Impact of ritonavir, atazanavir and their combination on the cyp3a4 induction by efavirenz in primary human hepatocytes

Drug Metabolism Letters

Volumn 4, Issue 1, 2010, Pages 45-50

  Mugundu, Ganesh M ^a   Hariparsad, Niresh ^a,b   Desai, Pankaj B ^a  

^a UNIVERSITY OF CINCINNATI MEDICAL CENTER   (United States)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6BETA HYDROXYTESTOSTERONE; ATAZANAVIR; CYTOCHROME P450 3A4; EFAVIRENZ; PREGNANE X RECEPTOR; RIFAMPICIN; RITONAVIR; TESTOSTERONE; UNCLASSIFIED DRUG; ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; BENZOXAZINE DERIVATIVE; CYP3A4 PROTEIN, HUMAN; CYTOCHROME P450 3A; OLIGOPEPTIDE; PYRIDINE DERIVATIVE; STEROID RECEPTOR;

ADULT; ARTICLE; CELL SURVIVAL; CELL VIABILITY; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ACTIVITY; ENZYME ACTIVITY; ENZYME INDUCTION; HUMAN; HUMAN CELL; LIVER CELL; PRIORITY JOURNAL; TRANSCRIPTION INITIATION; BIOSYNTHESIS; DOSE RESPONSE; DRUG COMBINATION; DRUG EFFECT; DRUG INTERACTION; GENETIC TRANSFECTION; METABOLISM; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION; TUMOR CELL LINE;

AMBYSTOMA TIGRINUM STEBBENSI VIRUS;

ANTI-HIV AGENTS; BENZOXAZINES; CELL LINE, TUMOR; CYTOCHROME P-450 CYP3A; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INTERACTIONS; DRUG THERAPY, COMBINATION; ENZYME INDUCTION; HEPATOCYTES; HUMANS; OLIGOPEPTIDES; PYRIDINES; RECEPTORS, STEROID; REVERSE TRANSCRIPTASE POLYMERASE CHAIN REACTION; RITONAVIR; TRANSFECTION;

EID: 77953243792     PISSN: 18723128     EISSN: None     Source Type: Journal    
DOI: 10.2174/187231210790980453     Document Type: Article

References (27)

1. Winston, A, Boffito, M. The management of HIV-1 protease in-hibitor pharmacokinetic interactions. J. Antimicrob. Chemother., 2005, 56(1), 1-5.
2. Pham, P.A.; Hendrix, C.W.; Barditch-Crovo, P.; Parsons, T.; Khan, W.; Parish, M.; Radebaugh, C.; Carson, K.A.; Pakes, G.E.; Qaqish, R.; Flexner, C. Amprenavir and lopinavir pharmacokinetics following coadministration of amprenavir or fosamprenavir with lopi-navir/ritonavir, with or without efavirenz. Antivir. Ther., 2007, 12(6), 963-969.
3. Barry, M.; Gibbons, S.; Back, D.; Mulcahy, F. Protease inhibitors in patients with HIV disease. Clinically important pharmacokinetic considerations. Clin. Pharmacokinet., 1997, 32(3), 194-209.
4. Pfister, M.; Labbé, L.; Lu, JF.; Hammer, S.M.; Mellors, J.; Bennett, K.K.; Rosenkranz, S.; Sheiner, L.B. AIDS Clinical Trial Group Protocol 398 Investigators. Effect of coadministration of nelfinavir, indinavir, and saquinavir on the pharmacokinetics of amprenavir. Clin. Pharmacol. Ther. 2002, 72(2), 133-141.
5. Moltó, J.; Blanco, A.; Miranda, C.; Miranda, J.; Puig, J.; Valle, M.; Delavarga, M.; Fumaz, CR.; Barbanoj, MJ.; Clotet, B. Variability in non-nucleoside reverse transcriptase and protease inhibitors concentrations among HIV-infected adults in routine clinical practice. Br. J. Clin. Pharmacol., 2007, 63(6), 715-721.
6. Hariparsad, N.; Nallani, S. C.; Sane, R. S.; Buckley, D. J.; Buckley, A. R.; Desai, P. B. Induction of CYP3A4 by efavirenz in primary human hepatocytes: comparison with rifampin and phenobarbital. J. Clin. Pharmacol., 2004, 44(11), 1273-1281.
7. Ma, Q.; Okusanya, O. O.; Smith, P. F.; Dicenzo, R.; Slish, J. C.; Catanzaro, L. M.; Forrest, A.; Morse, G. D. Pharmacokinetic drug interactions with non-nucleoside reverse transcriptase inhibitors. Expert. Opin. Drug Metab Toxicol., 2005, 1(3), 473-485.
8. Zeldin, R. K.; Petruschke, R. A. Pharmacological and therapeutic properties of ritonavir-boosted protease inhibitor therapy in HIV-infected patients. J. Antimicrob. Chemother., 2004, 53(1), 4-9.
9. Luo, G.; Cunningham, M.; Kim, S.; Burn, T.; Lin, J.; Sinz, M.; Hamilton, G.; Rizzo, C.; Jolley, S.; Gilbert, D.; Downey, A.; Mudra, D.; Graham, R.; Carroll, K.; Xie, J.; Madan, A.; Parkinson, A.; Christ, D.; Selling, B.; LeCluyse, E.; Gan, L. S. 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.
10. Faucette, S. R.; Wang, H.; Hamilton, G. A.; Jolley, S. L.; Gilbert, D.; Lindley, C.; Yan, B.; Negishi, M.; LeCluyse, E. L. Regulation of CYP2B6 in primary human hepatocytes by prototypical inducers. Drug Metab. Dispos., 2004, 32(3), 348-358.
11. Hogeland, G. W.; Swindells, S.; McNabb, J. C.; Kashuba, A. D.; Yee, G. C.; Lindley, C. M. Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects. Clin. Pharmacol. Ther., 2007, 81(1), 69-75.
12. Perloff, M. D.; Stormer, E.; von Moltke, L. L.; Greenblatt, D. J. Rapid assessment of P-glycoprotein inhibition and induction in vitro. Pharm. Res., 2003, 20(8), 1177-1183.
13. Busti, A. J.; Hall, R. G.; Margolis, D. M. Atazanavir for the treatment of human immunodeficiency virus infection. Pharmacotherapy 2004, 24(12), 1732-1747.
14. Molto, J.; Blanco, A.; Miranda, C.; Miranda, J.; Puig, J.; Valle, M.; Delavarga, M.; Fumaz, C. R.; Barbanoj, M. J.; Clotet, B. Variability in non-nucleoside reverse transcriptase and protease inhibitors concentrations among HIV-infected adults in routine clinical practice. Br. J. Clin. Pharmacol., 2007, 63(6), 715-721.
15. Morse, G.D.; Rosenkranz, S.; Para, M.F.; Segal, Y.; Difrancesco, R.; Adams, E.; Brizz, B.; Yarasheski, K.E.; Reichman, R.C. Amprenavir and efavirenz pharmacokinetics before and after the addition of nelfinavir, indinavir, ritonavir, or saquinavir in seronegative individuals. Antimicrob. Agents Chemother., 2005, 49(8), 3373-3381.
16. Fellay, J.; Marzolini, C.; Decosterd, L.; Golay, KP.; Baumann, P.; Buclin, T.; Telenti, A.; Eap, C.B. Variations of CYP3A activity induced by antiretroviral treatment in HIV-1 infected patients. Eur. J. Clin. Pharmacol., 2005, 60(12), 865-873.
17. Lehmann, J. M.; McKee, D. D.; Watson, M. A.; Willson, T. M.; Moore, J. T.; Kliewer, S. A. The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. J. Clin. Invest., 1998, 102(5), 1016-1023.
18. Desai, P. B.; Nallani, S. C.; Sane, R. S.; Moore, L. B.; Goodwin, B. J.; Buckley, D. J.; Buckley, A. R. Induction of cytochrome P450 3A4 in primary human hepatocytes and activation of the human pregnane X receptor by tamoxifen and 4-hydroxytamoxifen. Drug Metab. Dispos., 2002, 30(5), 608-612.
19. Kostrubsky, V. E.; Lewis, L. D.; Strom, S. C.; Wood, S. G.; Schuetz, E. G.; Schuetz, J. D.; Sinclair, P. R.; Wrighton, S. A.; Sinclair, J. F. Induction of cytochrome P4503A by taxol in primary cultures of human hepatocytes. Arch. Biochem. Biophys., 1998, 355(2), 131-136.
20. Kostrubsky, V. E.; Ramachandran, V.; Venkataramanan, R.; Dorko, K.; Esplen, J. E.; Zhang, S.; Sinclair, J. F.; Wrighton, S. A.; Strom, S. C. The use of human hepatocyte cultures to study the induction of cytochrome P-450. Drug Metab. Dispos., 1999, 27(8), 887-894.
21. Nallani, S. C.; Genter, M. B.; Desai, P. B. Increased activity of CYP3A enzyme in primary cultures of rat hepatocytes treated with docetaxel: comparative evaluation with paclitaxel. Cancer Chemother. Pharmacol., 2001, 48(2), 115-122.
22. Reinach, B.; de, S. G.; Dostert, P.; Ings, R.; Gugenheim, J.; Rahmani, R. Comparative effects of rifabutin and rifampicin on cytochromes P450 and UDP-glucuronosyl-transferases expression in fresh and cryopreserved human hepatocytes. Chem. Biol. Interact., 1999, 121(1), 37-48.
23. Luo, G.; Lin, J.; Fiske, W. D.; Dai, R.; Yang, T. J.; Kim, S.; Sinz, M.; LeCluyse, E.; Solon, E.; Brennan, J. M.; Benedek, I. H.; Jolley, S.; Gilbert, D.; Wang, L.; Lee, F. W.; Gan, L. S. Concurrent induction and mechanism-based inactivation of CYP3A4 by an L-valinamide derivative. Drug Metab. Dispos., 2003, 31(9), 1170-1175.
24. Ripp, S.L.; Mills, J.B.; Fahmi, O.A.; Trevena, K.A.; Liras, J.L.; Maurer, T.S.; de Morais, S.M. Use of immortalized human hepatocytes to predict the magnitude of clinical drug-drug interactions caused by CYP3A4 induction. Drug Metab. Dispos., 2006, 34(10), 1742-1748.
25. Fahmi, O.A.; Boldt, S.; Kish, M.; Obach, R.S.; Tremaine, LM. Prediction of drug-drug interactions from in vitro induction data: application of the relative induction score approach using cryopre-served human hepatocytes. Drug Metab. Dispos., 2008; 36(9), 1971-1974.
26. Yasuda, K.; Ranade, A.; Venkataramanan, R.; Strom, S.; Chupka, J.; Ekins, S.; Schuetz, E.; Bachmann, K. A comprehensive in vitro and in silico analysis of antibiotics that activate pregnane X receptor and induce CYP3A4 in liver and intestine. Drug Metab. Dispos., 2008, 36(8), 1689-1697.
27. Zhou, S.; Yung, C.S.; Cher, G.B.; Chan, E.; Duan, W.; Huang, M.; McLeod, H.L. Mechanism-Based Inhibition of Cytochrome P450 3A4 by Therapeutic Drugs. Clin. Pharmacokinet., 2005, 44(3), 279-304.