Atazanavir: Effects on P-glycoprotein transport and CYP3A metabolism in vitro

Drug Metabolism and Disposition

Volumn 33, Issue 6, 2005, Pages 764-770

  Perloff, Elke S ^a   Duan, Su X ^a   Skolnik, Paul R ^b   Greenblatt, David J ^a   Von Moltke, Lisa L ^a  

^a TUFTS UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b BOSTON UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMPRENAVIR; ATAZANAVIR; CYTOCHROME P450 3A; GLYCOPROTEIN P; INDINAVIR; LOPINAVIR; NELFINAVIR; RHODAMINE 123; RITONAVIR; SAQUINAVIR; TRIAZOLAM; VERAPAMIL;

ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG POTENCY; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME METABOLISM; HUMAN; HUMAN CELL; HYDROXYLATION; LIVER MICROSOME; POLYACRYLAMIDE GEL ELECTROPHORESIS; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FOLDING; PROTEIN INDUCTION; PROTEIN TRANSPORT; WESTERN BLOTTING;

ARYL HYDROCARBON HYDROXYLASES; CACO-2 CELLS; CELL LINE, TUMOR; CYTOCHROME P-450 CYP3A; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; HUMANS; INTRACELLULAR FLUID; OLIGOPEPTIDES; OXIDOREDUCTASES, N-DEMETHYLATING; P-GLYCOPROTEIN; PROTEIN TRANSPORT; PYRIDINES;

EID: 18844409566     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: 10.1124/dmd.104.002931     Document Type: Article

References (35)

1. Artursson P, Palm K, and Luthman K (1996) Caco-2 monolayers in experimental and theoretical predictions of drug transport. Adv Drug Deliv Rev 22:67-84.
2. Benet LZ, Cummins CL, and Wu CY (2003) Transporter-enzyme interactions: implications for predicting drug-drug interactions from in vitro data. Curr Drug Metab 4:393-398.
3. Boffito M, Kurowski M, Kruse G, Hill A, Benzie AA, Nelson MR, Moyle GJ, Gazzard BG, and Pozniak AL (2004) Atazanavir enhances saquinavir hard-gel concentrations in a ritonavir-boosted once-daily regimen. AIDS 18:1291-1297.
4. Colonno R, Rose R, McLaren C, Thiry A, Parkin N, and Friborg J (2004) Identification of I50L as the signature atazanavir (ATV)-resistance mutation in treatment-naive HIV-1-infected patients receiving ATV-containing regimens. J Infect Dis 189:1802-1810.
5. de Maat MM, Ekhart GC, Huitema AD, Koks CH, Mulder JW, and Beijnen JH (2003) Drug interactions between antiretroviral drugs and comedicated agents. Clin Pharmacokinet 42:223-282.
6. Goldsmith DR and Perry CM (2003) Atazanavir. Drugs 63:1679-1693.
7. Greenblatt DJ, von Moltke LL, Harmatz JS, Chen G, Weemhoff JL, Jen C, Kelley CJ, LeDuc BW, and Zinny MA (2003) Time course of recovery of cytochrome P450 3A function after single doses of grapefruit juice. Clin Pharmacol Ther 74:121-129.
8. Haas DW, Zala C, Schrader S, Piliero P, Jaeger H, Nunes D, Thiry A, Schnittman S, and Sension M (2003) Therapy with atazanavir plus saquinavir in patients failing highly active antiretroviral therapy: a randomized comparative pilot trial. AIDS 17:1339-1349.
9. Havlir DV and O'Marro SD (2004) Atazanavir: new option for treatment of HIV infection. Clin Infect Dis 38:1599-1604.
10. Herzog CE, Tsokos M, Bates SE, and Fojo AT (1993) Increased mdr-1/P-glycoprotein expression after treatment of human colon carcinoma cells with P-glycoprotein antagonists. J Biol Chem 268:2946-2952.
11. Kim RB, Fromm MF, Wandel C, Leake B, Wood AJ, Roden DM, and Wilkinson GR (1998) The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors. J Clin Investig 101:289-294.
12. Lee JS, Paull K, Alvarez M, Hose C, Monks A, Grever M, Fojo AT, and Bates SE (1994) Rhodamine efflux patterns predict P-glycoprotein substrates in the National Cancer Institute drug screen. Mol Pharmacol 46:627-638.
13. Li Q, Sai Y, Kato Y, Tamai I, and Tsuji A (2003) Influence of drugs and nutrients on transporter gene expression levels in Caco-2 and LS180 intestinal epithelial cell lines. Pharm Res (NY) 20:1119-1124.
14. Minderman H, Vanhoefer U, Toth K, Yin MB, Minderman MD, Wrzosek C, Slovak ML, and Rustum YM (1996) DiOC2(3) is not a substrate for multidrug resistance protein (MRP)-mediated drug efflux. Cytometry 25:14-20.
15. Musial BL, Chojnacki JK, and Coleman CI (2004) Atazanavir: a new protease inhibitor to treat HIV infection. Am J Health Syst Pharm 61:1365-1374.
16. Orrick JJ and Steinhart CR (2004) Atazanavir. Ann Pharmacother 38:1664-1674.
17. Perloff MD, Störmer E, von Moltke LL, and Greenblatt DJ (2003) Rapid assessment of P-glycoprotein inhibition and induction in vitro. Pharm Res (NY) 20:1177-1183.
18. Perloff MD, von Moltke LL, Fahey JM, Daily JP, and Greenblatt DJ (2000) Induction of P-glycoprotein expression by HIV protease inhibitors in cell culture. AIDS 14:1287-1289.
19. Perloff MD, von Moltke LL, and Greenblatt DJ (2002) Fexofenadine transport in Caco-2 cells: inhibition with verapamil and ritonavir. J Clin Pharmacol 42:1269-1274.
20. Perloff MD, Von Moltke LL, Marchand JE, and Greenblatt DJ (2001) Ritonavir induces P-glycoprotein expression, multidrug resistance-associated protein (MRP1) expression and drug transporter-mediated activity in a human intestinal cell line. J Pharm Sci 90:1829-1837.
21. Piliero PJ (2002) Atazanavir: a novel HIV-1 protease inhibitor. Expert Opin Investig Drugs 11:1295-1301.
22. Pinto M, Robine-Leon S, Appay M, Kedinger M, Triadou N, Dussaulx E, Lacroix B, Simon-Assmann P, Haffen K, Fogh J, and Zweibaum A (1983) Enterocyte-like differentiation and polarisation of the human colon carcinoma cell line Caco-2 in culture. Biol Cell 47:323-330.
23. Profit L, Eagling VA, and Back DJ (1999) Modulation of P-glycoprotein function in human lymphocytes and Caco-2 cell monolayers by HIV-1 protease inhibitors. AIDS 13:1623-1627.
24. Quaroni A and Hochman J (1996) Development of intestinal cell culture models for drug transport and metabolism studies. Adv Drug Deliv Rev 22:3-52.
25. Robinson BS, Riccardi KA, Gong YF, Guo Q, Stock DA, Blair WS, Terry BJ, Deminie CA, Djang F, Colonno RJ, et al. (2000) BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agents. Antimicrob Agents Chemother 44:2093-2099.
26. Schuetz EG, Beck WT, and Schuetz JD (1996) Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol Pharmacol 49:311-318.
27. Squires K, Lazzarin A, Gatell JM, Powderly WG, Pokrovskiy V, Delfraissy JF, Jemsek J, Rivero A, Rozenbaum W, Schrader S, et al. (2004) Comparison of once-daily atazanavir with efavirenz, each in combination with fixed-dose zidovudine and lamivudine, as initial therapy for patients infected with HIV. J Acquir Immune Defic Syndr 36:1011-1019.
28. Störmer E, von Moltke LL, Perloff MD, and Greenblatt DJ (2002) Differential modulation of P-glycoprotein expression and activity by non-nucleoside HIV-1 reverse transcriptase inhibitors in cell culture. Pharm Res (NY) 19:1038-1045.
29. Vishnuvardhan D, von Moltke LL, Richert C, and Greenblatt DJ (2003) Lopinavir: acute exposure inhibits p-glycoprotein; extended exposure induces P-glycoprotein. AIDS 17:1092-1094.
30. von Moltke LL, Durol AL, Duan SX, and Greenblatt DJ (2000) Potent mechanism-based inhibition of human CYP3A in vitro by amprenavir and ritonavir: comparison with ketoconazole. Eur J Clin Pharmacol 56:259-261.
31. von Moltke LL, Greenblatt DJ, Duan SX, Harmatz JS, and Shader RI (1998a) Inhibition of triazolam hydroxylation by ketoconazole, itraconazole, hydroxyitraconazole and fluconazole in-vitro. Pharm Pharmacol Commun 4:443-445.
32. von Moltke LL, Greenblatt DJ, Granda BW, Giancarlo GM, Duan SX, Daily JP, Harmatz JS, and Shader RI (2001) Inhibition of human cytochrome P450 isoforms by nonnucleoside reverse transcriptase inhibitors. J Clin Pharmacol 41:85-91.
33. von Moltke LL, Greenblatt DJ, Grassi JM, Granda BW, Duan SX, Fogelman SM, Daily JP, Harmatz JS, and Shader RI (1998b) Protease inhibitors as inhibitors of human cytochromes P450: high risk associated with ritonavir. J Clin Pharmacol 38:106-111.
34. von Moltke LL, Greenblatt DJ, Harmatz JS, and Shader RI (1993) Alprazolam metabolism in vitro: studies of human, monkey, mouse and rat liver microsomes. Pharmacology 47:268-276.
35. Weemhoff JL, von Moltke LL, Richert C, Hesse LM, Harmatz JS, and Greenblatt DJ (2003) Apparent mechanism-based inhibition of human CYP3A in-vitro by lopinavir. J Pharm Pharmacol 55:381-386.