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Volumn 102, Issue 7, 2013, Pages 2085-2095

Prediction of total hepatic clearance by combining metabolism, transport, and permeability data in the in vitro-in vivo extrapolation methods: Emphasis on an apparent fraction unbound in liver for drugs

Author keywords

Hepatocytes; in vitro in vivo correlation; in vitro in vivo extrapolation; Intrinsic clearance; IVIVE; Metabolism; PBPK modeling; Permeability; Pharmacokinetics; Physiologically based pharmacokinetics; Transport; Unbound fraction

Indexed keywords

ALBUMIN; ALISKIREN; ATORVASTATIN; BOSENTAN; CERIVASTATIN; CIPROFLOXACIN; CYCLOSPORIN; DIGOXIN; FEXOFENADINE; FLUINDOSTATIN; FUROSEMIDE; INDOMETACIN; KETOCONAZOLE; NAPSAGATRAN; PENICILLIN G; PITAVASTATIN; PRAVASTATIN; PROPRANOLOL; QUINIDINE; REPAGLINIDE; ROSUVASTATIN; VALSARTAN; VERAPAMIL;

EID: 84879018695     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.23562     Document Type: Article
Times cited : (31)

References (35)
  • 1
    • 84455208265 scopus 로고    scopus 로고
    • In vitro-in vivo extrapolation of clearance: Modeling hepatic metabolic clearance of highly bound drugs and comparative assessment with existing methods
    • Poulin P, Kenny JR, Hop ECA, Haddad S. 2012. In vitro-in vivo extrapolation of clearance: Modeling hepatic metabolic clearance of highly bound drugs and comparative assessment with existing methods. J Pharm Sci 101:838-851.
    • (2012) J Pharm Sci , vol.101 , pp. 838-851
    • Poulin, P.1    Kenny, J.R.2    Hop, E.C.A.3    Haddad, S.4
  • 2
    • 84866369227 scopus 로고    scopus 로고
    • Comparative assessment of in vitro--in vivo extrapolation methods used for predicting hepatic metabolic clearance of drugs
    • Poulin P, Hop ECJ, Haddad S, Kenny JT. 2012. Comparative assessment of in vitro--in vivo extrapolation methods used for predicting hepatic metabolic clearance of drugs. J Pharm Sci 101:4308-4326.
    • (2012) J Pharm Sci , vol.101 , pp. 4308-4326
    • Poulin, P.1    Hop, E.C.J.2    Haddad, S.3    Kenny, J.T.4
  • 3
    • 84881609631 scopus 로고    scopus 로고
    • Toward a new paradigm for the efficient in vitro-in vivo extrapolation of metabolic clearance in humans from hepatocyte data
    • Epub ahead of pr t. DOI: 10.1002/jps.23502].
    • Poulin P, Haddad S. 2013. Toward a new paradigm for the efficient in vitro-in vivo extrapolation of metabolic clearance in humans from hepatocyte data. J Pharm Sci. [Epub ahead of print. DOI: 10.1002/jps.23502].
    • (2013) J Pharm Sci
    • Poulin, P.1    Haddad, S.2
  • 5
    • 0030997056 scopus 로고    scopus 로고
    • Effect of binding protein surface charge on palmitate uptake by hepatocyte suspensions
    • Burczynski FJ, Wang GQ, Hnatowich M. 1997. Effect of binding protein surface charge on palmitate uptake by hepatocyte suspensions. Br J Pharmacol 120:1215-1220.
    • (1997) Br J Pharmacol , vol.120 , pp. 1215-1220
    • Burczynski, F.J.1    Wang, G.Q.2    Hnatowich, M.3
  • 6
    • 84877997299 scopus 로고    scopus 로고
    • Insight into tissue unbound concentration: Utility in drug discovery and development
    • Mariappan TT, Mandlekar S, Marathe P. 2013. Insight into tissue unbound concentration: Utility in drug discovery and development. Curr Drug Metab 14:324-340.
    • (2013) Curr Drug Metab , vol.14 , pp. 324-340
    • Mariappan, T.T.1    Mandlekar, S.2    Marathe, P.3
  • 7
    • 84862891507 scopus 로고    scopus 로고
    • Evaluation of hepatic clearance prediction using in vitro data: Emphasis of fraction unbound in plasma and drug ionization using a dataset of 107 drugs
    • Halifax D, Houston BJ. 2012. Evaluation of hepatic clearance prediction using in vitro data: Emphasis of fraction unbound in plasma and drug ionization using a dataset of 107 drugs. J Pharm Sci 101:2645-2652.
    • (2012) J Pharm Sci , vol.101 , pp. 2645-2652
    • Halifax, D.1    Houston, B.J.2
  • 8
    • 84879019148 scopus 로고    scopus 로고
    • The volume of distribution is an indicator of poor in vitro-in vivo extrapolation of clearance for acidic drugs in the rat
    • Epub ahead of pr t. DOI:10.3109/00498254.2012.755578].
    • Sohlenius-Sternbeck AK, Fagerholm U, Bylund J. 2013. The volume of distribution is an indicator of poor in vitro-in vivo extrapolation of clearance for acidic drugs in the rat. Xenobiotica. [Epub ahead of print. DOI:10.3109/00498254.2012.755578].
    • (2013) Xenobiotica
    • Sohlenius-Sternbeck, A.K.1    Fagerholm, U.2    Bylund, J.3
  • 9
    • 84860858293 scopus 로고    scopus 로고
    • Novel in vitro-in vivo extrapolation (IVIVE) method to predict hepatic organ clearance in rat
    • Umehara K, Camenisch G. 2012. Novel in vitro-in vivo extrapolation (IVIVE) method to predict hepatic organ clearance in rat. Pharm Res 29:603-617.
    • (2012) Pharm Res , vol.29 , pp. 603-617
    • Umehara, K.1    Camenisch, G.2
  • 10
    • 84861234645 scopus 로고    scopus 로고
    • Predicting human hepatic clearance from in vitro drug metabolism and transport data: A scientific and pharmaceutical perspective for assessing drug-drug interactions
    • Umehara K, Camenisch G. 2012. Predicting human hepatic clearance from in vitro drug metabolism and transport data: A scientific and pharmaceutical perspective for assessing drug-drug interactions. Biopharm Drug Dispos 33:179-194.
    • (2012) Biopharm Drug Dispos , vol.33 , pp. 179-194
    • Umehara, K.1    Camenisch, G.2
  • 12
    • 84864998767 scopus 로고    scopus 로고
    • Use of uptake intrinsic clearance from attached rat hepatocytes to predict hepatic clearance for poorly permeable compounds
    • Huang L, Chen A, Roberts J, Janosky B, Be X, Berry L, Lin MHJ. 2012. Use of uptake intrinsic clearance from attached rat hepatocytes to predict hepatic clearance for poorly permeable compounds. Xenobiotica 42:830-840.
    • (2012) Xenobiotica , vol.42 , pp. 830-840
    • Huang, L.1    Chen, A.2    Roberts, J.3    Janosky, B.4    Be, X.5    Berry, L.6    Lin, M.H.J.7
  • 13
    • 84865191410 scopus 로고    scopus 로고
    • Use of mechanistic modeling to assess interindividual variability and interspecies differences in active uptake in human and rat hepatocytes
    • Ménochet K, Kenworthy KE, Houston BJ, Galetin A. 2012. Use of mechanistic modeling to assess interindividual variability and interspecies differences in active uptake in human and rat hepatocytes. Drug Metab Dispos 40:1744-1756.
    • (2012) Drug Metab Dispos , vol.40 , pp. 1744-1756
    • Ménochet, K.1    Kenworthy, K.E.2    Houston, B.J.3    Galetin, A.4
  • 15
    • 71949116668 scopus 로고    scopus 로고
    • Mechanistic modeling of hepatic transport from cells to whole Body: Application to Napsagatran and Fexofenadine
    • Poirier A, Funk C, Scherrmann JM, Lavé T. 2009. Mechanistic modeling of hepatic transport from cells to whole Body: Application to Napsagatran and Fexofenadine. Mol Pharm 6:1716-1733.
    • (2009) Mol Pharm , vol.6 , pp. 1716-1733
    • Poirier, A.1    Funk, C.2    Scherrmann, J.M.3    Lavé, T.4
  • 16
    • 46449097700 scopus 로고    scopus 로고
    • Prediction of the pharmacokinetics of atorvastatin, cerivastatin, and indomethacin using kinetic models applied to isolated rat hepatocytes
    • Paine SW, Parker AJ, Gardiner P, Webborn PJH, Riley RJ. 2008. Prediction of the pharmacokinetics of atorvastatin, cerivastatin, and indomethacin using kinetic models applied to isolated rat hepatocytes. Drug Metab Dispos 36:1365-1374.
    • (2008) Drug Metab Dispos , vol.36 , pp. 1365-1374
    • Paine, S.W.1    Parker, A.J.2    Gardiner, P.3    Webborn, P.J.H.4    Riley, R.J.5
  • 17
    • 59649130318 scopus 로고    scopus 로고
    • Physiologically based pharmacokinetic modeling to predict transporter-mediated clearance and distribution of pravastatin in humans
    • Watanabe T, Kusuhara H, Maeda K, Shitara Y, Sugiyama Y. 2009. Physiologically based pharmacokinetic modeling to predict transporter-mediated clearance and distribution of pravastatin in humans. J Pharmacol Exp Ther 328:652-662.
    • (2009) J Pharmacol Exp Ther , vol.328 , pp. 652-662
    • Watanabe, T.1    Kusuhara, H.2    Maeda, K.3    Shitara, Y.4    Sugiyama, Y.5
  • 18
    • 76149124823 scopus 로고    scopus 로고
    • Investigation of the rate-determining process in the hepatic elimination of HMG-CoA reductase inhibitors in rats and humans
    • Watanabe T, Kusuhara H, Maeda K, Kanamaru H, Saito Y, Hu Z, Sugiyama Y. 2009. Investigation of the rate-determining process in the hepatic elimination of HMG-CoA reductase inhibitors in rats and humans. Drug Metab Dispos 38:215-222.
    • (2009) Drug Metab Dispos , vol.38 , pp. 215-222
    • Watanabe, T.1    Kusuhara, H.2    Maeda, K.3    Kanamaru, H.4    Saito, Y.5    Hu, Z.6    Sugiyama, Y.7
  • 20
    • 14044251501 scopus 로고    scopus 로고
    • The binding of drugs to hepatocytes and its relationship to physicochemical properties
    • Austin RP, Barton P, Mohmed S, Riley RJ. 2005. The binding of drugs to hepatocytes and its relationship to physicochemical properties. Drug Metab Dispos 33:419-425
    • (2005) Drug Metab Dispos , vol.33 , pp. 419-425
    • Austin, R.P.1    Barton, P.2    Mohmed, S.3    Riley, R.J.4
  • 21
    • 0242509092 scopus 로고    scopus 로고
    • Absolute oral bioavailability of rosuvastatin in healthy white adult male volunteers
    • Martin PD, Warwick MJ, Dane AL, Brindley C, Short T. 2003. Absolute oral bioavailability of rosuvastatin in healthy white adult male volunteers. Clin Ther 25:2553-2563.
    • (2003) Clin Ther , vol.25 , pp. 2553-2563
    • Martin, P.D.1    Warwick, M.J.2    Dane, A.L.3    Brindley, C.4    Short, T.5
  • 22
    • 0023429021 scopus 로고
    • Pharmacokinetics of cyclosporin: Influence of rate of constant intravenous infusion in renal transplant patients
    • Gupta SK, Legg B, Solomon LR, Johnson WG, Rowland M. 1987. Pharmacokinetics of cyclosporin: Influence of rate of constant intravenous infusion in renal transplant patients. Br J Clin Pharmacol 24:519-526.
    • (1987) Br J Clin Pharmacol , vol.24 , pp. 519-526
    • Gupta, S.K.1    Legg, B.2    Solomon, L.R.3    Johnson, W.G.4    Rowland, M.5
  • 23
    • 0032469937 scopus 로고    scopus 로고
    • Physiologically based pharmacokinetics of cyclosporine A: Extension to tissue distribution kinetics in rats and scale-up to human
    • Kawai R, Mathew D, Tanaka C, Rowland M. 1998. Physiologically based pharmacokinetics of cyclosporine A: Extension to tissue distribution kinetics in rats and scale-up to human. J Pharmacol Exp Ther 287:457-468.
    • (1998) J Pharmacol Exp Ther , vol.287 , pp. 457-468
    • Kawai, R.1    Mathew, D.2    Tanaka, C.3    Rowland, M.4
  • 24
    • 71649089269 scopus 로고    scopus 로고
    • Development of a novel method for predicting human volume of distribution at steady-state of basic drugs and comparative assessment with existing methods
    • Poulin P, Theil FP. 2009. Development of a novel method for predicting human volume of distribution at steady-state of basic drugs and comparative assessment with existing methods. J Pharm Sci 98:4941-4961.
    • (2009) J Pharm Sci , vol.98 , pp. 4941-4961
    • Poulin, P.1    Theil, F.P.2
  • 25
    • 79960952379 scopus 로고    scopus 로고
    • In vitro-in vivo extrapolation of CYP2C8-catalyzed paclitaxel 6α-hydroxylation: Effects of albumin on in vitro kinetic parameters and assessment of interindividual variability in predicted clearance
    • Wattanachai N, Polasek TM, Heath TM, Uchaipichat V, Wongwiwat T, Tassaneeyakul W, Miners JO. 2011. In vitro-in vivo extrapolation of CYP2C8-catalyzed paclitaxel 6α-hydroxylation: Effects of albumin on in vitro kinetic parameters and assessment of interindividual variability in predicted clearance. Eur J Clin Pharmacol 67:815-824.
    • (2011) Eur J Clin Pharmacol , vol.67 , pp. 815-824
    • Wattanachai, N.1    Polasek, T.M.2    Heath, T.M.3    Uchaipichat, V.4    Wongwiwat, T.5    Tassaneeyakul, W.6    Miners, J.O.7
  • 27
    • 0028870140 scopus 로고
    • Kinetics of bilirubin transfer between serum albumin and membrane vesicles
    • Zucker SD, Goessling W, Gollan JL. 1995. Kinetics of bilirubin transfer between serum albumin and membrane vesicles. J Biol Chem 270:1074-1081.
    • (1995) J Biol Chem , vol.270 , pp. 1074-1081
    • Zucker, S.D.1    Goessling, W.2    Gollan, J.L.3
  • 28
    • 0036259919 scopus 로고    scopus 로고
    • Effect of albumin on phenytoin and tolbutamide metabolism in human liver microsomes: An impact more than protein binding
    • Tang C, Lin Y, Rodrigues DA, Lin JH. 2002. Effect of albumin on phenytoin and tolbutamide metabolism in human liver microsomes: An impact more than protein binding. Drug Metab Dispos 30:648-654.
    • (2002) Drug Metab Dispos , vol.30 , pp. 648-654
    • Tang, C.1    Lin, Y.2    Rodrigues, D.A.3    Lin, J.H.4
  • 30
  • 31
    • 84858404510 scopus 로고    scopus 로고
    • Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: Comparison with liver and intestinal glucuronidation and impact of albumin
    • Gill KL, Houston BJ, Galetin A. 2012. Characterization of in vitro glucuronidation clearance of a range of drugs in human kidney microsomes: Comparison with liver and intestinal glucuronidation and impact of albumin. Drug Metb Dispos 40:825-835.
    • (2012) Drug Metb Dispos , vol.40 , pp. 825-835
    • Gill, K.L.1    Houston, B.J.2    Galetin, A.3
  • 32
    • 0036302860 scopus 로고    scopus 로고
    • Interaction of albumin with the endothelial cell surface
    • Osterloh K, Ewert U, Pries AR. 2002. Interaction of albumin with the endothelial cell surface. Am J Physiol 283:H398-H405.
    • (2002) Am J Physiol , vol.283
    • Osterloh, K.1    Ewert, U.2    Pries, A.R.3
  • 33
    • 84859358235 scopus 로고    scopus 로고
    • The pharmacokinetics and hepatic disposition of repaglinide in pigs: Mechanistic modeling of metabolism and transport
    • Sjögren E, Bredberg U, Lennernäs H. 2012. The pharmacokinetics and hepatic disposition of repaglinide in pigs: Mechanistic modeling of metabolism and transport. Mol Pharm 9:823-841.
    • (2012) Mol Pharm , vol.9 , pp. 823-841
    • Sjögren, E.1    Bredberg, U.2    Lennernäs, H.3
  • 34
    • 80053161024 scopus 로고    scopus 로고
    • Kinetic characterization of rat hepatic uptake of 16 actively transported drugs
    • Yabe Y, Galetin A, Houston BJ. 2011. Kinetic characterization of rat hepatic uptake of 16 actively transported drugs. Drug Metab Dispos 39:1808-1814.
    • (2011) Drug Metab Dispos , vol.39 , pp. 1808-1814
    • Yabe, Y.1    Galetin, A.2    Houston, B.J.3
  • 35
    • 77957357276 scopus 로고    scopus 로고
    • Extrapolating in vitro metabolic interactions to isolated perfused liver: Prediction of metabolic interactions between bufarolol, bunitrolol and debrisoquine
    • Haddad S, Poulin P, Funk C. 2010. Extrapolating in vitro metabolic interactions to isolated perfused liver: Prediction of metabolic interactions between bufarolol, bunitrolol and debrisoquine. J Pharm Sci 99:4406-4426.
    • (2010) J Pharm Sci , vol.99 , pp. 4406-4426
    • Haddad, S.1    Poulin, P.2    Funk, C.3


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