1,791
Views
147
CrossRef citations to date
0
Altmetric
Research Article

Induction of hepatic cytochrome P450 enzymes: methods, mechanisms, recommendations, and in vitro–in vivo correlations

, &
Pages 1196-1224 | Received 22 May 2007, Accepted 25 Jun 2007, Published online: 22 Sep 2008

References

  • Allen SW, Mueller L, Williams SN, Quattrochi LC, Raucy J. The use of a high-volume screening procedure to assess the effects of dietary flavonoids on human CYP1A1 expression. Drug Metabolism and Disposition 2001; 29(8)1074–1079
  • Aninat C, Piton A, Glaise D, Le Charpentier T, Langouët S, Morel F, Guguen-Guillouzo C, Guillouzo A. Expression of cytochromes p450, conjugating enzymes and nuclear receptors in human hepatoma HepaRG cells. Drug Metabolism and Disposition 2006; 34: 75–83
  • Baes M, Gulick T, Choi H-S, Martinoli MG, Sihma D, Moore DD. A new orphan member of the nuclear harmone receptor sufer family that interacts with a subset of retiboic acid responses elements. Molecular and Cellular Biology 1994; 14: 1544–1552
  • Barwick JL, Quattrochi LC, Mills AS, Potenza C, Tukey RH, Guzelian PS. Trans-species gene transfer for analysis of glucocorticoid-inducible transcriptional activation of transiently expressed human CYP3A4 and rabbit CYP3A6 in primary cultures of adult rat and rabbit hepatocytes. Molecular Pharmacology 1996; 50(1)10–16
  • Berthiaume F, Moghe PV, Toner M, Yarmush ML. Effect of extracellular matrix topology on cell structure, function, and physiological responsiveness:hepatocytes cultured in a sandwich configuration. FASEB Journal 1996; 10(13)1471–1484
  • Bjornsson TD, Callaghan JT, Einolf HJ, Fischer V, Gan L, Grimm S, Kao J, King SP, Miwa G, Ni L, et al. Pharmaceutical Research and Manufacturers of America Drug Metabolism/Clinical Pharmacology Technical Working Groups. The conduct of in vitro and in vivo drug–drug interaction studies: a PhRMA perspective. Journal of Clinical Pharmacology 2003; 43(5)443–469
  • Choi HS, Chung M, Tzameli I, Simha D, Lee YK, Seol W, Moore DD. Differential transactivation by two isoforms of the orphan nuclear hormone receptor CAR. Journal of Biological Chemistry 1997; 272: 23565–23571
  • Connor K, Safe S, Jefcoate CR, Larsen M. Structure-dependent induction of CYP2B by polychlorinated biphenyl congeners in female Sprague–Dawley rats. Biochemistry and Pharmacology 1995; 50(11)1913–1920
  • Dai Y, Rashba-Step J, Cederbaum AI. Stable expression of human cytochrome P4502E1 in HepG2 cells: Characterization of catalytic activities and production of reactive oxygen intermediates. Biochemistry 1993; 32(27)6928–6937
  • Degawa M, Kobayashi K, Miura S, Arai H, Esumi H, Sugimura T, Hashimoto Y. Species difference among experimental rodents in induction of P450IA family enzymes by 2-amino-1-methyl-6-phenylimidazo[4,5-b]pyridine. Japanese Journal of Cancer Research 1992; 83(10)1047–1051
  • Diaz D, Fabre I, Daujat M, Saint Aubert B, Bories P, Michel H, Maurel P. Omeprazole is an aryl hydrocarbon-like inducer of human hepatic cytochrome P450. Gastroenterology 1990; 99(3)737–747
  • Dimaraki EV, Jaffe CA. Troglitazone induces CYP3A4 activity leading to falsely abnormal dexamethasone suppression test. Journal of Clinical Endocrinology and Metabolism 2003; 88(7)3113–3116
  • Drocourt L, Pascussi JM, Assenat E, Fabre JM, Maurel P, Vilarem MJ. Calcium channel modulators of the dihydropyridine family are human pregnane X receptor activators and inducers of CYP3A, CYP2B, and CYP2C in human hepatocytes. Drug Metabolism and Disposition 2001; 29(10)1325–1331
  • El-Sankary W, Gibson GG, Ayrton A, Plant N. Use of a reporter gene assay to predict and rank the potency and efficacy of CYP3A4 inducers. Drug Metabolism and Disposition 2001; 29(11)1499–1504
  • Fardel O, Jigorel E, Le Vee M, Payen L. Physiological, pharmacological and clinical features of the multidrug resistance protein 2. Biomedicine and Pharmacotherapy 2005; 59: 104–114
  • Faucette SR, Sueyoshi T, Smith CM, Negishi M, LeCluyse EL, Wang H. Differential regulation of hepatic CYP2B6 and CYP3A4 genes by constitutive androstane receptor but not pregnane X receptor. Journal of Pharmacology and Experimental Therapeutics 2006; 317(3)1200–1209
  • Faucette SR, Wang H, Hamilton GA, Jolley SL, Gilbert D, Lindley C, Yan B, Negishi M, LeCluyse EL. Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers. Drug Metabolism and Disposition 2004; 32(3)348–358
  • Faucette SR, Zhang TC, Moore R, Sueyoshi T, Omiecinski CJ, LeCluyse EL, Negishi M, Wang H. Relative activation of human pregnane X receptor versus constitutive androstane receptor defines distinct classes of CYP2B6 and CYP3A4 inducers. Journal of Pharmacology and Experimental Therapeutics 2007; 320(1)72–80
  • Ferrini JB, Pichard L, Domergue J, Maurel P. Long-term primary cultures of adult human hepatocytes. Chemico-Biological Interactions 1997; 107: 31–45
  • Fontaine SM, Hoyer PB, Halpert JR, Sipes IG. Role of induction of specific hepatic cytochrome P450 isoforms in epoxidation of 4-vinylcyclohexene. Drug Metabolism and Disposition 2001; 29(9)1236–1242
  • Funck-Brentano C, Raphael M, Lafontaine M, Arnould JP, Verstuyft C, Lebot M, Costagliola D, Roussel R. Effects of type of smoking (pipe, cigars or cigarettes) on biological indices of tobacco exposure and toxicity. Lung Cancer 2006; 54(1)11–18
  • Garcia M, Rager J, Wang Q, Strab R, Hidalgo IJ, Owen A, Li J. Cryopreserved human hepatocytes as alternative in vitro model for cytochrome p450 induction studies. In Vitro Cellular and Developmental Biology — Animal 2003; 39(7)283–287
  • Geick A, Eichelbaum M, Burk O. Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. Journal of Biological Chemistry 2001; 276: 14581–14587
  • Gerbal-Chaloin S, Pascussi JM, Pichard-Garcia L, Daujat M, Waechter F, Fabre JM, Carrere N, Maurel P. Induction of CYP2C genes in human hepatocytes in primary culture. Drug Metabolism and Disposition 2001; 29(3)242–251
  • Goff DA, Spunt AL, Jung D, Bellur SN, Fischer JH. Absorption characteristics of three phenytoin sodium products after administration of oral loading doses. Clinical Pharmacology 1984; 3(6)634–638
  • Gómez-Lechón MJ, Donato MT, Castell JV, Jover R. Human hepatocytes in primary culture: The choice to investigate drug metabolism in man. Current Drug Metabolism 2004; 5(5)443–462
  • Goodwin B, Hodgson E, Liddle C. The orphan human pregnane X receptor mediates the transcriptional activation of CYP3A4 by rifampicin through a distal enhancer module. Molecular Pharmacology 1999; 56(6)1329–1339
  • Goodwin B, Moore LB, Stoltz CM, McKee DD, Kliewer SA. Regulation of the human CYP2B6 gene by the nuclear pregnane X receptor. Molecular Pharmacology 2001; 60(3)427–431
  • Greuet J, Pichard L, Ourlin JC, Bonfils C, Domergue J, Le Treut P, Maurel P. Effect of cell density and epidermal growth factor on the inducible expression of CYP3A and CYP1A genes in human hepatocytes in primary culture. Hepatology 1997; 25(5)1166–1175
  • Guengerich FP, Shimada T, Iwasaki M, Butler MA, Kadlubar FF. Activation of carcinogens by human liver cytochromes P-450. Basic Life Sciences 1990; 53: 381–396
  • Harris RZ, Inglis AM, Miller AK, Thompson KA, Finnerty D, Patterson S, Jorkasky DK, Freed MI. Rosiglitazone has no clinically significant effect on nifedipine pharmacokinetics. Journal of Clinical Pharmacology 1999; 39(11)1189–1194
  • Hebert MF, Roberts JP, Prueksaritanont T, Benet LZ. Bioavailability of cyclosporine with concomitant RIF administration is markedly less than predicted by hepatic enzyme induction. Clinical Pharmacology and Therapeutics 1992; 52(5)453–457
  • Hewitt NJ, De Kanter R, LeCluyse E. a. Induction of drug metabolizing enzymes: A survey of in vitro methodologies and interpretations used in the pharmaceutical industry — do they comply with FDA recommendations?. Chemico-Biological Interactions 2007; 168(1)51–65
  • Hewitt NJ, Gomez-Lechon MJ, Houston JB, Hallifax D, Brown HS, Maurel P, Kenna JG, Gustavsson L, Lohmann C, Skonberg C, et al. Primary hepatocytes: Current understanding of the regulation of metabolic enzymes and transporter proteins, and pharmaceutical practice for the use of hepatocytes in metabolism, enzyme induction, transporter, clearance, and hepatotoxicity studies. Drug Metabolism Reviews 2007b; 39(1)159–234
  • Hewitt NJ, Hewitt P. Phase I and II enzyme characterization of two sources of HepG2 cell lines. Xenobiotica 2004; 34(3)243–256
  • Holt RJ. Topical pharmacology of imidazole antifungals. Journal of Cutaneous Pathology 1976; 3(1)45–59
  • Honkakoski P, Sueyoshi T, Negishi M. Drug-activated nuclear receptors CAR and PXR. Annals of Medicine 2003; 35(3)172–182
  • Huang S-M. Drug interaction studies — study design, data analysis, and implications for dosing and labelling. 2004, Preliminary Concept Paper
  • Huang S-M, Stifano T. Guidance for industry: Drug interaction studies — study design, data analysis, and implications for dosing and labelling. 2006, Draft Guidance
  • Jackson JP, Ferguson SS, Negishi M, Goldstein JA. Phenytoin induction of the cyp2c37 gene is mediated by the constitutive androstane receptor. Drug Metabolism and Disposition 2006; 34(12)2003–2010
  • Jigorel E, Le Vee M, Boursier-Neyret C, Parmentier Y, Fardel O. Differential regulation of sinusoidal and canalicular hepatic drug transporter expression by xenobiotics activating drug-sensing receptors in primary human hepatocytes. Drug Metabolism and Disposition 2006; 34(10)1756–1763
  • Jones SA, Moore LB, Shenk JL, Wisely GB, Hamilton GA, McKee DD, Tomkinson NC, LeCluyse EL, Lambert MH, Willson TM, et al. The pregnane X receptor: A promiscuous xenobiotic receptor that has diverged during evolution. Molecular Endocrinology 2000; 14(1)27–39
  • Jover R, Bort R, Gomez-Lechon MJ, Castell JV. Re-expression of C/EBP alpha induces CYP2B6, CYP2C9 and CYP2D6 genes in HepG2 cells. FEBS Letters 1998; 431(2)227–230
  • Juan D, Worwag EM, Schoeller DA, Kotake AN, Hughes RL, Frederiksen MC. Effects of dietary protein on theophylline pharmacokinetics and caffeine and aminopyrine breath tests. Clinical Pharmacology and Therapeutics 1986; 40(2)187–194
  • Kafert-Kasting S, Alexandrova K, Barthold M, Laube B, Friedrich G, Arseniev L, Hengstler JG. Enzyme induction in cryopreserved human hepatocyte cultures. Toxicology 2006; 220(2–3)117–125
  • Kall MA, Vang O, Clausen J. Effects of dietary broccoli on human in vivo drug metabolizing enzymes: Evaluation of caffeine, oestrone and chlorzoxazone metabolism. Carcinogenesis 1996; 17(4)793–799
  • Kato M, Chiba K, Horikawa M, Sugiyama Y. The quantitative prediction of in vivo enzyme-induction caused by drug exposure from in vitro information on human hepatocytes. Drug Metabolism and Pharmacokinetics 2005; 20(4)236–243
  • Kawamoto T, Sueyoshi T, Zelko I, Moore R, Washburn K, Negishi M. Phenobarbital-responsive nuclear translocation of the receptor CAR in induction of the CYP2B gene. Molecular and Cellular Biology 1999; 19(9)6318–6322
  • Kawana K, Ikuta T, Kobayashi Y, Gotoh O, Takeda K, Kawajiri K. Molecular mechanism of nuclear translocation of an orphan nuclear receptor, SXR. Molecular Pharmacology 2003; 63(3)524–531
  • Klaassen CD, Slitt AL. Regulation of hepatic transporters by xenobiotic receptors. Current Drug Metabolism 2005; 6: 309–328
  • Kostrubsky VE, Lewis LD, Strom SC, Wood SG, Schuetz EG, Schuetz JD, Sinclair PR, Wrighton SA, Sinclair JF. Induction of cytochrome P4503A by taxol in primary cultures of human hepatocytes. Archives in Biochemical Biophysics 1999; 355(2)131–136
  • Lambert GH, Needham LL, Turner W, Lai TJ, Patterson DG, Guo YL. Induced CYP1A2 activity as a phenotypic biomarker in humans highly exposed to certain PCBs/PCDFs. Environmental Science and Technology 2006; 40(19)6176–6180
  • Larsen JT, Brøsen K. Consumption of charcoal-broiled meat as an experimental tool for discerning CYP1A2-mediated drug metabolism in vivo. Basic and Clinical Pharmacology and Toxicology 2005; 97(3)141–148
  • LeCluyse EL. Human hepatocyte culture systems for the in vitro evaluation of cytochrome P450 expression and regulation. European Journal of Pharmaceutical Sciences 2001; 13(4)343–368
  • LeCluyse EL, Bullock P, Madan A, Carroll K, Parkinson A. Influence of extracellular matrix overlay and medium formulation on the induction of cytochrome p-450 2b enzymes in primary cultures of rat hepatocytes. Drug Metabolism and Disposition 1999; 27(8)909–915
  • LeCluyse EL, Madan A, Hamilton G, Carroll K, DeHaan R, Parkinson A. Expression and regulation of cytochrome P450 enzymes in primary cultures of human hepatocytes. Journal of Biochemical and Molecular Toxicology 2000; 14(4)177–188
  • Lehmann JM, McKee DD, Watson MA, Willson TM, Moore JT, Kliewer SA. The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. Journal of Clinical Investigation 1998; 102(5)1016–1023
  • Li AP, Maurel P, Gomez-Lechon MJ, Cheng LC, Jurima-Romet M. Preclinical evaluation of drug–drug interaction potential: Present status of the application of primary human hepatocytes in the evaluation of cytochrome P450 induction. Chemico-Biological Interactions 1997; 107(1–2)5–16
  • Li W, Harper PA, Tang BK, Okey AB. Regulation of cytochrome P450 enzymes by aryl hydrocarbon receptor in human cells: CYP1A2 expression in the LS180 colon carcinoma cell line after treatment with 2,3,7,8-tetrachlorodibenzo-p-dioxin or 3-methylcholanthrene. Biochemical Pharmacology 1998; 56(5)599–612
  • Li Z, Seeram NP, Lee R, Thames G, Minutti C, Wang HJ, Heber D. Plasma clearance of lovastatin versus Chinese red yeast rice in healthy volunteers. Journal of Alternative and Complementary Medicine 2005; 11(6)1031–1038
  • Lin JH. CYP induction-mediated drug interactions: In vitro assessment and clinical implications. Pharmaceutical Research 2006; 23(6)1089–1116
  • Lin JH, Wong BK. Complexities of glucuronidation affecting in vitro in vivo extrapolation. Current Drug Metabolism 2002; 3(6)623–646
  • Lindros KO, Oinonen T, Kettunen E, Sippel H, Muro-Lupori C, Koivusalo M. Aryl hydrocarbon receptor-associated genes in rat liver: Regional coinduction of aldehyde dehydrogenase 3 and glutathione transferase Ya. Biochemical Pharmacology 1998; 55(4)413–421
  • Loi CM, Randinitis EJ, Vassos AB, Kazierad DJ, Koup JR, Sedman AJ. Lack of effect of type II diabetes on the pharmacokinetics of troglitazone in a multiple-dose study. Journal of Clinical Pharmacology 1997; 37(12)1114–1120
  • Lu C, Li AP. Species comparison in P450 induction: Effects of dexamethasone, omeprazole, and rifampin on P450 isoforms 1A and 3A in primary cultured hepatocytes from man, Sprague–Dawley rat, minipig, and beagle dog. Chemico-Biological Interactions 2001; 134(3)271–281
  • Luo G, Cunningham M, Kim S, Burn T, Lin J, Sinz M, Hamilton G, Rizzo C, Jolley S, Gilbert D, et al. CYP3A4 induction by drugs: correlation between a pregnane X receptor reporter gene assay and CYP3A4 expression in human hepatocytes. Drug Metabolism and Disposition 2002; 30(7)795–804
  • Madabushi R, Frank B, Drewelow B, Derendorf H, Butterweck V. Hyperforin in St. John's wort drug interactions. European Journal of Clinical Pharmacology 2006; 62(3)225–233
  • Madan A, Graham RA, Carroll KM, Mudra DR, Burton LA, Krueger LA, Downey AD, Czerwinski M, Forster J, Ribadeneira MD, et al. Effects of prototypical microsomal enzyme inducers on cytochrome P450 expression in cultured human hepatocytes. Drug Metabolism and Disposition 2003; 31(4)421–431
  • Maglich JM, Parks DJ, Moore LB, Collins JL, Goodwin B, Billin AN, Stoltz CA, Kliewer SA, Lambert MH, Willson TM, et al. Identification of a novel human constitutive androstane receptor (CAR) agonist and its use in the identification of CAR target genes. Journal of Biological Chemistry 2003; 278(19)17277–17283
  • Mahmood I, Chamberlin N. A limited sampling method for the estimation of AUC and Cmax of carbamazepine and carbamazepine epoxide following a single and multiple dose of a sustained-release product. British Journal of Clinical Pharmacology 1998; 45(3)241–246
  • Masuyama H, Suwaki N, Tateishi Y, Nakatsukasa H, Segawa T, Hiramatsu Y. The pregnane X receptor regulates gene expression in a ligand- and promoter-selective fashion. Molecular Endocrinology 2005; 19(5)1170–1180
  • Maurel P. The use of adult human hepatocytes in primary culture and other in vitro systems to investigate drug metabolism in man. Advanced Drug Delivery Reviews 1996; 22(1)105–132
  • McCune JS, Hawke RL, LeCluyse EL, Gillenwater HH, Gillenwater HH, Hamilton GA, Ritchie J, Lindley C. In-vivo and in-vitro induction of human cytochrome P450 3A4 by dexamethasone. Clinical and Pharmacology Therapy 2000; 68: 356–366
  • McDonnell WM, Scheiman JM, Traber PG. Induction of cytochrome P450IA genes (CYP1A) by omeprazole in the human alimentary tract. Gastroenterology 1992; 103(5)1509–1516
  • Meunier V, Bourrie M, Julian B, Marti E, Guillou F, Berger Y, Fabre G. Expression and induction of CYP1A1/1A2, CYP2A6 and CYP3A4 in primary cultures of human hepatocytes: A 10-year follow-up. Xenobiotica 2000; 30(6)589–607
  • Moore LB, Maglich JM, McKee DD, Wisely B, Willson TM, Kliewer SA, Lambert MH, Moore JT. Pregnane X receptor (PXR), constitutive androstane receptor (CAR), and benzoate X receptor (BXR) define three pharmacologically distinct classes of nuclear receptors. Molecular Endocrinology 2002; 16(5)977–986
  • Moore LB, Parks DJ, Jones SA, Bledsoe RK, Consler TG, Stimmel JB, Goodwin B, Liddle C, Blanchard SG, Willson TM, et al. Orphan nuclear receptors constitutive androstane receptor and pregnane X receptor share xenobiotic and steroid ligands. Journal of Biological Chemistry 2000; 275(20)15122–15127
  • Morgan ET. Regulation of cytochrome p450 by inflammatory mediators: why and how?. Drug Metabolism and Disposition 2001; 29(3)207–212, erratum 29(6):932
  • Nishimura M, Koeda A, Suzuki E, Kawano Y, Nakayama M, Satoh T, Narimatsu S, Naito S. Regulation of mRNA expression of MDR1, MRP1, MRP2 and MRP3 by prototypical microsomal enzyme inducers in primary cultures of human and rat hepatocytes. Drug Metabolism and Pharmacokinetics 2006; 21(4)297–307
  • Novak RF, Woodcroft KJ. The alcohol-inducible form of cytochrome P450 (CYP 2E1): Role in toxicology and regulation of expression. Archives of Pharmaceutical Research 2000; 23(4)267–282
  • Pantuck EJ, Pantuck CB, Garland WA, Min BH, Wattenberg LW, Anderson KE, Kappas A, Conney AH. Stimulatory effect of Brussels sprouts and cabbage on human drug metabolism. Clinical Pharmacology and Therapeutics 1979; 25(1)88–95
  • Parkinson A, Mudra DR, Johnson C, Dwyer A, Caroll KM. The effects of gender, age, ethnicity, and liver cirrhosis on cytochrome P450 enzyme activity in human liver microsomes and inducibility in cultured human hepatocytes. Toxicology and Applied Pharmacology 2004; 199: 193–209
  • Pascussi JM, Drocourt L, Fabre JM, Maurel P, Vilarem MJ. Dexamethasone induces pregnane X receptor and retinoid X receptor-alpha expression in human hepatocytes: Synergistic increase of CYP3A4 induction by pregnane X receptor activators. 2000a; 58(2)361–372
  • Pascussi JM, Gerbal-Chaloin S, Fabre JM, Maurel P, Vilarem MJ. Dexamethasone enhances constitutive androstane receptor expression in human hepatocytes: Consequences on cytochrome P450 gene regulation. Molecular Pharmacology 2000b; 58(6)1441–1450
  • Pascussi JM, Jounaidi Y, Drocourt L, Domergue J, Balabaud C, Maurel P, Vilarem MJ. Evidence for the presence of a functional pregnane X receptor response element in the CYP3A7 promoter gene. Biochemical and Biophysical Research Communications 1999; 260(2)377–381
  • Rae JM, Johnson MD, Lippman ME, Flockhart DA. Rifampin is a selective, pleiotropic inducer of drug metabolism genes in human hepatocytes: Studies with cDNA and oligonucleotide expression arrays. Journal of Pharmacology and Experimental Therapeutics 2001; 299(3)849–857
  • Raucy JL, Lasker J, Ozaki K, Zoleta V. Regulation of CYP2E1 by ethanol and palmitic acid and CYP4A11 by clofibrate in primary cultures of human hepatocytes. Toxicological Sciences 2004; 79(2)233–241
  • Richter CA, Tillitt DE, Hannink M. Regulation of subcellular localization of the aryl hydrocarbon receptor (AhR). Archives of Biochemistry and Biophysics 2001; 389(2)207–217
  • Riley RJ, Grime K, Weaver R. Time-dependent CYP inhibition. Expert Opinion on Drug Metabolism and Toxicology 2007; 3(1)51–66
  • Ripp SL, Mills JB, Fahmi OA, Trevena KA, Liras JL, Maurer TS, De Morais SM. Use of immortalized human hepatocytes to predict the magnitude of clinical drug–drug interactions caused by CYP3A4 induction. Drug Metabolism and Disposition 2006; 34(10)1742–1748
  • Rizzo N, Hispard E, Dolbeault S, Dally S, Leverge R, Girre C. Impact of long-term ethanol consumption on CYP1A2 activity. Clinical Pharmacology and Therapeutics 1997; 62(5)505–509
  • Robertson P, DeCory HH, Madan A, Parkinson A. In vitro inhibition and induction of human hepatic cytochrome P450 enzymes by modafinil. Drug Metabolism and Disposition 2000; 28(6)664–671
  • Rost KL, Brosicke H, Scheffler M, Roots I. Dose dependent induction of CYP1A2 activity by omeprazole (Antra). International Journal of Clinical Pharmacology and Therapeutic Toxicology 1992; 30(11)542–543
  • Rost KL, Roots I. Accelerated caffeine metabolism after omeprazole treatment is indicated by urinary metabolite ratios: Coincidence with plasma clearance and breath test. Clinical Pharmacology and Therapeutics 1994; 55(4)402–411
  • Roymans D, Annaert P, Van Houdt J, Weygers A, Noukens J, Sensenhauser C, Silva J, Van Looveren C, Hendrickx J, Mannens G, et al. Expression and induction potential of cytochromes P450 in human cryopreserved hepatocytes. Drug Metabolism and Disposition 2005; 33(7)1004–1016
  • Roymans D, Van Looveren C, Leone A, Parker JB, McMillian M, Johnson MD, Koganti A, Gilissen R, Silber P, Mannens G, et al. Determination of cytochrome P450 1A2 and cytochrome P450 3A4 induction in cryopreserved human hepatocytes. Biochemical Pharmacology 2004; 67(3)427–437
  • Ruegg CE, Silber PM, Mughal RA, Ismail J, Lu C, Bode DC, Li AP. Cytochrome-P450 induction and conjugated metabolism in primary human hepatocytes after cryopreservation. In Vitro Technologies 1997; 10: 217–222
  • Sidhu JS, Farin FM, Omiecinski CJ. Influence of extracellular matrix overlay on phenobarbital-mediated induction of CYP2B1, 2B2, and 3A1 genes in primary adult rat hepatocyte culture. Archives of Biochemistry and Biophysics 1993; 301(1)103–113
  • Silva JM, Day SH, Nicoll-Griffith DA. Induction of cytochrome-P450 in cryopreserved rat and human hepatocytes. Chemico-Biological Interactions 1999; 121: 49–63
  • Silva JM, Morin PE, Day SH, Kennedy BP, Payette P, Rushmore T, Yergey JA, Nicoll-Griffith DA. Refinement of an in vitro cell model for cytochrome P450 induction. Drug Metabolism and Disposition 1998; 26(5)490–496
  • Smirlis D, Muangmoonchai R, Edwards M, Phillips IR, Shephard EA. Orphan receptor promiscuity in the induction of cytochromes p450 by xenobiotics. Journal of Biological Chemistry 2001; 276(16)12822–12826
  • Smith CM, Graham RA, Krol WL, Silver IS, Negishi M, Wang H, LeCluyse EL. Differential UGT1A1 induction by chrysin in primary human hepatocytes and HepG2 Cells. Journal of Pharmacology and Experimental Therapeutics 2005; 315(3)1256–1264
  • Smith DA, Dickins M, Fahmi OA, Iwasaki K, Lee C, Obach RS, Padbury G, De Morais SM, Ripp SL, Stevens J, et al. The time to move cytochrome p450 induction into mainstream pharmacology is long overdue. Drug Metabolism and Disposition 2007; 35(4)697–698
  • Squires EJ, Sueyoshi T, Negishi M. Cytoplasmic localization of pregnane X receptor and ligand-dependent nuclear translocation in mouse liver. Journal of Biological Chemistry 2004; 279(47)49307–49314
  • Sueyoshi T, Kawamoto T, Zelko I, Honkakoski P, Negishi M. The repressed nuclear receptor CAR responds to phenobarbital in activating the human CYP2B6 gene. Journal of Biological Chemistry 1999; 274(10)6043–6046
  • Takikawa H. Hepatobiliary transport of bile acids and organic anions. Journal of Hepatobiliary Pancreatic Surgery 2002; 9(4)443–447
  • Tang C, Lin JH, Lu AYH. Metabolism-based drug–drug interactions: What determines individual variability in cytochrome P450 induction?. Drug Metabolism and Disposition 2005; 33: 603–613
  • Thompson-Culkin K, Zussman B, Miller AK, Freed MI. Pharmacokinetics of rosiglitazone in patients with end-stage renal disease. Journal of International Medical Research 2002; 30(4)391–399
  • Tirona RG, Leake BF, Wolkoff AW, Kim RB. Human organic anion transporting polypeptide-C (SLC21A6) is a major determinant of rifampin-mediated pregnane X receptor activation. Journal of Pharmacology and Experimental Therapeutics 2003; 304(1)223–228
  • Toal CB. Formulation dependent pharmacokinetics — does the dosage form matter for nifedipine?. Journal of Cardiovascular Pharmacology 2004; 44(1)82–86
  • Tucker GT, Houston JB, Huang SM. Optimizing drug development: strategies to assess drug metabolism/transporter interaction potential — toward a consensus. Pharmaceutical Research 2001; 18(8)1071–1080
  • Tuschl G, Mueller SO. Effects of cell culture conditions on primary rat hepatocytes-cell morphology and differential gene expression. Toxicology 2006; 218(2–3)205–215
  • Vora J, Stern R, Lathia C. Clinical pharmacokinetics of CI-1011, an ACAT inhibitor. Pharmaceutical Research (NY) 1997; 14: S505
  • Vyhlidal CA, Gaedigk R, Leeder JS. Nuclear receptor expression in fetal and pediatric liver: Correlation with CYP3A expression. Drug Metabolism and Disposition 2006; 34(1)131–137
  • Walgren JL, Mitchell MD, Thompson DC. Role of metabolism in drug-induced idiosyncratic hepatotoxicity. Critical Reviews in Toxicology 2005; 35(4)325–331
  • Wang H, Faucette S, Moore R, Sueyoshi T, Negishi M, LeCluyse E. Human constitutive androstane receptor mediates induction of CYP2B6 gene expression by phenytoin. Journal of Biological Chemistry 2004; 279(28)29295–29301
  • Wang H, LeCluyse EL. Role of orphan nuclear receptors in the regulation of drug-metabolising enzymes. Clinical Pharmacokinetics 2003; 42(15)1331–1357
  • Watanabe H, Kosuge K, Nishio S, Yamada H, Uchida S, Satoh H, Hayashi H, Ishizaki T, Ohashi K. Pharmacokinetic and pharmacodynamic interactions between simvastatin and diltiazem in patients with hypercholesterolemia and hypertension. Life Sciences 2004; 76(3)281–292
  • Waxman DJ, Pampori NA, Ram PA, Agrawal AK, Shapiro BH. Interpulse interval in circulating growth hormone patterns regulates sexually dimorphic expression of hepatic cytochrome P450. Proceedings of the National Academy of Sciences of the United States of America 1991; 88(15)6868–6872
  • White IN, Davies A, Smith LL, Dawson S, De Matteis F. Induction of CYP2B1 and 3A1, and associated monoxygenase activities by tamoxifen and certain analogues in the livers of female rats and mice. Biochemical Pharmacology 1993; 45(1)21–30
  • Wilkening S, Stahl F, Bader A. Comparison of primary human hepatocytes and hepatoma cell line Hepg2 with regard to their biotransformation properties. Drug Metabolism and Disposition 2003; 31(8)1035–1042
  • Williams A, Ellis A, Ribadeneira MD, Otmani S, Grimm S, Obusek M, Ferguson SS, LeCluyse EL. Evaluation of gene expression differences between FA2N-4 cells and cultured human hepatocytes using Affymetrix HGU1332.0 gene chips. Drug Metabolism Reviews 2006; 38(2)117–118
  • Xie W, Barwick JL, Simon CM, Pierce AM, Safe S, Blumberg B, Guzelian PS, Evans RM. Reciprocal activation of xenobiotic response genes by nuclear receptors SXR/PXR and CAR. Genes and Development 2000; 14(23)3014–3023
  • Xu C, Li CY, Kong AN. Induction of phase I, II and III drug metabolism/transport by xenobiotics. Archives in Pharmaceutical Research 2005; 28(3)249–268
  • Yoshitomi S, Ikemoto K, Takahashi J, Miki H, Namba M, Asahi S. Establishment of the transformants expressing human cytochrome P450 subtypes in HepG2, and their applications on drug metabolism and toxicology. Toxicology In Vitro 2001; 15(3)245–256
  • Zhang H, LeCulyse E, Liu L, Hu M, Matoney L, Zhu W, Yan B. Rat pregnane X receptor: Molecular cloning, tissue distribution, and xenobiotic regulation. Archives of Biochemical Biophysics 1999; 368(1)14–22
  • Zhou J, Zhang J, Xie W. Xenobiotic nuclear receptor-mediated regulation of UDP-glucuronosyl-transferases. Current Drug Metabolism 2005; 6(4)289–298
  • Zuber R, Anzenbacherova E, Anzenbacher P. Cytochromes P450 and experimental models of drug metabolism. Journal of Cellular and Molecular Medicine 2002; 6(2)189–198

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.