Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 37, 2007 - Issue 9
294
Views
24
CrossRef citations to date
0
Altmetric
Research Article

Development of an in vivo rat screen model to predict pharmacokinetic interactions of CYP3A4 substrates

, , , , , & show all
Pages 923-942 | Received 09 Jun 2007, Accepted 12 Jul 2007, Published online: 22 Sep 2008

References

  • Alfaro CL. Emerging role of drug interaction studies in drug development: the good, the bad, and the unknown. Psychopharmacology Bulletin 2001; 35(4)80–93
  • Backman JT, Karjalainen MJ, Neuvonen M, Laitila J, Neuvonen PJ. Rofecoxib is a potent inhibitor of cytochrome P450 1A2: studies with tizanidine and caffeine in healthy subjects. British Journal of Clinical Pharmacology 2006; 62(3)345–357
  • Bailey DG, Bend JR, Arnold JM, Tran LT, Spence JD. Erythromycin–felodipine interaction: magnitude, mechanism, and comparison with grapefruit juice. Clinical Pharmacology and Therapeutics 1996; 60(1)25–33
  • Balimane PV, Chong S, Morrison RA. Current methodologies used for evaluation of intestinal permeability and absorption. Journal of Pharmacology and Toxicology Methods 2000; 44(1)301–312
  • Balimane PV, Patel K, Marino A, Chong S. Utility of 96 well Caco-2 cell system for increased throughput of P-gp screening in drug discovery. European Journal of Pharmacology and Biopharmacology 2004; 58(1)99–105
  • Barraud de Lagerie S, Comets E, Gautrand C, Fernandez C, Auchere D, Singlas E, Mentre F, Gimenez F. Cerebral uptake of mefloquine enantiomers with and without the P-gp inhibitor elacridar (GF120918) in mice. British Journal of Pharmacology 2004; 141(7)1214–1222
  • Bjornsson TD, Callaghan JT, Einolf HJ, Fischer V, Gan L, Grimm S, Kao J, King SP, Miwa G, Ni L, et al. The conduct of in vitro and in vivo drug–drug interaction studies: a PhRMA perspective. Journal of Clinical Pharmacology 2003; 43(5)443–469
  • Brown CS, Farmer RG, Soberman JE, Eichner SF. Pharmacokinetic factors in the adverse cardiovascular effects of antipsychotic drugs. Clinical Pharmacokinetics 2004; 43(1)33–56
  • Cummins CL, Samphati L, Reid MJ, Benet LZ. In vivo modulation of intestinal CYP3A metabolism by P-glycoprotein: Studies using the rat single-pass intestinal perfusion model. Journal of Pharmacology and Experimental Therapeutics 2003; 305(1)306–314
  • Dambach DM, Andrews BA, Moulin F. New technologies and screening strategies for hepatotoxicity: Use of in vitro models. Toxicology and Pathology 2005; 33(1)17–26
  • Dresser GK, Bailey DG. A basic conceptual and practical overview of interactions with highly prescribed drugs. Canadian Journal of Clinical Pharmacology 2002; 9(4)191–198
  • Emoto C, Murase S, Iwasaki K. Approach to the prediction of the contribution of major cytochrome P450 enzymes to drug metabolism in the early drug-discovery stage. Xenobiotica 2006; 36(8)671–683
  • Fahey J, Pritchard G, von Moltke LL, Pratt J, Grassi J, Ri S, Greenblatt D. The effects of ketoconazole on triazolam pharmacokinetics, pharmacodynamics and benzodiazepine receptor binding in mice. Journal of Pharmacology and Experimental Therapeutics 1998; 285(1)271–276
  • Ghosal A, Satoh K, Thomas PE, Bush E, Moore D. Inhibition of kinetics of cytochrome P4503A activity in microsomes from rat, human and cDNA-expressed human cytochrome P450. Drug Metabolism and Disposition 1996; 24(9)940–947
  • Gorski JC, Jones DR, Haehner-Daniels BD, Hamman MA, O’Mara EM, Jr, Hall SD. The contribution of intestinal and hepatic CYP3A to the interaction between midazolam and clarithromycin. Clinical Pharmacology and Therapeutics 1998; 64(2)133–143
  • Guengerich FP. Cytochrome P-450 3A4: Regulation and role in drug metabolism. Annual Review of Pharmacology and Toxicology 1999; 39: 1–17
  • Hara Y, Nakajima M, Miyamoto KI, Yokoi T. Inhibitory effects of psychotropic drugs on mexiletine metabolism in human liver microsomes: Prediction of in vivo drug interactions. Xenobiotica 2005; 35(6)549–560
  • Ho RH, Kim RB. Transporters and drug therapy: Implications for drug disposition and disease. Clinical Pharmacology and Therapeutics 2005; 78(3)260–277
  • Honig PK, Wortham DC, Hull R, Zamani K, Smith JE, Cantilena LR. Itraconazole affects single-dose terfenadine pharmacokinetics and cardiac repolarization pharmacodynamics. Journal of Clinical Pharmacology 1993a; 33(12)1201–1206
  • Honig PK, Wortham DC, Zamani K, Conner DP, Mullin JC, Cantilena LR. Terfenadine–ketoconazole interaction. Pharmacokinetic and electrocardiographic consequences. Journal of the American Medical Association 1993b; 269(12)1513–1518
  • Hutzler M, Messing DM, Wienkers LC. Predicting drug–drug interactions in drug discovery: where are we now and where are we going?. Current Opinions in Drug Discovery and Development 2005; 8(1)51–58
  • Ito K, Iwatsubo T, Kanamitsu S, Nakajima Y, Sugiyama Y. Quantitative prediction of in vivo drug clearance and drug interactions from in vitro data on metabolism, together with binding and transport. Annual Reviews in Pharmacology and Toxicology 1998a; 38: 461–499
  • Ito K, Iwatsubo T, Kanamitsu S, Ueda K, Suzuki H, Sugiyama Y. Prediction of pharmacokinetic alterations caused by drug–drug interactions: Metabolic interaction in the liver. Pharmacological Reviews 1998b; 50(3)387–412
  • Jones PH, Davidson MH. Reporting rate of rhabdomyolysis with fenofibrate + statin versus gemfibrozil + any statin. American Journal of Cardiology 2005; 95(1)120–122
  • Kaddoumi A, Fleisher D, Heimbach T, Li LY, Cole S. Factors influencing regional differences in intestinal absorption of UK-343,664 in rat: Possible role in dose-dependent pharmacokinetics. Journal of Pharmaceutical Sciences 2006; 95(2)435–445
  • Kageyama M, Namiki H, Fukushima H, Ito Y, Shibata N, Takada K. In vivo effects of cyclosporin A and ketoconazole on the pharmacokinetics of representative substrates for P-glycoprotein and cytochrome P450 (CYP) 3A in rats. Biology and Pharmacology Bulletin 2005; 28(2)316–322
  • Kanamitsu S, Ito K, Sugiyama Y. Quantitative prediction of in vivo drug–drug interactions from in vitro data based on physiological pharmacokinetics: Use of maximum unbound concentration of inhibitor at the inlet to the liver. Pharmaceutical Research 2000; 17(3)336–343
  • Kanazu T, Okamura N, Yamaguchi Y, Baba T, Koike M. Assessment of the hepatic and intestinal first-pass metabolism of midazolam in a CYP3A drug–drug interaction model rats. Xenobiotica 2005; 35(4)305–317
  • Kanazu T, Yamaguchi Y, Okamura N, Baba T, Koike M. Model for the drug–drug interaction responsible for CYP3A enzyme inhibition. I: Evaluation of cynomolgus monkeys as surrogates for humans. Xenobiotica 2004; 34(5)391–402
  • Kim MJ, Kim H, Cha IJ, Park JS, Shon JH, Liu KH, Shin JG. High-throughput screening of inhibitory potential of nine cytochrome P450 enzymes in vitro using liquid chromatography/tandem mass spectrometry. Rapid Communications in Mass Spectrometry 2005; 19(18)2651–2658
  • Kind AH, Zakowski LJ, McBride PE. Rhabdomyolysis from the combination of a statin and gemfibrozil: An uncommon but serious adverse reaction. Wisconsin Medical Journal 2002; 101(7)53–56
  • Kivisto KT, Lilja JJ, Backman JT, Neuvonen PJ. Repeated consumption of grapefruit juice considerably increases plasma concentrations of cisapride. Clinical Pharmacology and Therapeutics 1999; 66(5)448–453
  • Kobayashi K, Urashima K, Shimada N, Chiba K. Selectivities of human cytochrome P450 inhibitors toward rat P450 isoforms: Study with cDNA-expressed systems of the rat. Drug Metabolism and Disposition 2003; 31(7)833–836
  • Kotegawa T, Laurijssens BE, Durol AL, Greenblatt DJ. Pharmacokinetics and electroencephalographic effects of ketoconazole in the rat. Biopharmaceutics and Drug Disposition 1999; 20(1)49–52
  • Kotegawa T, Laurijssens BE, Von Moltke LL, Cotreau MM, Perloff MD, Venkatakrishnan K, Warrington JS, Granda BW, Harmatz JS, Greenblatt DJ. In vitro, pharmacokinetics, and pharmacodynamic interactions of ketoconazole and midozolam in the rat. Journal of Pharmacology and Experimental Therapeutics 2002; 302(3)1228–1237
  • Kuroha M, Azumano A, Kuze Y, Shimoda M, Kokue E. Effect of multiple dosing of ketoconazole on pharmacokinetics of midazolam, a cytochrome P450 3A substrate in beagle dogs. Drug Metabolism and Disposition 2002a; 30(1)63–68
  • Kuroha M, Kayaba H, Kishimoto S, Khalil WF, Shimoda M, Kokue E. Effect of oral ketoconazole on first-pass effect of nifedipine after oral administration in dogs. Journal of Pharmaceutical Sciences 2002b; 91(3)868–873
  • Lam YW, Alfaro CL, Ereshefsky L, Miller M. Pharmacokinetic and pharmacodynamic interactions of oral midazolam with ketoconazole, fluoxetine, fluvoxamine, and nefazodone. Journal of Clinical Pharmacology 2003; 43(11)1274–1282
  • Lees RS, Lees AM. Rhabdomyolysis from the coadministration of lovastatin and the antifungal agent itraconazole. New England Journal of Medicine 1995; 333(10)664–665
  • Marathe PH, Rodrigues AD. In vivo animal models for investigating potential CYP3A- and Pgp-mediated drug–drug interactions. Current Drug Metabolism 2006; 7(7)687–704
  • Obach RS, Walsky RL, Venkatakrishnan K, Houston JB, Tremaine LM. In vitro cytochrome P450 inhibition data and the prediction of drug–drug interactions: qualitative relationships, quantitative predictions, and the rank-order approach. Clinical Pharmacology and Therapeutics 2005; 78(6)582–592
  • Ogilvie BW, Zhang D, Li W, Rodrigues AD, Gipson AE, Holsapple J, Toren P, Parkinson A. Glucuronidation converts gemfibrozil to a potent, metabolism-dependent inhibitor of CYP2C8: Implications for drug–drug interactions. Drug Metabolism and Disposition 2006; 34(1)191–197
  • Pea F, Furlanut M. Pharmacokinetic aspects of treating infections in the intensive care unit: Focus on drug interactions. Clinical Pharmacokinetics 2001; 40(11)833–868
  • Persson KP, Ekehed S, Otter C, Lutz ES, McPheat J, Masimirembwa CM, Andersson TB. Evaluation of human liver slices and reporter gene assays as systems for predicting the cytochrome P450 induction potential of drugs in vivo in humans. Pharmacology Research 2006; 23(1)56–59
  • Piquette RK. Torsade de pointes induced by cisapride/clarithromycin interaction. Annals of Pharmacotherapy 1999; 33(1)22–26
  • Rodrigues AD. Integrated cytochrome P450 reaction phenotyping: Attempting to bridge the gap between cDNA-expressed cytochromes P450 and native human liver microsomes. Biochemical Pharmacology 1999; 57(5)465–480
  • Rodrigues AD. Drug–drug interactions. Marcel Dekker, New York 2002
  • Salphati L, Benet LZ. Effects of ketoconazole on digoxin absorption and disposition in rat. Pharmacology 1998; 56(6)308–313
  • Shitara Y, Hirano M, Sato H, Sugiyama Y. Gemfibrozil and its glucuronide inhibit the organic anion transporting polypeptide 2 (OATP2/OATP1B1: SLC21A6)-mediated hepatic uptake and CYP2C8-mediated metabolism of cerivastatin: analysis of the mechanism of the clinically relevant drug–drug interaction between cerivastatin and gemfibrozil. Journal of Pharmacology and Experimental Therapeutics 2004; 311(1)228–236
  • Stouch TR, Gudmundsson O. Progress in understanding the structure–activity relationships of P-glycoprotein. Advances in Drug Delivery Reviews 2002; 54(3)315–328
  • Tang C, Fang Y, Booth-Genthe C, Kuo Y, Kuduk SD, Rushmore TH, Carr BA. Diclofenac hydroxylation in monkeys: efficiency, regioselectivity, and response to inhibitors. Biochemistry and Pharmacology 2007; 73(6)880–890
  • Thomas AR, Chan LN, Bauman JL, Olopade CO. Prolongation of the QT interval related to cisapride–diltiazem interaction. Pharmacotherapy 1998; 18(2)381–385
  • Thummel KE, Shen DD, Podoll TD, Kunze KL, Trager WF, Hartwell PS, Raisys VA, Marsh CL, McVicar JP, Barr DM, Perkins JD, Carithers RL. Use of midazolam as a human cytochrome P450 3A probe: I. In vitro–in vivo correlations in liver transplant patients. Journal of Pharmacology and Experimental Therapeutics 1994; 271(1)549–556
  • Thummel KE, Wilkinson GR. In vitro and in vivo drug interactions involving human CYP3A. Annual Reviews in Pharmacology and Toxicology 1998; 38: 389–430
  • Tsunoda SM, Velez RL, Von Moltke LL, Greenblatt DJ. Differentiation of intestinal and hepatic cytochrome P450 3A activity with use of midazolam as an in vivo probe: effect of ketoconazole. Clinical Pharmacology and Therapeutics 1999; 66(5)461–471
  • Venkatakrishnan K, Von Moltke LL, Greenblatt DJ. Effects of the antifungal agents on oxidative drug metabolism: clinical relevance. Clinical Pharmacokinetics 2000; 38(2)111–180
  • Wacher VJ, Silverman JA, Zhang Y, Benet LZ. Role of P-glycoprotein and cytochrome P450 3A in limiting oral absorption of peptides and peptidomimetics. Journal of Pharmaceutical Sciences 1998; 87(11)1322–1330
  • Wang EJ, Lew K, Casciano CN, Clement RP, Johnson WW. Interaction of common azole antifungals with P glycoprotein. Antimicrobial Agents and Chemotherapy 2002; 46(1)160–165
  • Ward KW, Stelman GJ, Morgan JA, Zeigler KS, Azzarano LM, Kehler JR, McSurdy-Freed JE, Proksch JW, Smith BR. Development of an in vivo preclinical screen model to estimate absorption and first-pass hepatic extraction of xenobiotics. II. Use of ketoconazole to identify P-glycoprotein/CYP3A-limited bioavailability in the monkey. Drug Metabolism and Disposition 2004; 32(2)172–177
  • Williams JA, Bauman J, Cai H, Conlon K, Hansel S, Hurst S, Sadagopan N, Tugnait M, Zhang L, Sahi J. In vitro ADME phenotyping in drug discovery: Current challenges and future solutions. Current Opinions in Drug Discovery and Development 2005; 8(1)78–88
  • Yamano K, Yamanoto K, Kotaki K, Sawada Y, Iga T. Quantitative prediction of metabolic inhibition of midazolam by itraconazole and ketoconazole in rats: Implication of concentrative uptake of inhibitors of into liver. Drug Metabolism and Disposition 1999; 27(3)395–402
  • Yamazaki M, Akiyama S, Ni’inuma K, Nishigaki R, Sugiyama Y. Biliary excretion of pravastatin in rats: Contribution of the excretion pathway mediated by canalicular multispecific organic anion transporter. Drug Metabolism and Disposition 1997; 25(10)1123–1129
  • Yamreudeewong W, DeBisschop M, Martin LG, Lower DL. Potentially significant drug interactions of class III antiarrhythmic drugs. Drug Safety 2003; 26(6)421–438
  • Yasuda K, Lan LB, Sanglard D, Furuya K, Schuetz JD, Schuetz EG. Interaction of cytochrome P450 3A inhibitors with P-glycoprotein. Journal of Pharmacology and Experimental Therapeutics 2002; 303(1)323–332
  • Yu DK. The contribution of P-glycoprotein to pharmacokinetic drug–drug interactions. Journal of Clinical Pharmacology 1999; 39(12)1203–1211
  • Zhang H, Zhang D, Li W, Yao M, D’Arienzo C, Li YX, Ewing WR, Gu Z, Zhu Y, Murugesan N, et al. Reduction of site-specific CYP3A-mediated metabolism for dual angiotensin and endothelin receptor antagonists in various in vitro systems and in cynomolgus monkeys. Drug Metabolism and Disposition 2007; 35(5)795–805

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.