Synergistic inhibition of protease-inhibitor-resistant HIV type 1 by saquinavir in combination with atazanavir or lopinavir

Antiviral Therapy

Volumn 12, Issue 3, 2007, Pages 371-380

  Dam, Elisabeth ^a,b   Lebel Binay, Sophie ^a   Rochas, Séverine ^a   Thibaut, Laurent ^a   Faudon, Jean Louis ^a   Thomas, Claire Marie ^a   Essioux, Laurent ^c   Hill, Andrew ^d   Schutz, Malte ^e   Clavel, François ^b  

^a Viralliance   (France)

^b INSERM   (France)

^c UNIVERSITY OF LIVERPOOL   (United Kingdom)

^d F HOFFMANN LA ROCHE LTD   (Switzerland)

^e ROCHE PRODUCTS LTD   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ATAZANAVIR; LOPINAVIR; PROTEINASE INHIBITOR; SAQUINAVIR;

ANTIBIOTIC RESISTANCE; ANTIVIRAL ACTIVITY; ARTICLE; CONTROLLED STUDY; CYTOTOXICITY; DRUG MECHANISM; DRUG POTENTIATION; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; NONHUMAN; PRIORITY JOURNAL; SITE DIRECTED MUTAGENESIS; VIRUS INHIBITION; VIRUS RECOMBINANT; VIRUS RESISTANCE; VIRUS STRAIN; WILD TYPE;

CELL LINE, TUMOR; DRUG RESISTANCE, VIRAL; DRUG SYNERGISM; HIV PROTEASE INHIBITORS; HIV-1; HUMANS; INHIBITORY CONCENTRATION 50; MICROBIAL SENSITIVITY TESTS; OLIGOPEPTIDES; PYRIDINES; PYRIMIDINONES; RECOMBINATION, GENETIC; SAQUINAVIR; TRANSFECTION;

EID: 34249078918     PISSN: 13596535     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (30)

1. Van Heeswijk RP, Veldkamp A, Mulder JW, et al. Combination of protease inhibitors for the treatment of HIV-1-infected patients: a review of pharmacokinetics and clinical experience. Antivir Ther 2001; 6:201-229.
2. Moyle GJ, Back D. Principles and practice of HIV-protease inhibitor pharmacoenhancement. HIV Med 2001; 2:105-113.
3. Cahn PE, Gatell JM, Squires K, et al. Atazanavir - a once-daily HIV protease inhibitor that does not cause dyslipidemia in newly treated patients: results from two randomized clinical trials. J Int Assoc Physicians AIDS Care (Chic Ill) 2004; 3:92-98.
4. Boffito M, Dickinson L, Hill A, et al. Steady-state pharmacokinetics of saquinavir hard-gel/ritonavir/fosamprenavir in HIV-1-infected patients. J Acquir Immune Defic Syndr 2004; 37:1376-1384.
5. Boffito M, Kurowski M, Kruse G, et al. Atazanavir enhances saquinavir hard-gel concentrations in a ritonavir-boosted once-daily regimen. AIDS 2004; 18:1291-1297.
6. Stephan C, Hentig N, Kourbeti I, et al. Saquinavir drug exposure is not impaired by the boosted double protease inhibitor combination of lopinavir/ritonavir. AIDS 2004; 18:503-508.
7. Johnson VA, Brun-Vezinet F, Clotet B, et al. Update of the Drug Resistance Mutations in HIV-1: 2005. Top HIV Med 2005; 13:51-57.
8. Kempf DJ, Isaacson JD, King MS, et al. Identification of genotypic changes in human immunodeficiency virus protease that correlate with reduced susceptibility to the protease inhibitor lopinavir among viral isolates from protease inhibitor-experienced patients. J Virol 2001; 75:7462-7469.
9. Hellinger J, Cohen C, Morris A, et al. Pilot study of saquinavir and lopinavir/ritonavir twice daily in protease inhibitor-naive HIV-positive patients. HIV Clin Trials 2005; 6:107-117
10. Knechten H, Braun P, Weismann F, Ehret R, Hoehn C. Switching from a non PI-containing regimen to saquinavir and lopinavir in therapy-experienced HIV-1-infected patients: a 48 weeks follow up. XV International AIDS conference. Bangkok, Thailand, 11-16 July 2004. Abstract TuPe B4573.
11. Staszewski S, Dauer B, Carlebach A, et al. The LOPSAQ salvage study: 48 week analysis of the full cohort treated with lopinavir plus saquinavir without any additional antiretroviral therapy. XV International AIDS Conference. Bangkok, Thailand, 11-16 July 2004. Abstract B10840.
12. Gong YF, Robinson BS, Rose RE, et al. In vitro resistance profile of the human immunodeficiency virus type 1 protease inhibitor BMS-232632. Antimicrob Agents Chemother 2000; 44:2319-2326.
13. Ford J, Boffito M, Wildfire A, et al. The intracellular and plasma pharmacokinetics of saquinavir, atazanavir and ritonavir 1600/1200/100mg administered once daily in HIV-infected patients. 7th International Conference on Drug Therapy in HIV infection. Glasgow, UK, 14-18 November 2004. Abstract PL6.3b.
14. Von Hentig N, Mueller A, Haberi A, et al. The ATSAQ-1 cohort study: pharmacokinetic interactions of atazanavir and saquinavir in a ritonavir-boosted protease inhibitor therapy regimen. XV International AIDS conference. Bangkok, Thailand. 11-16 July 2004. Abstract WeOrB1235.
15. Patick AK, Boritzki TJ, Bloom LA. Activities of the human immunodeficiency virus type 1 (HIV-1) protease inhibitor nelfinavir mesylate in combination with reverse transcriptase and protease inhibitors against acute HIV-1 infection in vitro. Antimicrob Agents Chemother 1997; 41:2159-64.
16. Tremblay C, Merrill DP, Chou TC, Hirsch MS. Interactions among combinations of two and three protease inhibitors against drug-susceptible and drug-resistant HIV-1 isolates. J Acquir Immune Defic Syndr 1999; 22:430-436.
17. Deminie CA, Bechtold CM, Stock D, et al. Evaluation of reverse transcriptase and protease inhibitors in two-drug combinations against human immunodeficiency virus replication. Antimicrob Agents Chemother 1996; 40:1346-1351.
18. Robinson BS, Riccardi KA, Gong YF, et al. BMS-232632, a highly potent human immunodeficiency virus protease inhibitor that can be used in combination with other available antiretroviral agents. Antimicrob Agents Chemother 2000; 44:2093-2099.
19. Molla A, Mo H, Vasavanonda S, et al. In vitro antiviral interaction of lopinavir with other protease inhibitors. Antimicrob Agents Chemother 2002; 46:2249-2253.
20. Charneau P, Mirambeau G, Roux P, Paulous S, Buc H, Clavel F. HIV-1 reverse transcription. A termination step at the center of the genome. J Mol Biol 1994; 241:651-662.
21. Mammano F, Trouplin V, Zennou V, Clavel F. Retracing the Evolutionary Pathways of Human Immunodeficiency Virus Type 1 Resistance to Protease Inhibitors: Virus Fitness in the Absence and in the Presence of Drug. J Virol 2000; 74:8524-8531.
22. Chou TC, Talalay P. Quantitative analysis of dose-effect relationships: the combined effects of multiple drugs or enzyme inhibitors. Adv Enzyme Regul 1984; 22:27-55.
23. Belen'kii MS, Schinazi RF. Multiple drug effect analysis with confidence interval. Antiviral Res 1994; 25:1-11.
24. Nascimbeni M, Lamotte C, Peytavin G, Farinotti R, Clavel F. Kinetics of antiviral activity and intracellular pharmacokinetics of human immunodeficiency virus type 1 protease inhibitors in tissue culture. Antimicrob Agents Chemother 1999; 43:2629-2634.
25. Srinivas RV, Middlemas D, Flynn P, Fridland A. Human immunodeficiency virus protease inhibitors serve as substrates for multidrug transporter proteins MDR1 and MRP1 but retain antiviral efficacy in cell lines expressing these transporters. Antimicrob Agents Chemother 1998; 42:3157-3162.
26. Jones K, Bray PG, Khoo SH, et al. P-Glycoprotein and transporter MRP1 reduce HIV protease inhibitor uptake in CD4 cells: potential for accelerated viral drug resistance? AIDS 2001; 15:1353-1358.
27. Olson DP, Scadden DT, D'aquila R T, De Pasquale M P. The protease inhibitor ritonavir inhibits the functional activity of the multidrug resistance related-protein 1 (MRP-1). AIDS 2002; 16:1743-1747.
28. Huisman MT, Smit JW, Wiltshire HR, Hoetelmans RM, Beijnen JH, Schinkel AH. P-glycoprotein limits oral availability, brain, and fetal penetration of saquinavir even with high doses of ritonavir. Mol Pharmacol 2001; 59:806-813.
29. Vishnuvardhan D, Moltke LL, Richert C, Greenblatt DJ. Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein. AIDS 2003; 17:1092-1094.
30. Lucia MB, Golotta C, Rutella S, Rastrelli E, Savarino A, Cauda R. Atazanavir inhibits P-glycoprotein and multidrug resistance-associated protein efflux activity. J Acquir Immune Defic Syndr 2005; 39:635-637.