Application of a substrate cocktail approach in the assessment of cytochrome P450 induction using cultured human hepatocytes

Journal of Biomolecular Screening

Volumn 18, Issue 2, 2013, Pages 199-210

  Pelletier, Robert D ^a,b   Lai, W George ^a   Wong, Y Nancy ^a  

^a EISAI INC   (United States)

^b UNIVERSITY OF WASHINGTON   (United States)

Author keywords

CYP induction; drug drug interaction; high throughput screening

Indexed keywords

BETA NAPHTHOFLAVONE; CARBAMAZEPINE; CLOZAPINE; CYTOCHROME P450; CYTOCHROME P450 1A; CYTOCHROME P450 2B6; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; IBUPROFEN; MESSENGER RNA; METOPROLOL; MEVINOLIN; MIDAZOLAM; NEVIRAPINE; OMEPRAZOLE; PHENOBARBITAL; PHENYTOIN; RIFAMPICIN; RITONAVIR; TROGLITAZONE;

ARTICLE; CELL COUNT; CELL VIABILITY; CONTROLLED STUDY; CYTOTOXICITY; DRUG POTENCY; ENZYME ACTIVITY; ENZYME INDUCTION; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL; HUMAN CELL CULTURE; LIVER CELL; LIVER CELL CULTURE; PRIORITY JOURNAL; PROTEIN FOLDING; REAL TIME POLYMERASE CHAIN REACTION;

CELLS, CULTURED; CYTOCHROME P-450 ENZYME SYSTEM; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; ENZYME ACTIVATION; GENE EXPRESSION REGULATION; HEPATOCYTES; HUMANS; RIFAMPIN; SUBSTRATE SPECIFICITY;

EID: 84872573356     PISSN: 10870571     EISSN: 1552454X     Source Type: Journal    
DOI: 10.1177/1087057112463732     Document Type: Article

References (30)

1. Guengerich F. P.. Cytochrome p450 and Chemical Toxicology. Chem. Res. Toxicol. 2008 ; 21 (1). 70-83
2. Lin J. H.. CYP Induction-Mediated Drug Interactions: In Vitro Assessment and Clinical Implications. Pharm. Res. 2006 ; 23 (6). 1089-1116
3. Hardwick J. P., Gonzalez F. J., Kasper C. B.. Transcriptional Regulation of Rat Liver Epoxide Hydratase, NADPH-Cytochrome P-450 Oxidoreductase, and Cytochrome P-450b Genes by Phenobarbital. J. Biol. Chem. 1983 ; 258 (13). 8081-8085
4. Parsons W. D., Neims A. H.. Effect of Smoking on Caffeine Clearance. Clin. Pharmacol. Ther. 1978 ; 24 (1). 40-45
5. Li A. P., Reith M. K., Rasmussen A., Gorski J. C., Hall S. D., Xu L., Kaminski D. L., Cheng L. K.. Primary Human Hepatocytes as a Tool for the Evaluation of Structure-Activity Relationship in Cytochrome P450 Induction Potential of Xenobiotics: Evaluation of Rifampin, Rifapentine and Rifabutin. Chem. Biol. Interact. 1997 ; 107 (1-2). 17-30
6. Sueyoshi T., Negishi M.. Phenobarbital Response Elements of Cytochrome P450 Genes and Nuclear Receptors. Annu. Rev. Pharmacol. Toxicol. 2001 ; 41: 123-143
7. Chen S., Wang K., Wan Y. J.. Retinoids Activate RXR/CAR-Mediated Pathway and Induce CYP3A. Biochem. Pharmacol. 2010 ; 79 (2). 270-276
8. Pelkonen O., Turpeinen M., Hakkola J., Honkakoski P., Hukkanen J., Raunio H.. Inhibition and Induction of Human Cytochrome P450 Enzymes: Current Status. Arch. Toxicol. 2008 ; 82 (10). 667-715
9. Chu V., Einolf H. J., Evers R., Kumar G., Moore D., Ripp S., Silva J., Sinha V., Sinz M., Skerjanec A.. In Vitro and In Vivo Induction of Cytochrome p450: A Survey of the Current Practices and Recommendations: A Pharmaceutical Research and Manufacturers of America Perspective. Drug Metab. Dispos. 2009 ; 37 (7). 1339-1354
10. Fahmi O. A., Kish M., Boldt S., Obach R. S.. Cytochrome P450 3A4 mRNA Is a More Reliable Marker Than CYP3A4 Activity for Detecting Pregnane X Receptor-Activated Induction of Drug-Metabolizing Enzymes. Drug Metab. Dispos. 2010 ; 38 (9). 1605-1611
11. Mugundu G. M., Hariparsad N., Desai P. B.. Impact of Ritonavir, Atazanavir and Their Combination on the CYP3A4 Induction Potential of Efavirenz in Primary Human Hepatocytes. Drug Metab. Lett. 2010 ; 4 (1). 45-50
12. Walsky R. L., Obach R. S.. Validated Assays for Human Cytochrome P450 Activities. Drug Metab. Dispos. 2004 ; 32 (6). 647-660
13. Feidt D. M., Klein K., Hofmann U., Riedmaier S., Knobeloch D., Thasler W. E., Weiss T. S., Schwab M., Zanger U. M.. Profiling Induction of Cytochrome p450 Enzyme Activity by Statins Using a New Liquid Chromatography-Tandem Mass Spectrometry Cocktail Assay in Human Hepatocytes. Drug Metab. Dispos. 2010 ; 38 (9). 1589-1597
14. Lahoz A., Donato M. T., Picazo L., Castell J. V., Gómez- Lechón M. J.. Assessment of Cytochrome P450 Induction in Human Hepatocytes Using the Cocktail Strategy plus Liquid Chromatography Tandem Mass Spectrometry. Drug Metab. Lett. 2008 ; 2 (3). 205-209
15. Rhodes S. P., Otten J. N., Hingorani G. P., Hartley D. P., Franklin R. B.. Simultaneous Assessment of Cytochrome P450 Activity in Cultured Human Hepatocytes for Compound-Mediated Induction of CYP3A4, CYP2B6, and CYP1A2. J. Pharmacol. Toxicol. Methods. 2011 ; 63 (3). 223-226
16. Cawley G. F., Batie C. J., Backes W. L.. Substrate-Dependent Competition of Different P450 Isozymes for Limiting NADPH-Cytochrome P450 Reductase. Biochemistry. 1995 ; 34 (4). 1244-1247
17. Nishimura M., Koeda A., Suganuma Y., Suzuki E., Shimizu T., Nakayama M., Satoh T., Narimatsu S., Naito S.. Comparison of Inducibility of CYP1A and CYP3A mRNAs by Prototypical Inducers in Primary Cultures of Human, Cynomolgus Monkey, and Rat Hepatocytes. Drug Metab. Pharmacokinet. 2007 ; 22 (3). 178-186
18. Maglich J. M., Stoltz C. M., Goodwin B., Hawkins-Brown D., Moore J. T., Kliewer S. A.. Nuclear Pregnane X Receptor and Constitutive Androstane Receptor Regulate Overlapping but Distinct Sets of Genes Involved in Xenobiotic Detoxification. Mol. Pharmacol. 2002 ; 62 (3). 638-646
19. Wang H., Li H., Moore L. B., Johnson M. D., Maglich J. M., Goodwin B., Ittoop O. R., Wisely B., Creech K., Parks D. J., et al. The Phytoestrogen Coumestrol Is a Naturally Occurring Antagonist of the Human Pregnane X Receptor. Mol. Endocrinol. 2008 ; 22 (4). 838-857
20. Lim Y. P., Kuo S. C., Lai M. L., Huang J. D.. Inhibition of CYP3A4 Expression by Ketoconazole Is Mediated by the Disruption of Pregnane X Receptor, Steroid Receptor Coactivator-1, and Hepatocyte Nuclear Factor 4alpha Interaction. Pharmacogenet. Genomics. 2009 ; 19 (1). 11-24
21. Zhou C., Poulton E. J., Grün F., Bammler T. K., Blumberg B., Thummel K. E., Eaton D. L.. The Dietary Isothiocyanate Sulforaphane Is an Antagonist of the Human Steroid and Xenobiotic Nuclear Receptor. Mol. Pharmacol. 2007 ; 71 (1). 220-229
22. Podvinec M., Handschin C., Looser R., Meyer U. A.. Identification of the Xenosensors Regulating Human 5-Aminolevulinate Synthase. Proc. Natl. Acad. Sci. U. S. A. 2004 ; 101 (24). 9127-9132
23. Ulbrichova D., Hrdinka M., Saudek V., Martasek P.. Acute Intermittent Porphyria - Impact of Mutations Found in the Hydroxymethylbilane Synthase Gene on Biochemical and Enzymatic Protein Properties. FEBS J. 2009 ; 276 (7). 2106-2115
24. Curi-Pedrosa R., Daujat M., Pichard L., Ourlin J. C., Clair P., Gervot L., Lesca P., Domergue J., Joyeux H., Fourtanier G.. Omeprazole and Lansoprazole Are Mixed Inducers of CYP1A and CYP3A in Human Hepatocytes in Primary Culture. J. Pharmacol. Exp. Ther. 1994 ; 269 (1). 384-392
25. Ramachandran V., Kostrubsky V. E., Komoroski B. J., Zhang S., Dorko K., Esplen J. E., Strom S. C., Venkataramanan R.. Troglitazone Increases Cytochrome P-450 3A Protein and Activity in Primary Cultures of Human Hepatocytes. Drug Metab. Dispos. 1999 ; 27 (10). 1194-1199
26. Pelkonen O., Myllynen P., Taavitsainen P., Boobis A. R., Watts P., Lake B. G., Price R. J., Renwick A. B., Gómez-Lechón M. J., Castell J. V., et al. Carbamazepine: A 'Blind' Assessment of CVP-Associated Metabolism and Interactions in Human Liver-Derived In Vitro Systems. Xenobiotica. 2001 ; 31 (6). 321-343
27. Hariparsad N., Carr B. A., Evers R., Chu X.. Comparison of Immortalized Fa2N-4 cells and Human Hepatocytes as In Vitro Models for Cytochrome P450 Induction. Drug Metab. Dispos. 2008 ; 36 (6). 1046-1055
28. Sahi J., Shord S. S., Lindley C., Ferguson S., LeCluyse E. L.. Regulation of Cytochrome P450 2C9 Expression in Primary Cultures of Human Hepatocytes. J. Biochem. Mol. Toxicol. 2009 ; 23 (1). 43-58
29. 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 Metab. Dispos. 2002 ; 30 (7). 795-804
30. Hull M. W., Montaner J. S.. Ritonavir-Boosted Protease Inhibitors in HIV Therapy. Ann. Med. 2011 ; 43 (5). 375-388