메뉴 건너뛰기




Volumn 38, Issue 7, 2010, Pages 1147-1158

Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data

Author keywords

[No Author keywords available]

Indexed keywords

ALFENTANIL; ATORVASTATIN; BUSPIRONE; CISAPRIDE; CYCLOSPORIN; FELODIPINE; INDINAVIR; METHADONE; METOPROLOL; MEVINOLIN; MIDAZOLAM; MULTIDRUG RESISTANCE PROTEIN 1; NADOLOL; NIFEDIPINE; NISOLDIPINE; NITRENDIPINE; REPAGLINIDE; RIFABUTIN; SAQUINAVIR; SILDENAFIL; SIMVASTATIN; TACROLIMUS; TALINOLOL; TERFENADINE; TRAZODONE; VERAPAMIL; ZOLPIDEM; CYP3A PROTEIN, HUMAN; CYTOCHROME P450 3A; DRUG;

EID: 77953737073     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.110.032649     Document Type: Article
Times cited : (265)

References (49)
  • 1
    • 67049114269 scopus 로고    scopus 로고
    • Methodology for development of a physiological model incorporating CYP3A and P-glycoprotein for the prediction of intestinal drug absorption
    • Badhan R, Penny J, Galetin A, and Houston JB (2009) Methodology for development of a physiological model incorporating CYP3A and P-glycoprotein for the prediction of intestinal drug absorption. J Pharm Sci 98:2180-2197.
    • (2009) J Pharm Sci , vol.98 , pp. 2180-2197
    • Badhan, R.1    Penny, J.2    Galetin, A.3    Houston, J.B.4
  • 2
    • 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
    • 84930274769 scopus 로고    scopus 로고
    • Hepatology 35:1550-1551.
    • Hepatology , vol.35 , pp. 1550-1551
  • 5
    • 0030908131 scopus 로고    scopus 로고
    • Hepatic and intestinal metabolism of indinavir, an HIV protease inhibitor, in rat and human microsomes. Major role of CYP3A
    • Chiba M, Hensleigh M, and Lin JH (1997) Hepatic and intestinal metabolism of indinavir, an HIV protease inhibitor, in rat and human microsomes. Major role of CYP3A. Biochem Pharmacol 53:1187-1195.
    • (1997) Biochem Pharmacol , vol.53 , pp. 1187-1195
    • Chiba, M.1    Hensleigh, M.2    Lin, J.H.3
  • 6
    • 0030852009 scopus 로고    scopus 로고
    • Differential inhibition of cytochrome P450 isoforms by the protease inhibitors, ritonavir, saquinavir and indinavir
    • Eagling VA, Back DJ, and Barry MG (1997) Differential inhibition of cytochrome P450 isoforms by the protease inhibitors, ritonavir, saquinavir and indinavir. Br J Clin Pharmacol 44:190-194.
    • (1997) Br J Clin Pharmacol , vol.44 , pp. 190-194
    • Eagling, V.A.1    Back, D.J.2    Barry, M.G.3
  • 7
    • 13244299150 scopus 로고    scopus 로고
    • Mechanism-based inactivation of CYP3A by HIV protease inhibitors
    • Ernest CS 2nd, Hall SD, and Jones DR (2005) Mechanism-based inactivation of CYP3A by HIV protease inhibitors. J Pharmacol Exp Ther 312:583-591.
    • (2005) J Pharmacol Exp Ther , vol.312 , pp. 583-591
    • Ernest II, C.S.1    Hall, S.D.2    Jones, D.R.3
  • 8
    • 47949115175 scopus 로고    scopus 로고
    • A combined model for predicting CYP3A4 clinical net drug-drug interaction based on CYP3A4 inhibition, inactivation, and induction determined in vitro
    • Fahmi OA, Maurer TS, Kish M, Cardenas E, Boldt S, and Nettleton D (2008) A combined model for predicting CYP3A4 clinical net drug-drug interaction based on CYP3A4 inhibition, inactivation, and induction determined in vitro. Drug Metab Dispos 36:1698-1708.
    • (2008) Drug Metab Dispos , vol.36 , pp. 1698-1708
    • Fahmi, O.A.1    Maurer, T.S.2    Kish, M.3    Cardenas, E.4    Boldt, S.5    Nettleton, D.6
  • 10
    • 9444270510 scopus 로고    scopus 로고
    • Utility of recombinant enzyme kinetics in prediction of human clearance: Impact of variability, CYP3A5, and CYP2C19 on CYP3A4 probe substrates
    • Galetin A, Brown C, Hallifax D, Ito K, and Houston JB (2004) Utility of recombinant enzyme kinetics in prediction of human clearance: impact of variability, CYP3A5, and CYP2C19 on CYP3A4 probe substrates. Drug Metab Dispos 32:1411-1420.
    • (2004) Drug Metab Dispos , vol.32 , pp. 1411-1420
    • Galetin, A.1    Brown, C.2    Hallifax, D.3    Ito, K.4    Houston, J.B.5
  • 11
    • 0042357511 scopus 로고    scopus 로고
    • Multisite kinetic analysis of interactions between prototypical CYP3A4 subgroup substrates: Midazolam, testosterone, and nifedipine
    • Galetin A, Clarke SE, and Houston JB (2003) Multisite kinetic analysis of interactions between prototypical CYP3A4 subgroup substrates: midazolam, testosterone, and nifedipine. Drug Metab Dispos 31:1108-1116.
    • (2003) Drug Metab Dispos , vol.31 , pp. 1108-1116
    • Galetin, A.1    Clarke, S.E.2    Houston, J.B.3
  • 12
    • 49649116162 scopus 로고    scopus 로고
    • Potential role of intestinal first-pass metabolism in the prediction of drug-drug interactions
    • Galetin A, Gertz M, and Houston JB (2008) Potential role of intestinal first-pass metabolism in the prediction of drug-drug interactions. Expert Opin Drug Metab Toxicol 4:909-922.
    • (2008) Expert Opin Drug Metab Toxicol , vol.4 , pp. 909-922
    • Galetin, A.1    Gertz, M.2    Houston, J.B.3
  • 13
    • 77949281429 scopus 로고    scopus 로고
    • Contribution of intestinal cytochrome p450-mediated metabolism to drug-drug inhibition and induction interactions
    • Galetin A, Gertz M, and Houston JB (2010) Contribution of intestinal cytochrome p450-mediated metabolism to drug-drug inhibition and induction interactions. Drug Metab Pharmacokinet 25:28-47.
    • (2010) Drug Metab Pharmacokinet , vol.25 , pp. 28-47
    • Galetin, A.1    Gertz, M.2    Houston, J.B.3
  • 14
    • 33747599176 scopus 로고    scopus 로고
    • Intestinal and hepatic metabolic activity of five cytochrome P450 enzymes: Impact on prediction of first-pass metabolism
    • Galetin A and Houston JB (2006) Intestinal and hepatic metabolic activity of five cytochrome P450 enzymes: impact on prediction of first-pass metabolism. J Pharmacol Exp Ther 318: 1220-1229.
    • (2006) J Pharmacol Exp Ther , vol.318 , pp. 1220-1229
    • Galetin, A.1    Houston, J.B.2
  • 15
    • 58149347476 scopus 로고    scopus 로고
    • Grapefruit juice-drug interaction studies as a method to assess the extent of intestinal availability: Utility and limitations
    • Gertz M, Davis JD, Harrison A, Houston JB, and Galetin A (2008a) Grapefruit juice-drug interaction studies as a method to assess the extent of intestinal availability: utility and limitations. Curr Drug Metab 9:785-795.
    • (2008) Curr Drug Metab , vol.9 , pp. 785-795
    • Gertz, M.1    Davis, J.D.2    Harrison, A.3    Houston, J.B.4    Galetin, A.5
  • 16
    • 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 (2008b) 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
  • 19
    • 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
  • 20
    • 16244396867 scopus 로고    scopus 로고
    • Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin
    • DOI 10.1023/B:PHAM.0000041466.84653.8c
    • Hochman JH, Pudvah N, Qiu J, Yamazaki M, Tang C, Lin JH, and Prueksaritanont T (2004) Interactions of human P-glycoprotein with simvastatin, simvastatin acid, and atorvastatin. Pharm Res 21:1686-1691. (Pubitemid 41184401)
    • (2004) Pharmaceutical Research , vol.21 , Issue.9 , pp. 1686-1691
    • Hochman, J.H.1    Pudvah, N.2    Qiu, J.3    Yamazaki, M.4    Tang, C.5    Lin, J.H.6    Prueksaritanont, T.7
  • 22
    • 17644381224 scopus 로고    scopus 로고
    • Prediction of human drug clearance from in vitro and preclinical data using physiologically based and empirical approaches
    • 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.
    • (2005) Pharm Res , vol.22 , pp. 103-112
    • Ito, K.1    Houston, J.B.2
  • 23
    • 0033007704 scopus 로고    scopus 로고
    • Effects of intestinal CYP3A4 and P-glycoprotein on oral drug absorption - Theoretical approach
    • Ito K, Kusuhara H, and Sugiyama Y (1999) Effects of intestinal CYP3A4 and P-glycoprotein on oral drug absorption-theoretical approach. Pharm Res 16:225-231. (Pubitemid 29135126)
    • (1999) Pharmaceutical Research , vol.16 , Issue.2 , pp. 225-231
    • Ito, K.1    Kusuhara, H.2    Sugiyama, Y.3
  • 26
    • 0031790709 scopus 로고    scopus 로고
    • Metabolism of the human immunodeficiency virus protease inhibitors indinavir and ritonavir by human intestinal microsomes and expressed cytochrome P4503A4/3A5: Mechanism-based inactivation of cytochrome P4503A by ritonavir
    • Koudriakova T, Iatsimirskaia E, Utkin I, Gangl E, Vouros P, Storozhuk E, Orza D, Marinina J, and Gerber N (1998) Metabolism of the human immunodeficiency virus protease inhibitors indinavir and ritonavir by human intestinal microsomes and expressed cytochrome P4503A4/3A5: mechanism-based inactivation of cytochrome P4503A by ritonavir. Drug Metab Dispos 26:552-561.
    • (1998) Drug Metab Dispos , vol.26 , pp. 552-561
    • Koudriakova, T.1    Iatsimirskaia, E.2    Utkin, I.3    Gangl, E.4    Vouros, P.5    Storozhuk, E.6    Orza, D.7    Marinina, J.8    Gerber, N.9
  • 27
    • 35649009910 scopus 로고    scopus 로고
    • Intestinal permeability and its relevance for absorption and elimination
    • Lennernäs H (2007) Intestinal permeability and its relevance for absorption and elimination. Xenobiotica 37:1015-1051.
    • (2007) Xenobiotica , vol.37 , pp. 1015-1051
    • Lennernäs, H.1
  • 28
    • 0033009998 scopus 로고    scopus 로고
    • Is the role of the small intestine in first-pass metabolism overemphasized?
    • Lin JH, Chiba M, and Baillie TA (1999) Is the role of the small intestine in first-pass metabolism overemphasized? Pharmacol Rev 51:135-158.
    • (1999) Pharmacol Rev , vol.51 , pp. 135-158
    • Lin, J.H.1    Chiba, M.2    Baillie, T.A.3
  • 30
    • 0032733974 scopus 로고    scopus 로고
    • 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
    • Obach RS (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 27:1350-1359.
    • (1999) Drug Metab Dispos , vol.27 , pp. 1350-1359
    • Obach, R.S.1
  • 33
    • 0017603437 scopus 로고
    • Hepatic clearance of drugs. I. Theoretical considerations of a "well-stirred" model and a "parallel tube" model. Influence of hepatic blood flow, plasma and blood cell binding, and the hepatocellular enzymatic activity on hepatic drug clearance
    • Pang KS and Rowland M (1977) Hepatic clearance of drugs. I. Theoretical considerations of a "well-stirred" model and a "parallel tube" model. Influence of hepatic blood flow, plasma and blood cell binding, and the hepatocellular enzymatic activity on hepatic drug clearance. J Pharmacokinet Biopharm 5:625-653.
    • (1977) J Pharmacokinet Biopharm , vol.5 , pp. 625-653
    • Pang, K.S.1    Rowland, M.2
  • 35
    • 23944451585 scopus 로고    scopus 로고
    • A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes
    • Riley RJ, McGinnity DF, and Austin RP (2005) A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes. Drug Metab Dispos 33:1304-1311.
    • (2005) Drug Metab Dispos , vol.33 , pp. 1304-1311
    • Riley, R.J.1    McGinnity, D.F.2    Austin, R.P.3
  • 36
    • 0036614033 scopus 로고    scopus 로고
    • The effects of portal shunts on intestinal cytochrome P450 3A activity
    • Rostami-Hodjegan A and Tucker GT (2002) The effects of portal shunts on intestinal cytochrome P450 3A activity. Hepatology 35:1549-1550.
    • (2002) Hepatology , vol.35 , pp. 1549-1550
    • Rostami-Hodjegan, A.1    Tucker, G.T.2
  • 37
    • 13244287685 scopus 로고    scopus 로고
    • 'In silico' simulations to assess the 'in vivo' consequences of 'in vitro' metabolic drug-drug interactions
    • Rostami-Hodjegan A and Tucker G (2004) 'In silico' simulations to assess the 'in vivo' consequences of 'in vitro' metabolic drug-drug interactions. Drug Discov Today 1:441.
    • (2004) Drug Discov Today , vol.1 , pp. 441
    • Rostami-Hodjegan, A.1    Tucker, G.2
  • 38
    • 33947587274 scopus 로고    scopus 로고
    • Simulation and prediction of in vivo drug metabolism in human populations from in vitro data
    • Rostami-Hodjegan A and Tucker GT (2007) Simulation and prediction of in vivo drug metabolism in human populations from in vitro data. Nat Rev Drug Discov 6:140-148.
    • (2007) Nat Rev Drug Discov , vol.6 , pp. 140-148
    • Rostami-Hodjegan, A.1    Tucker, G.T.2
  • 39
    • 4744368269 scopus 로고    scopus 로고
    • Abundance of cytochrome P450 in human liver: A meta-analysis
    • Rowland-Yeo, Rostami-Hodjegan A, and Tucker GT (2004) Abundance of cytochrome P450 in human liver: a meta-analysis. Br J Clin Pharmacol 57:687-688.
    • (2004) Br J Clin Pharmacol , vol.57 , pp. 687-688
    • Rowland-Yeo1    Rostami-Hodjegan, A.2    Tucker, G.T.3
  • 40
    • 0019604592 scopus 로고
    • Some suggestions for measuring predictive performance
    • Sheiner LB and Beal SL (1981) Some suggestions for measuring predictive performance. J Pharmacokinet Biopharm 9:503-512.
    • (1981) J Pharmacokinet Biopharm , vol.9 , pp. 503-512
    • Sheiner, L.B.1    Beal, S.L.2
  • 41
    • 0034948386 scopus 로고    scopus 로고
    • Identification of cyclosporine A and tacrolimus glucuronidation in human liver and the gastrointestinal tract by a differentially expressed UDP-glucuronosyltransferase: UGT2B7
    • Strassburg CP, Barut A, Obermayer-Straub P, Li Q, Nguyen N, Tukey RH, and Manns MP (2001) Identification of cyclosporine A and tacrolimus glucuronidation in human liver and the gastrointestinal tract by a differentially expressed UDP-glucuronosyltransferase: UGT2B7. J Hepatol 34:865-872.
    • (2001) J Hepatol , vol.34 , pp. 865-872
    • Strassburg, C.P.1    Barut, A.2    Obermayer-Straub, P.3    Li, Q.4    Nguyen, N.5    Tukey, R.H.6    Manns, M.P.7
  • 42
    • 0036805724 scopus 로고    scopus 로고
    • Comparison of human duodenum and Caco-2 gene expression profiles for 12,000 gene sequences tags and correlation with permeability of 26 drugs
    • Sun D, Lennernas H, Welage LS, Barnett JL, Landowski CP, Foster D, Fleisher D, Lee KD, and Amidon GL (2002) Comparison of human duodenum and Caco-2 gene expression profiles for 12,000 gene sequences tags and correlation with permeability of 26 drugs. Pharm Res 19:1400-1416.
    • (2002) Pharm Res , vol.19 , pp. 1400-1416
    • Sun, D.1    Lennernas, H.2    Welage, L.S.3    Barnett, J.L.4    Landowski, C.P.5    Foster, D.6    Fleisher, D.7    Lee, K.D.8    Amidon, G.L.9
  • 43
    • 0141569640 scopus 로고    scopus 로고
    • Influence of P-glycoprotein, transfer clearances, and drug binding on intestinal metabolism in Caco-2 cell monolayers or membrane preparations: A theoretical analysis
    • Tam D, Sun H, and Pang KS (2003) Influence of P-glycoprotein, transfer clearances, and drug binding on intestinal metabolism in Caco-2 cell monolayers or membrane preparations: a theoretical analysis. Drug Metab Dispos 31:1214-1226.
    • (2003) Drug Metab Dispos , vol.31 , pp. 1214-1226
    • Tam, D.1    Sun, H.2    Pang, K.S.3
  • 45
    • 0842282550 scopus 로고    scopus 로고
    • Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites
    • Wang YH, Jones DR, and Hall SD (2004) Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites. Drug Metab Dispos 32:259-266.
    • (2004) Drug Metab Dispos , vol.32 , pp. 259-266
    • Wang, Y.H.1    Jones, D.R.2    Hall, S.D.3
  • 46
    • 0032480901 scopus 로고    scopus 로고
    • Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach
    • Winiwarter S, Bonham NM, Ax F, Hallberg A, Lennernäs H, and Karlén A (1998) Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach. J Med Chem 41:4939-4949.
    • (1998) J Med Chem , vol.41 , pp. 4939-4949
    • Winiwarter, S.1    Bonham, N.M.2    Ax, F.3    Hallberg, A.4    Lennernäs, H.5    Karlén, A.6
  • 47
    • 0034059327 scopus 로고    scopus 로고
    • Atorvastatin transport in the Caco-2 cell model: Contributions of P-glycoprotein and the proton-monocarboxylic acid co-transporter
    • Wu X, Whitfield LR, and Stewart BH (2000) Atorvastatin transport in the Caco-2 cell model: contributions of P-glycoprotein and the proton-monocarboxylic acid co-transporter. Pharm Res 17:209-215.
    • (2000) Pharm Res , vol.17 , pp. 209-215
    • Wu, X.1    Whitfield, L.R.2    Stewart, B.H.3
  • 49
    • 0032927243 scopus 로고    scopus 로고
    • Simultaneous investigation of indinavir nonlinear pharmacokinetics and bioavailability in healthy volunteers using stable isotope labeling technique: Study design and model-independent data analysis
    • Yeh KC, Stone JA, Carides AD, Rolan P, Woolf E, and Ju WD (1999) Simultaneous investigation of indinavir nonlinear pharmacokinetics and bioavailability in healthy volunteers using stable isotope labeling technique: study design and model-independent data analysis. J Pharm Sci 88:568-573.
    • (1999) J Pharm Sci , vol.88 , pp. 568-573
    • Yeh, K.C.1    Stone, J.A.2    Carides, A.D.3    Rolan, P.4    Woolf, E.5    Ju, W.D.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.