메뉴 건너뛰기




Volumn 38, Issue 6, 2010, Pages 905-916

In vitro characterization of sarizotan metabolism: Hepatic clearance, identification and characterization of metabolites, drug-metabolizing enzyme identification, and evaluation of cytochrome P450 inhibition

Author keywords

[No Author keywords available]

Indexed keywords

CYTOCHROME P450; CYTOCHROME P450 1A2; CYTOCHROME P450 2C19; CYTOCHROME P450 2C8; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; SARIZOTAN;

EID: 77952309437     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.109.029835     Document Type: Article
Times cited : (5)

References (27)
  • 1
    • 0027935778 scopus 로고
    • Diazepam metabolism by human liver microsomes is mediated by both S-mephenytoin hydroxylase and CYP3A isoforms
    • Andersson T, Miners JO, Veronese ME, and Birkett DJ (1994) Diazepam metabolism by human liver microsomes is mediated both by S-mephenytoin hydroxylase and CYP3A4 isoforms. Br J Clin Pharmacol 38:131-137. (Pubitemid 24247754)
    • (1994) British Journal of Clinical Pharmacology , vol.38 , Issue.2 , pp. 131-137
    • Andersson, T.1    Miners, J.O.2    Veronese, M.E.3    Birkett, D.J.4
  • 2
    • 0036891948 scopus 로고    scopus 로고
    • The influence of nonspecific microsomal binding on apparent intrinsic clearance, and its prediction from physicochemical properties
    • DOI 10.1124/dmd.30.12.1497
    • Austin RP, Barton P, Cockroft SL, Wenlock MC, and Riley RJ (2002) The influence of nonspecific microsomal binding on apparent intrinsic clearance, and its prediction from physicochemical properties. Drug Metab Dispos 30:1497-1503. (Pubitemid 35397059)
    • (2002) Drug Metabolism and Disposition , vol.30 , Issue.12 , pp. 1497-1503
    • Austin, R.P.1    Barton, P.2    Cockroft, S.L.3    Wenlock, M.C.4    Riley, R.J.5
  • 3
    • 33845996187 scopus 로고    scopus 로고
    • Scaling factors for the extrapolation of in vivo metabolic drug clearance from in vitro data: Reaching a consensus on values of human microsomal protein and hepatocellularity per gram of liver
    • Barter ZE, Bayliss MK, Beaune PH, Boobis AR, Carlile DJ, Edwards RJ, Houston JB, Lake BG, Lipscomb JC, Pelkonen OR, et al. (2007) Scaling factors for the extrapolation of in vivo metabolic drug clearance from in vitro data: reaching a consensus on values of human microsomal protein and hepatocellularity per gram of liver. Curr Drug Metab 8:33-45.
    • (2007) Curr Drug Metab , vol.8 , pp. 33-45
    • Barter, Z.E.1    Bayliss, M.K.2    Beaune, P.H.3    Boobis, A.R.4    Carlile, D.J.5    Edwards, R.J.6    Houston, J.B.7    Lake, B.G.8    Lipscomb, J.C.9    Pelkonen, O.R.10
  • 4
    • 13444273340 scopus 로고    scopus 로고
    • Continuous dopaminergic stimulation reduces risk of motor complications in parkinsonian primates
    • DOI 10.1016/j.expneurol.2004.11.013
    • Bibbiani F, Costantini LC, Patel R, and Chase TN (2005) Continuous dopaminergic stimulation reduces risk of motor complications in parkinsonian primates. Exp Neurol 192:73-78. (Pubitemid 40208539)
    • (2005) Experimental Neurology , vol.192 , Issue.1 , pp. 73-78
    • Bibbiani, F.1    Costantini, L.C.2    Patel, R.3    Chase, T.N.4
  • 5
    • 10744232330 scopus 로고    scopus 로고
    • The conduct of in vitro and in vivo drug-drug interaction studies: A Pharmaceutical Research and Manufacturers of America (PhRMA) perspective
    • Bjornsson TD, Callaghan JT, Einolf HJ, Fischer V, Gan L, Grimm S, Kao J, King SP, Miwa G, Ni L, et al. (2003) The conduct of in vitro and in vivo drug-drug interaction studies: a Pharmaceutical Research and Manufacturers of America (PhRMA) perspective. Drug Metab Dispos 31:815-832.
    • (2003) Drug Metab Dispos , vol.31 , pp. 815-832
    • Bjornsson, T.D.1    Callaghan, J.T.2    Einolf, H.J.3    Fischer, V.4    Gan, L.5    Grimm, S.6    Kao, J.7    King, S.P.8    Miwa, G.9    Ni, L.10
  • 6
    • 0027275566 scopus 로고
    • Physiological parameters in laboratory animals and humans
    • DOI 10.1023/A:1018943613122
    • Davies B and Morris T (1993) Physiological parameters in laboratory animals and humans. Pharm Res 10:1093-1095. (Pubitemid 23211439)
    • (1993) Pharmaceutical Research , vol.10 , Issue.7 , pp. 1093-1095
    • Davies, B.1    Morris, T.2
  • 7
    • 40849096159 scopus 로고    scopus 로고
    • Drug lipophilicity and microsomal protein concentration as determinants in the prediction of the fraction unbound in microsomal incubations
    • DOI 10.1124/dmd.107.018713
    • Gertz M, Kilford PJ, Houston JB, and Galetin A (2008) Drug lipophilicity and microsomal protein concentration as determinants in the prediction of the fraction unbound in microsomal incubations. Drug Metab Dispos 36:535-542. (Pubitemid 351397979)
    • (2008) Drug Metabolism and Disposition , vol.36 , Issue.3 , pp. 535-542
    • Gertz, M.1    Kilford, P.J.2    Houston, J.B.3    Galetin, A.4
  • 8
    • 0002636550 scopus 로고    scopus 로고
    • Xenobiotic metabolism in epithelial cell cultures
    • Shaw JA ed IRL Press, Oxford
    • Guillouzo A and Chesné C (1996) Xenobiotic metabolism in epithelial cell cultures, in Epithelial Cell Culture: A Practical Approach (Shaw JA ed) pp 67-85, IRL Press, Oxford.
    • (1996) Epithelial Cell Culture: A Practical Approach , pp. 67-85
    • Guillouzo, A.1    Chesné, C.2
  • 9
    • 33645100073 scopus 로고    scopus 로고
    • Binding of drugs to hepatic microsomes: Comment and assessment of current prediction methodology with recommendation for improvement
    • Hallifax D and Houston JB (2006) Binding of drugs to hepatic microsomes: comment and assessment of current prediction methodology with recommendation for improvement. Drug Metab Dispos 34:724-727.
    • (2006) Drug Metab Dispos , vol.34 , pp. 724-727
    • Hallifax, D.1    Houston, J.B.2
  • 10
    • 0346992330 scopus 로고    scopus 로고
    • Progress towards prediction of human pharmacokinetic parameters from in vitro technologies
    • Houston JB and Galetin A (2003) Progress towards prediction of human pharmacokinetic parameters from in vitro technologies. Drug Metab Rev 35:393-415.
    • (2003) Drug Metab Rev , vol.35 , pp. 393-415
    • Houston, J.B.1    Galetin, A.2
  • 11
    • 17644381224 scopus 로고    scopus 로고
    • Prediction of human drug clearance from in vitro and preclinical data using physiologically based and empirical approaches
    • DOI 10.1007/s11095-004-9015-1
    • Ito K and Houston JB (2005) Prediction of human drug clearance from in vitro and preclinical data using physiologically based and empirical approaches. Pharm Res 22:103-112. (Pubitemid 40558152)
    • (2005) Pharmaceutical Research , vol.22 , Issue.1 , pp. 103-112
    • Ito, K.1    Houston, J.B.2
  • 12
    • 0031723235 scopus 로고    scopus 로고
    • Prediction of pharmacokinetic alterations caused by drug-drug interactions: Metabolic interaction in the liver
    • Ito K, Iwatsubo T, Kanamitsu S, Ueda K, Suzuki H, and Sugiyama Y (1998) Prediction of pharmacokinetic alterations caused by drug-drug interactions: metabolic interaction in the liver. Pharmacol Rev 50:387-411. (Pubitemid 28477680)
    • (1998) Pharmacological Reviews , vol.50 , Issue.3 , pp. 387-411
    • Ito, K.1    Iwatsubo, T.2    Kanamitsu, S.3    Ueda, K.4    Suzuki, H.5    Sugiyama, Y.6
  • 13
    • 46449126478 scopus 로고    scopus 로고
    • Hepatocellular binding of drugs: Correction for unbound fraction in hepatocyte incubations using microsomal binding or drug lipophilicity data
    • DOI 10.1124/dmd.108.020834
    • Kilford PJ, Gertz M, Houston JB, and Galetin A (2008) Hepatocellular binding of drugs: correction for unbound fraction in hepatocyte incubations using microsomal binding or drug lipophilicity data. Drug Metab Dispos 36:1194-1197. (Pubitemid 351929330)
    • (2008) Drug Metabolism and Disposition , vol.36 , Issue.7 , pp. 1194-1197
    • Kilford, P.J.1    Gertz, M.2    Houston, J.B.3    Galetin, A.4
  • 14
    • 77952300104 scopus 로고    scopus 로고
    • The effect of erythromycin on the pharmacokinetics of sarizotan and its metabolites in healthy male volunteers
    • Abstract P01.100
    • Kovar A, Kroesser S, and Dolgos H (2006) The effect of erythromycin on the pharmacokinetics of sarizotan and its metabolites in healthy male volunteers (Abstract P01.100). Int J Neuropsychopharmacol 9 (Suppl 1):S127.
    • (2006) Int J Neuropsychopharmacol , vol.9 , Issue.SUPPL. 1
    • Kovar, A.1    Kroesser, S.2    Dolgos, H.3
  • 15
    • 77952310871 scopus 로고    scopus 로고
    • Investigation of the bioavailability of sarizotan and the pharmacokinetic effects of food
    • Abstract P01.099
    • Kroesser S, Fluck M, Wolna P, and Kovar A (2006a) Investigation of the bioavailability of sarizotan and the pharmacokinetic effects of food (Abstract P01.099). Int J Neuropsychopharmacol 9 (Suppl 1):S127.099.
    • (2006) Int J Neuropsychopharmacol , vol.9 , Issue.SUPPL. 1
    • Kroesser, S.1    Fluck, M.2    Wolna, P.3    Kovar, A.4
  • 16
    • 33645686908 scopus 로고    scopus 로고
    • Investigation of sarizotan's impact on the pharmacokinetics of probe drugs for major cytochrome P450 isoenzymes: A combined cocktail trial
    • Krösser S, Neugebauer R, Dolgos H, Fluck M, Rost KL, and Kovar A (2006b) Investigation of sarizotan's impact on the pharmacokinetics of probe drugs for major cytochrome P450 isoenzymes: a combined cocktail trial. Eur J Clin Pharmacol 62:277-284.
    • (2006) Eur J Clin Pharmacol , vol.62 , pp. 277-284
    • Krösser, S.1    Neugebauer, R.2    Dolgos, H.3    Fluck, M.4    Rost, K.L.5    Kovar, A.6
  • 18
    • 0037707638 scopus 로고    scopus 로고
    • Metabolic stability for drug discovery and development: Pharmacokinetic and biochemical challenges
    • Masimirembwa CM, Bredberg U, and Andersson TB (2003) Metabolic stability for drug discovery and development: pharmacokinetic and biochemical challenges. Clin Pharmacokinet 42:515-528. (Pubitemid 36801870)
    • (2003) Clinical Pharmacokinetics , vol.42 , Issue.6 , pp. 515-528
    • Masimirembwa, C.M.1    Bredberg, U.2    Andersson, T.B.3
  • 19
    • 0035031472 scopus 로고    scopus 로고
    • In vitro high throughput screening of compounds for favorable metabolic properties in drug discovery
    • Masimirembwa CM, Thompson R, and Andersson TB (2001) In vitro high throughput screening of compounds for favorable metabolic properties in drug discovery. Comb Chem High Throughput Screen 4:245-263.
    • (2001) Comb Chem High Throughput Screen , vol.4 , pp. 245-263
    • Masimirembwa, C.M.1    Thompson, R.2    Andersson, T.B.3
  • 20
    • 0019579579 scopus 로고
    • Autocatalytic alkylation of the cytochrome P-450 prosthetic haem group by 1-aminobenzotriazole. Isolation of an NN-bridged benzyne-protoporphyrin IX adduct
    • Ortiz de Montellano PR and Mathews JM (1981) Autocatalytic alkylation of the cytochrome P-450 prosthetic haem group by 1-aminobenzotriazole. Isolation of an NN-bridged benzyne-protoporphyrin IX adduct. Biochem J 195:761-764.
    • (1981) Biochem J , vol.195 , pp. 761-764
    • De Ortiz Montellano, P.R.1    Mathews, J.M.2
  • 21
    • 0030834058 scopus 로고    scopus 로고
    • Human cytochrome P450 enzymes: A status report summarizing their reactions, substrates, inducers, and inhibitors
    • Rendic S and Di Carlo FJ (1997) Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors. Drug Metab Rev 29:413-580.
    • (1997) Drug Metab Rev , vol.29 , pp. 413-580
    • Rendic, S.1    Di Carlo, F.J.2
  • 23
    • 0034329374 scopus 로고    scopus 로고
    • Early ADME in support of drug discovery: The role of metabolic stability studies
    • Thompson TN (2000) Early ADME in support of drug discovery: the role of metabolic stability studies. Curr Drug Metab 1:215-241.
    • (2000) Curr Drug Metab , vol.1 , pp. 215-241
    • Thompson, T.N.1
  • 25
    • 0035079928 scopus 로고    scopus 로고
    • Application of the relative activity factor approach in scaling from heterologously expressed cytochromes P450 to human liver microsomes: Studies on amitriptyline as a model substrate
    • Venkatakrishnan K, von Moltke LL, and Greenblatt DJ (2001) Application of the relative activity factor approach in scaling from heterologously expressed cytochromes P450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther 297:326-337.
    • (2001) J Pharmacol Exp Ther , vol.297 , pp. 326-337
    • Venkatakrishnan, K.1    Von Moltke, L.L.2    Greenblatt, D.J.3
  • 26
    • 0016566218 scopus 로고
    • Commentary: A physiological approach to hepatic drug clearance
    • Wilkinson GR and Shand DG (1975) Commentary: a physiological approach to hepatic drug clearance. Clin Pharmacol Ther 18:377-390.
    • (1975) Clin Pharmacol Ther , vol.18 , pp. 377-390
    • Wilkinson, G.R.1    Shand, D.G.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.