drugDrug interactions. Pharmacol Ther 106:97-132.
    • (2005) Pharmacol Ther , vol.106 , pp. 97-132
    • Kiang, T.K.1    Ensom, M.H.2    Chang, T.K.3
  • 11
    • 0038685671 scopus 로고    scopus 로고
    • Validation of serotonin (5-hydroxtryptamine) as an in vitro substrate probe for human UDP-glucuronosyltransferase (UGT) 1A6
    • DOI 10.1124/dmd.31.1.133
    • Krishnaswamy S., Duan S.X., Von Moltke L.L., Greenblatt DJ, and Court M.H. (2003) Validation of serotonin (5- Hydroxtryptamine) as an in vitro substrate probe for human UDP- Hydroxtryptamine) as an in vitro substrate probe for human UDPGlucuronosyltransferase (UGT) 1A6. Drug Metab Dispos 31:133-139. (Pubitemid 36735267)
    • (2003) Drug Metabolism and Disposition , vol.31 , Issue.1 , pp. 133-139
    • Krishnaswamy, S.1    Duan, S.X.2    Von Moltke, L.L.3    Greenblatt, D.J.4    Court, M.H.5
  • 12
    • 77953801115 scopus 로고    scopus 로고
    • Preclinical pharmacokinetics and in vitro metabolism of BMS- 690514, a potent inhibitor of EGFR and VEGFR2
    • Marathe P., Tang Y., Sleczka B., Rodrigues D., Gavai A., Wong T., Christopher L, and Zhang H. (2010) Preclinical pharmacokinetics and in vitro metabolism of BMS- 690514, a potent inhibitor of EGFR and VEGFR2. J Pharm Sci 99:3579-3593.
    • (2010) J Pharm Sci , vol.99 , pp. 3579-3593
    • Marathe, P.1    Tang, Y.2    Sleczka, B.3    Rodrigues, D.4    Gavai, A.5    Wong, T.6    Christopher, L.7    Zhang, H.8
  • 13
    • 70349100116 scopus 로고    scopus 로고
    • An in vitro evaluation of the victim and perpetrator potential of the anticancer agent laromustine (VNP40101M), based on reaction phenotyping and inhibition and induction of cytochrome P450 enzymes
    • Nassar A.E., King I., Paris B.L., Haupt L., Ndikum-Moffor F., Campbell R., Usuki E., Skibbe J., Brobst D., Ogilvie B.W., et al. (2009) An in vitro evaluation of the victim and perpetrator potential of the anticancer agent laromustine (VNP40101M), based on reaction phenotyping and inhibition and induction of cytochrome P450 enzymes. Drug Metab Dispos 37:1922-1930.
    • (2009) Drug Metab Dispos , vol.37 , pp. 1922-1930
    • Nassar, A.E.1    King, I.2    Paris, B.L.3    Haupt, L.4    Ndikum-Moffor, F.5    Campbell, R.6    Usuki, E.7    Skibbe, J.8    Brobst, D.9    Ogilvie, B.W.10
  • 14
    • 85146106485 scopus 로고    scopus 로고
    • In vitro approaches for studying the inhibition of drug- Metabolizing enzymes and identifying the drug- Metabolizing enzymes and identifying the drugMetabolizing enzymes responsible for the metabolism of drugs (reaction phenotyping) with emphasis on cytochrome P450
    • Rodrigues AD ed Informa Healthcare, New York
    • Ogilvie B.W., Usuki E., Yerino P, and Parkinson A. (2008) In vitro approaches for studying the inhibition of drug- Metabolizing enzymes and identifying the drug- Metabolizing enzymes and identifying the drugMetabolizing enzymes responsible for the metabolism of drugs (reaction phenotyping) with emphasis on cytochrome P450, in Drug-Drug Interactions: Drugs and Pharmaceutical Sciences (Rodrigues AD ed) pp 231-358, Informa Healthcare, New York.
    • (2008) Drug-Drug Interactions: Drugs and Pharmaceutical Sciences , pp. 231-358
    • Ogilvie, B.W.1    Usuki, E.2    Yerino, P.3    Parkinson, A.4
  • 15
    • 84881323217 scopus 로고    scopus 로고
    • Conjugative metabolism of drugs
    • Zhang D, Zhu M, and Humphreys WG eds John Wiley & Sons, Inc., Hoboken, NJ
    • Remmel R., Nagar S, and Argikar U. (2007) Conjugative metabolism of drugs, in Drug Metabolism in Drug Design and Development (Zhang D, Zhu M, and Humphreys WG eds) pp 37-88, John Wiley & Sons, Inc., Hoboken, NJ.
    • (2007) Drug Metabolism in Drug Design and Development , pp. 37-88
    • Remmel, R.1    Nagar, S.2    Argikar, U.3
  • 16
    • 0033105118 scopus 로고    scopus 로고
    • Integrated cytochrome P450 reaction phenotyping: Attempting to bridge the gap between cDNA- Expressed cytochromes P450 and native human liver microsomes
    • Rodrigues A.D. (1999) Integrated cytochrome P450 reaction phenotyping: attempting to bridge the gap between cDNA- Expressed cytochromes P450 and native human liver microsomes. Biochem Pharmacol 57:465-480.
    • (1999) Biochem Pharmacol , vol.57 , pp. 465-480
    • Rodrigues, A.D.1
  • 18
    • 0034013033 scopus 로고    scopus 로고
    • Assessment of specificity of eight chemical inhibitors using cDNA-expressed cytochromes P450
    • Sai Y., Dai R., Yang T.J., Krausz K.W., Gonzalez F.J., Gelboin HV, and Shou M. (2000) Assessment of specificity of eight chemical inhibitors using cDNA- Expressed cytochromes P450. Xenobiotica 30:327-343. (Pubitemid 30251243)
    • (2000) Xenobiotica , vol.30 , Issue.4 , pp. 327-343
    • Sai, Y.1    Dai, R.2    Yang, T.J.3    Krausz, K.W.4    Gonzalez, F.J.5    Gelboin, H.V.6    Shou, M.7
  • 19
    • 53849093733 scopus 로고    scopus 로고
    • Current industrial practices in assessing CYP450 enzyme induction: Preclinical and clinical
    • Sinz M., Wallace G, and Sahi J. (2008) Current industrial practices in assessing CYP450 enzyme induction: Preclinical and clinical. Aaps J 10:391-400.
    • (2008) Aaps J , vol.10 , pp. 391-400
    • Sinz, M.1    Wallace, G.2    Sahi, J.3
  • 20
    • 34147130694 scopus 로고    scopus 로고
    • The role of VEGF and EGFR inhibition: Implications for combining anti- VEGF and anti- VEGF and antiEGFR agents
    • Tabernero J. (2007) The role of VEGF and EGFR inhibition: implications for combining anti- VEGF and anti- VEGF and antiEGFR agents. Mol Cancer Res 5:203-220.
    • (2007) Mol Cancer Res , vol.5 , pp. 203-220
    • Tabernero, J.1
  • 21
    • 51149086367 scopus 로고    scopus 로고
    • Combined targeting of EGFR- Dependent and VEGF- Dependent and VEGFDependent pathways: Rationale, preclinical studies and clinical applications
    • Tortora G., Ciardiello F, and Gasparini G. (2008) Combined targeting of EGFR- Dependent and VEGF- Dependent and VEGFDependent pathways: rationale, preclinical studies and clinical applications. Nat Clin Pract Oncol 5:521-530.
    • (2008) Nat Clin Pract Oncol , vol.5 , pp. 521-530
    • Tortora, G.1    Ciardiello, F.2    Gasparini, G.3
  • 22
    • 33344473930 scopus 로고    scopus 로고
    • Selectivity of substrate (trifluoperazine) and inhibitor (amitriptyline, androsterone, canrenoic acid, hecogenin, phenylbutazone, quinidine, quinine, and sulfinpyrazone) "probes" for human UDPglucuronosyltransferases
    • Uchaipichat V., Mackenzie P.I., Elliot DJ, and Miners J.O. (2006a) Selectivity of substrate (trifluoperazine) and inhibitor (amitriptyline, androsterone, canrenoic acid, hecogenin, phenylbutazone, quinidine, quinine, and sulfinpyrazone) "probes" for human UDPglucuronosyltransferases. Drug Metab Dispos 34:449-456.
    • (2006) Drug Metab Dispos , vol.34 , pp. 449-456
    • Uchaipichat, V.1    Mackenzie, P.I.2    Elliot, D.J.3    Miners, J.O.4
  • 23
    • 33344478229 scopus 로고    scopus 로고
    • Quantitative prediction of in vivo inhibitory interactions involving glucuronidated drugs from in vitro data: The effect of fluconazole on zidovudine glucuronidation
    • Uchaipichat V., Winner L.K., Mackenzie P.I., Elliot D.J., Williams JA, and Miners J.O. (2006b) Quantitative prediction of in vivo inhibitory interactions involving glucuronidated drugs from in vitro data: The effect of fluconazole on zidovudine glucuronidation. Br J Clin Pharmacol 61:427-439.
    • (2006) Br J Clin Pharmacol , vol.61 , pp. 427-439
    • Uchaipichat, V.1    Winner, L.K.2    Mackenzie, P.I.3    Elliot, D.J.4    Williams, J.A.5    Miners, J.O.6
  • 24
    • 0346099111 scopus 로고    scopus 로고
    • Role of Orphan Nuclear Receptors in the Regulation of Drug-Metabolising Enzymes
    • DOI 10.2165/00003088-200342150-00003
    • Wang H and LeCluyse E.L. (2003) Role of orphan nuclear receptors in the regulation of drug- Metabolising enzymes. Clin Pharmacokinet 42:1331-1357. (Pubitemid 38045840)
    • (2003) Clinical Pharmacokinetics , vol.42 , Issue.15 , pp. 1331-1357
    • Wang, H.1    LeCluyse, E.L.2
  • 25
    • 0025646324 scopus 로고
    • The isoenzyme pattern of cytochrome P450 in rat hepatocytes in primary culture, comparing different enzyme activities in microsomal incubations and in intact monolayers
    • Wortelboer H.M., De Kruif C.A., Van Iersel A.A., Falke H.E., Noordhoek J, and Blaauboer B.J. (1990) The isoenzyme pattern of cytochrome P450 in rat hepatocytes in primary culture, comparing different enzyme activities in microsomal incubations and in intact monolayers. Biochem Pharmacol 40:2525-2534.
    • (1990) Biochem Pharmacol , vol.40 , pp. 2525-2534
    • Wortelboer, H.M.1    De Kruif, C.A.2    Van Iersel, A.A.3    Falke, H.E.4    Noordhoek, J.5    Blaauboer, B.J.6
  • 27
    • 34047252007 scopus 로고    scopus 로고
    • Development and full validation of six inhibition assays for five major cytochrome P450 enzymes in human liver microsomes using an automated 96-well microplate incubation format and LC-MS/MS analysis
    • DOI 10.1016/j.jpba.2007.02.034, PII S0731708507001471
    • Yao M., Zhu M., Sinz M.W., Zhang H., Humphreys W.G., Rodrigues AD, and Dai R. (2007) Development and full validation of six inhibition assays for five major cytochrome P450 enzymes in human liver microsomes using an automated 96- Well microplate incubation format and LC- Well microplate incubation format and LCMS/MS analysis. J Pharm Biomed Anal 44:211-223. (Pubitemid 46551606)
    • (2007) Journal of Pharmaceutical and Biomedical Analysis , vol.44 , Issue.1 , pp. 211-223
    • Yao, M.1    Zhu, M.2    Sinz, M.W.3    Zhang, H.4    Humphreys, W.G.5    Rodrigues, A.D.6    Dai, R.7
  • 28
    • 2042474751 scopus 로고    scopus 로고
    • Amide N-glucuronidation of maxipost catalyzed by UDP- glucuronosyltransferase 2B7 in humans
    • DOI 10.1124/dmd.32.5.545
    • Zhang D., Zhao W., Roongta V.A., Mitroka J.G., Klunk LJ, and Zhu M. (2004) Amide N- Glucuronidation of MaxiPost catalyzed by UDP- Glucuronidation of MaxiPost catalyzed by UDPGlucuronosyltransferase 2B7 in humans. Drug Metab Dispos 32:545-551. (Pubitemid 38535033)
    • (2004) Drug Metabolism and Disposition , vol.32 , Issue.5 , pp. 545-551
    • Zhang, D.1    Zhao, W.2    Roongta, V.A.3    Mitroka, J.G.4    Klunk, L.J.5    Zhu, M.6
  • 29
    • 79955471895 scopus 로고    scopus 로고
    • Metabolism- Mediated drug- Mediated drugDrug interactions
    • Zhang D, Zhu M, and Humphreys WG eds John Willey & Sons, Inc., Hoboken, NJ
    • Zhang H., Sinz MW, and Rodrigues A.D. (2007) Metabolism- Mediated drug- Mediated drugDrug interactions, in Drug Metabolism in Drug Design and Development (Zhang D, Zhu M, and Humphreys WG eds) pp 113-136, John Willey & Sons, Inc., Hoboken, NJ.
    • (2007) Drug Metabolism in Drug Design and Development , pp. 113-136
    • Zhang, H.1    Sinz, M.W.2    Rodrigues, A.D.3


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.