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An Evaluation of the Dilution Method for Identifying Metabolism-Dependent Inhibitors of Cytochrome P450 Enzymes

Parkinson, Andrew, Kazmi, Faraz, Buckley, David B., Yerino, Phyllis, Paris, Brandy L., Holsapple, Jeff, Toren, Paul, Otradovec, Steve M., Ogilvie, Brian W.·2011·Drug Metabolism and Disposition
DOI 10.1124/dmd.111.038596
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Research works printed but not linked: 35

  1. Atkinson, 2005, Automated assessment of time-dependent inhibition of human cytochrome P450 enzymes using liquid chromatography-tandem mass spectrometry analysis, Drug Metab Dispos, 33, 1637, 10.1124/dmd.105.005579 · DOI
  2. Austin, 2002, The influence of nonspecific microsomal binding on apparent intrinsic clearance, and its prediction from physicochemical properties, Drug Metab Dispos, 30, 1497, 10.1124/dmd.30.12.1497 · DOI · Paper page
  3. Berry, 2008, An examination of IC50 and IC50-shift experiments in assessing time-dependent inhibition of CYP3A4, CYP2D6 and CYP2C9 in human liver microsomes, Drug Metab Lett, 2, 51, 10.2174/187231208783478407 · DOI
  4. Buckley, 2008, Metabolism-dependent cytochrome P450 inhibitors: in vitro assessment of reversibility by ultracentrifugation methods, Drug Metab Rev, 40, 172
  5. Cheng, 1973, Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction, Biochem Pharmacol, 22, 3099, 10.1016/0006-2952(73)90196-2 · DOI · Paper page
  6. Fowler, 2008, In vitro evaluation of reversible and irreversible cytochrome P450 inhibition: current status on methodologies and their utility for predicting drug-drug interactions, AAPS J, 10, 410, 10.1208/s12248-008-9042-7 · DOI
  7. Gertz, 2008, Drug lipophilicity and microsomal protein concentration as determinants in the prediction of the fraction unbound in microsomal incubations, Drug Metab Dispos, 36, 535, 10.1124/dmd.107.018713 · DOI
  8. Ghanbari, 2006, A critical evaluation of the experimental design of studies of mechanism based enzyme inhibition, with implications for in vitro-in vivo extrapolation, Curr Drug Metab, 7, 315, 10.2174/138920006776359293 · DOI
  9. Grime, 2009, Mechanism-based inhibition of cytochrome P450 enzymes: an evaluation of early decision making in vitro approaches and drug-drug interaction prediction methods, Eur J Pharm Sci, 15, 175, 10.1016/j.ejps.2008.10.002 · DOI
  10. Grimm, 2009, The conduct of in vitro studies to address time-dependent inhibition of drug-metabolizing enzymes: a perspective of the Pharmaceutical Research and Manufacturers of America, Drug Metab Dispos, 37, 1355, 10.1124/dmd.109.026716 · DOI · Paper page
  11. Hallifax, 2006, Binding of drugs to hepatic microsomes: comment and assessment of current prediction methodology with recommendation for improvement, Drug Metab Dispos, 34, 724, 10.1124/dmd.105.007658 · DOI
  12. Huang, 2008, New era in drug interaction evaluation: US Food and Drug Administration update on CYP enzymes, transporters, and the guidance process, J Clin Pharmacol, 48, 662, 10.1177/0091270007312153 · DOI · Paper page
  13. Jones, 1999, Diltiazem inhibition of cytochrome P-450 3A activity is due to metabolite intermediate complex formation, J Pharmacol Exp Ther, 290, 1116, 10.1016/S0022-3565(24)35013-X · DOI
  14. Johnson, 2008, Cytochrome P450 inactivation by pharmaceuticals and phytochemicals: therapeutic relevance, Drug Metab Rev, 40, 101, 10.1080/03602530701836704 · DOI
  15. Kawakami, 2011, Simultaneous absolute quantification of 11 cytochrome P450 isoforms in human liver microsomes by liquid chromatography tandem mass spectrometry with in silico target peptide selection, J Pharm Sci, 100, 341, 10.1002/jps.22255 · DOI
  16. Kitz, 1962, Esters of methanesulfonic acid as irreversible inhibitors of acetylcholinesterase, J Biol Chem, 237, 3245, 10.1016/S0021-9258(18)50153-8 · DOI · Paper page
  17. Krippendorff, 2009, Mechanism-based inhibition: deriving KI and kinact directly from time-dependent IC50 values, J Biomol Screen, 14, 913, 10.1177/1087057109336751 · DOI
  18. López-Garcia, 1994, Thiophene derivatives as new mechanism-based inhibitors of cytochromes P-450: inactivation of yeast-expressed human liver cytochrome P-450 2C9 by tienilic acid, Biochemistry, 33, 166, 10.1021/bi00167a022 · DOI
  19. Maurer, 2000, Impact of mechanism-based enzyme inactivation on inhibitor potency: implications for rational drug discovery, J Pharm Sci, 89, 1404, 10.1002/1520-6017(200011)89:11<1404::AID-JPS4>3.0.CO;2-# · DOI
  20. Obach, 2007, Mechanism-based inactivation of human cytochrome p450 enzymes and the prediction of drug-drug interactions, Drug Metab Dispos, 35, 246, 10.1124/dmd.106.012633 · DOI
  21. Ogilvie, 2006, Glucuronidation converts gemfibrozil to a potent, metabolism-dependent inhibitor of CYP2C8: implications for drug-drug interactions, Drug Metab Dispos, 34, 191, 10.1124/dmd.105.007633 · DOI
  22. Paris, 2009, In vitro inhibition and induction of human liver cytochrome P450 enzymes by milnacipran, Drug Metab Dispos, 37, 2045, 10.1124/dmd.109.028274 · DOI
  23. Parkinson, 2004, The effects of gender, age, ethnicity, and liver cirrhosis on cytochrome P450 enzyme activity in human liver microsomes and inducibility in cultured human hepatocytes, Toxicol Appl Pharmacol, 199, 193, 10.1016/j.taap.2004.01.010 · DOI · Paper page
  24. Pearce, 1996, Identification of the human P450 enzymes involved in lansoprazole metabolism, J Pharmacol Exp Ther, 277, 805, 10.1016/S0022-3565(25)12938-8 · DOI
  25. Perloff, 2009, Validation of cytochrome P450 time-dependent inhibition assays: a two-time point IC50 shift approach facilitates kinact assay design, Xenobiotica, 39, 99, 10.1080/00498250802638155 · DOI
  26. Polasek, 2007, In vitro approaches to investigate mechanism-based inactivation of CYP enzymes, Expert Opin Drug Metab Toxicol, 3, 321, 10.1517/17425255.3.3.321 · DOI
  27. Prueksaritanont, 1999, Metabolic interactions between mibefradil and HMG-CoA reductase inhibitors: an in vitro investigation with human liver preparations, Br J Clin Pharmacol, 47, 291, 10.1046/j.1365-2125.1999.00903.x · DOI
  28. Robertson, 2000, In vitro inhibition and induction of human hepatic cytochrome P450 enzymes by modafinil, Drug Metab Dispos, 28, 664, 10.1016/S0090-9556(24)15146-X · DOI
  29. Silverman, 1995, Mechanism-based enzyme inactivators, Methods Enzymol, 249, 240, 10.1016/0076-6879(95)49038-8 · DOI
  30. Tran, 2002, Microsomal protein concentration modifies the apparent inhibitory potency of CYP3A inhibitors, Drug Metab Dispos, 30, 1441, 10.1124/dmd.30.12.1441 · DOI
  31. Van, 2006, The impact of experimental design on assessing mechanism-based inactivation of CYP2D6 by MDMA (Ecstasy), J Psychopharmacol, 20, 834, 10.1177/0269881106062902 · DOI
  32. Van, 2007, Kinetics of the time-dependent inactivation of CYP2D6 in cryopreserved human hepatocytes by methylenedioxymethamphetamine (MDMA), Eur J Pharm Sci, 31, 53, 10.1016/j.ejps.2007.02.005 · DOI
  33. Venkatakrishnan, 2007, Drug-drug interactions via mechanism-based cytochrome P450 inactivation: points to consider for risk assessment from in vitro data and clinical pharmacologic evaluation, Curr Drug Metab, 8, 449, 10.2174/138920007780866861 · DOI
  34. Yang, 2005, Kinetic values for mechanism-based enzyme inhibition: assessing the bias introduced by the conventional experimental protocol, Eur J Pharm Sci, 26, 334, 10.1016/j.ejps.2005.07.005 · DOI
  35. Yerino, 2007, Effects of microsomal protein concentration on the IC50 shift for mechanism-based inhibitors of CYP1A2, 2A6, 2B6, 2C9, 2C19, 2D6 and 2E1, Drug Metab Rev, 39, 223

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Metadata

Authors
Parkinson, A., Kazmi, F., Buckley, D. B., Yerino, P., Paris, B. L., Holsapple, J., Toren, P., Otradovec, S. M., & Ogilvie, B. W.
Venue
Drug Metabolism and Disposition
Publisher
Elsevier BV
Published
2011-08
Volume
39
Issue
8
Pages
1370-1387
ISSN
0090-9556
DOI
10.1124/dmd.111.038596
Cited by
67
References
0
Language
en
Licence
  • www.elsevier.com/tdm/userlicense/1.0/ (tdm)
  • www.elsevier.com/legal/tdmrep-license (tdm)

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CoChat. (2026). Citation check: An Evaluation of the Dilution Method for Identifying Metabolism-Dependent Inhibitors of Cytochrome P450 Enzymes. https://app.cochat.ai/papers/10.1124/dmd.111.038596
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Parkinson, A., Kazmi, F., Buckley, D. B., Yerino, P., Paris, B. L., Holsapple, J., Toren, P., Otradovec, S. M., & Ogilvie, B. W. (2011). An Evaluation of the Dilution Method for Identifying Metabolism-Dependent Inhibitors of Cytochrome P450 Enzymes. Drug Metabolism and Disposition. https://doi.org/10.1124/dmd.111.038596

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