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Xenobiotica
the fate of foreign compounds in biological systems
Volume 35, 2005 - Issue 5
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Research Article

Impact of end-product inhibition on the determination of in vitro metabolic clearance

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Pages 439-454 | Received 19 Jan 2005, Published online: 16 Oct 2008

References

  • Ashforth EIL, Carlile DJ, Chenery R, Houston JB. 1995. Prediction of in vivo disposition from in vitro systems: Clearance of phenytoin and tolbutamide using rat hepatic microsomal and hepatocyte data. Journal of Pharmacology and Experimental Therapeutics 274:761–766.
  • Ashley JJ, Levy G. 1972. Inhibition of diphenylhydantoin elimination by its major metabolite. Research Communications in Chemical Pathology and Pharmacology 4:297–306.
  • Carlile DJ, Stevens AJ, Ashforth EIL, Waghela D, Houston JB. 1998. In vivo clearance of ethoxycoumarin and its prediction from in vitro systems. Drug Metabolism and Disposition 26:216–221.
  • Carlile DJ, Zomorodi K, Houston JB. 1997. Scaling factors to relate drug metabolic clearance in hepatic microsomes, isolated hepatocytes and the intact liver: Studies with induced livers involving diazepam. Drug Metabolism and Disposition 25:903–911.
  • Chenery RJ, Ayrton A, Oldham HG, Standring P, Norman SJ, Seddon T, Kirby R. 1987. Diazepam metabolism in cultured hepatocytes from rat, rabbit, dog, guinea pig and man. Drug Metabolism and Disposition 15:312–317.
  • Fisher MB, Campanale K, Ackermann BL, Vandenbranden M, Wrighton SA. 2000. In vitro glucuronidation using human liver microsomes and the pore-forming peptide alamethicin. Drug Metabolism and Disposition 28:560–566.
  • Fisher MB, Paine MF, Strelevitz TJ, Wrighton SA. 2001. The role of hepatic and extrahepatic UDP-glucuronosyltransferases in human drug metabolism. Drug Metabolism Reviews 33:273–297.
  • Foti RS, Fisher MB. 2004. Impact of incubation conditions on bufuralol human clearance predictions: Enzyme lability and non-specific binding. Drug Metabolism and Disposition 32:295–304.
  • Houston JB. 1994. Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance. Biochemical Pharmacology 47:1469–1479.
  • Houston JB, Carlile DJ. 1997. Prediction of hepatic clearance from microsomes, hepatocytes and liver slices. Drug Metabolism Reviews 29:891–922.
  • Houston JB, Kenworthy KE, Galetin A. 2003. Typical and atypical enzyme kinetics. In: Lee JS, Obach RS, Fisher MB, editors. Drug metabolizing enzymes. Cytochrome P450 and other enzymes in drug discovery and development. Lausanne: Fontis Media, and New York: Marcel Dekker. pp 211–254.
  • Ito K, Houston JB. 2004. Comparison of the use of liver models for predicting drug clearance using in vitro kinetic data from hepatic microsomes and isolated hepatocytes. Pharmaceutical Research 21:785–792.
  • Iwatsubo T, Hirota N, Ooie T, Suzuki H, Shimada N, Chiba K, Ishizaki T, Green CE, Tyson CA, Sugiyama Y. 1997. Prediction of in vivo drug metabolism in the human liver from in vitro metabolism data. Pharmacology and Therapeutics 73:147–171.
  • Jones HM, Hallifax D, Houston JB. 2004. Quantitative prediction of the in vivo inhibition of diazepam metabolism by omeprazole using rat liver microsomes and hepatocytes. Drug Metabolism and Disposition 32:572–580.
  • Jones HM, Houston JB. 2004. Use of the substrate depletion approach for determining in vitro metabolic clearance: Time dependencies in hepatocyte and microsomal incubations. Drug Metabolism and Disposition 32:973–982.
  • Kitagawa H, Esumi Y, Kurosawa S, Sekine S, Yokoshima T. 1979. Metabolism of 8-chloro-6-(o-chloropheny1)-1-methyl-4H-s-triazolo[4,3-a] [1,4]benzodiazepine, triazolarn, a new central depressant. II. Identification and determination of metabolites in rats and dogs. Xenobiotica 9:429–439.
  • Lave T, Dupin S, Schmitt C, Valles B, Ubead G, Chou RC, Jaeck D, Coassolo P. 1997. The use of human hepatocytes to select compounds based on their expected hepatic extraction ratios in humans. Pharmaceutical Research 14:152–155.
  • Levy G, Ashley JJ. 1972. Effect of an inhibitor of glucuronide formation on elimination kinetics of diphenylhydantoin in rats. Journal of Pharmaceutical Sciences 62:161–162.
  • Little JM, Lehman PA, Nowell S, Samokyszyn V, Radominska A. 1997. Glucuronidation of all-trans-rannoic acid and 5,6-epoxy-all-trans-rannoic acid. Drug Metabolism and Disposition 25:5–11.
  • Madan A, Usuki E, Burton LA, Ogilvie BW, Parkinson A. 2002. In vitro approaches for studying the inhibition of drug-metabolising enzymes and identifying the drug-metabolising enzymes responsible for the metabolism of drugs. In: Rodrigues A, editor. Drug-drug interactions. New York: Marcel-Dekker. pp 217–293.
  • Margolis JM, Obach RS. 2003. Impact of nonspecific binding to microsomes and phospholipid on the inhibition of cytochrome P4502D6: Implications for relating in vitro inhibition data to in vivo drug interactions. Drug Metabolism and Disposition 31:606–611.
  • McGinnity DF, Riley RJ. 2001. Predicting drug pharmacokinetics in humans from in vitro metabolism studies. Biochemical Society Transactions 29:135–139.
  • 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 Metabolism and Disposition 27:1350–1359.
  • Obach RS. 2001. The prediction of human clearance from hepatic microsomal data. Current Opinions in Drug Discovery and Development 4:36–44.
  • Obach RS, Reed-Hagen AE. 2002. Measurement of Michaelis constants for cytochrome P450-mediated biotransformation reactions using the substrate depletion approach. Drug Metabolism and Disposition 30:831–837.
  • Savenije-Chapel EM, Bast A, Noordhoek J. 1985. Inhibition of diazepam metabolism in microsomal and perfumed liver preparations of the rat by desmethyldiazepam, N-methyloxazepam and oxazepam. European Journal of Drug Metabolism and Pharmacokinetics 10:15–20.
  • Seddon T, Michelle I, Chenery RJ. 1989. Comparative drug metabolism of diazepam in hepatocytes isolated from man, rat, monkey and dog. Biochemical Pharmacology 38:1657–1665.
  • Shou M, Mei Q, Ettore MW, Dai R, Baille TA, Rushmore TH. 1999. Sigmoidal kinetic model for two co-operative substrate binding sites in a cytochrome P450 3A4 active site: An example of the metabolism of diazepam and its derivatives. Biochemical Journal 340:845–853.
  • Tran TH, Von Moltke LL, Venkatakrishnan K, Granda BW, Gibbs MA, Obach RS, Harmatz JS, Greenblatt DJ. 2002. Microsomal protein concentration modifies the apparent inhibitory potency of CYP3A inhibitors. Drug Metabolism and Disposition 30:1441–1445.
  • Zomorodi K, Carlile DJ, Houston JB. 1995. Kinetics of diazepam metabolism in rat hepatic microsomes and hepatocytes and their use in predicting in vivo hepatic clearance. Xenobiotica 25:907–916.

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