Anti-human immunodeficiency virus drug combination strategies

Antiviral Chemistry and Chemotherapy

Volumn 9, Issue 3, 1998, Pages 187-203

  Vandamme, A M ^a   Van Vaerenbergh, K ^a   De Clercq, E ^a  

^a REGA INSTITUTE FOR MEDICAL RESEARCH   (Belgium)

Author keywords

Antiviral drug resistance; Antiviral therapy; Drug combination therapy; HAART; HIV

Indexed keywords

ABACAVIR; ADEFOVIR; ANTACID AGENT; ANTIARRHYTHMIC AGENT; ANTIBIOTIC AGENT; ANTICOAGULANT AGENT; ANTICONVULSIVE AGENT; ANTIFUNGAL AGENT; ANTINEOPLASTIC AGENT; ANTIRETROVIRUS AGENT; DELAVIRDINE; DIDANOSINE; DIPIVOX; GASTROINTESTINAL AGENT; GLUCOCORTICOID; HISTAMINE H2 RECEPTOR ANTAGONIST; INDINAVIR; LAMIVUDINE; NELFINAVIR; NEVIRAPINE; ORAL CONTRACEPTIVE AGENT; PROTEINASE INHIBITOR; PSYCHOTROPIC AGENT; RITONAVIR; RNA DIRECTED DNA POLYMERASE INHIBITOR; SAQUINAVIR; STAVUDINE; UNCLASSIFIED DRUG; UNINDEXED DRUG; ZALCITABINE; ZIDOVUDINE;

BLOOD TOXICITY; CARDIOTOXICITY; COMBINATION CHEMOTHERAPY; DRUG RESISTANCE; EYE TOXICITY; FATIGUE; FEVER; GASTROINTESTINAL SYMPTOM; GENE MUTATION; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; LIVER TOXICITY; MYOPATHY; NEPHROLITHIASIS; NEUROTOXICITY; PRIORITY JOURNAL; REVIEW; SKIN TOXICITY; TREATMENT FAILURE;

EID: 0031799218     PISSN: 09563202     EISSN: None     Source Type: Journal    
DOI: 10.1177/095632029800900301     Document Type: Review

References (149)

1. Aboulker JP & Swarts M (1993). Preliminary analysis of the Concorde trial. Concorde Coordinating Committee. Lancet 341: 889-890.
2. Ala PJ, Huston EE, Klabe RM, McCabe DD, Duke JL, Rizzo CJ, Korant BD, DeLoskey RJ, Lam PY, Hodge CN & Chang CH (1997) Molecular basis of HIV-1 protease drug resistance: structural analysis of mutant proteases complexed with cyclic urea inhibitors. Biochemistry 36:1573-1580.
3. Arts EJ & Wainberg MA (1996) Mechanisms of nucleoside analog antiviral activity and resistance during human immunodeficiency virus reverse transcription. Antimicrobial Agents and Chemotherapy 40:527-540.
4. Autran B, Carcelain G, Li TS, Blanc C, Mathez D, Tubiana R, Katlama C, Debré P & Leibowitch J (1997) Positive effects of combined antiretroviral therapy on CD4+ T cell homeostasis and function in advanced HIV disease. Science 277:112-116.
5. Baldwin ET, Bhat TN, Liu B, Pattabiraman N & Erickson JW (1995) Structural basis of drug resistance for the V82A mutant of HIV-1 proteinase. Nature Structural Biology 2:244-249.
6. Balzarini J, Karlsson A, Pérez-Pérez M-J, Camarasa M-J, Tarpley WG & De Clercq E (1993b) Treatment of human immunodeficiency virus type 1 (HIV-1)-infected cells with combinations of HIV-1-specific inhibitors results in a different resistance pattern than does treatment with single-drug therapy. Journal of Virology 67:5353-5359.
7. Balzarini J, Karlsson A, Vandamme A-M, Pérez-Pérez M-J, Zhang H, Vrang L, Öberg B, Bäckbro K, Unge T, San-Felix A, Velazquez S, Camarasa M-J & De Clercq E (1993a) Human immunodeficiency virus type 1 (HIV-1) strains selected for resistance against the HIV-1-specific [2′,5′-bis-O-(tert-butyldimethylsilyl)-3′-spiro-5″- (4″-amino-1″,2″-oxathiole-2″,2″-dioxide)]-β- D-pentofuranosyl (TSAO) nucleoside analogues retain sensitivity to HIV-1-specific nonnucleoside inhibitors. Proceedings of the National Academy of Sciences, USA 90:6952-6956.
8. Bartlett JA, Benoit SL, Johnson VA, Quinn JB, Sepulveda GE, Ehmann WC, Tsoukas C, Fallon MA, Self PL & Rubin M (1996) Lamivudine plus zidovudine compared with zalcitabine plus zidovudine in patients with HIV infection. A randomized, double-blind, placebo-controlled trial. Annals of Internal Medicine 125:161-172.
9. Boucher CAB (1997) Human immunodeficiency viruses and human T-lymphotropic viruses. In Antiviral Agents and Human Viral Diseases, pp. 607-698. Edited by GJ Galasso, RJ Whitley and TC Merigan. Philadelphia: Lippincott-Raven.
10. Boucher CAB, O'Sullivan E, Mulder JW, Ramautarsing C, Kellam P, Darby G, Lange JMA, Goudsmit J & Larder BA (1992) Ordered appearance of zidovudine resistance mutations during treatment of 18 human immunodeficiency virus-positive subjects. Journal of Infectious Diseases 165:105-110.
11. Boyer PL, Currens MJ, McMahon JB, Boyd MR & Hughes SH (1993) Analysis of nonnucleoside drug-resistant variants of human immunodeficiency virus type 1 reverse transcriptase. Journal of Virology 67:2412-2420.
12. Boyer PL & Hughes SH (1995) Analysis of mutations at position 184 in reverse transcriptase of human immunodeficiency virus type 1. Antimicrobial Agents and Chemotherapy 39:1624-1628.
13. Boyer PL, Tantillo C, Jacobo-Molina A, Nanni RG, Ding JP, Arnold E & Hughes SH (1994) Sensitivity of wild-type human immunodeficiency virus type 1 reverse transcriptase to dideoxynucleotides depends on template length. Proceedings of the National Academy of Sciences, USA 91:4882-4886.
14. Browne MJ, Mayer KH, Chafee SB, Dedley MN, Posner MR, Steinberg SM, Graham KK, Geletko SM, Zinner SH & Denman SL (1993) 2′,3′-didehydro-3′-deoxythymidine (d4T) in patients with AIDS or AIDS-related complex: a phase I trial. Journal of Infectious Diseases 167:21-29.
15. Carpenter CCJ, Fischl MA, Hammer SM, Hirsch MS, Jacobson DM, Katzenstein DA, Montaner JSG, Richman DD, Saag MS, Schooley RT, Thompson MA, Vella S, Yeni PG & Volberding PA (1997) Antiretroviral therapy for HIV infection in 1997. Updated recommendations of the international AIDS society-USA panel. Journal of the American Medical Association 277:1962-1969.
16. Cavert W, Notermans DW, Staskus K, Wietgrefe SW, Zupancic M, Gebhard K, Henry K, Zhang Z-Q, Mills R, McDade H, Goudsmit J, Danner SA & Haase AT (1997) Kinetics of response in lymphoid tissues to antiretroviral therapy of HIV-1 infection. Science 276:960-962.
17. Cheeseman SH, Havlir D, McLaughlin MM, Greenough TC, Sullivan JL, Hall D, Hattox SE, Spector SA, Stein DS, Myers M & Richman DD (1995) Phase I/II evaluation of nevirapine alone and in combination with zidovudine for infection with human immunodeficiency virus. Journal of Acquired Immune Deficiency Syndromes and Human Retrovirology 8:141-151.
18. Chun T-W, Fauci AS, Stuyver L, Mizell SB, Ehler LA, Mican JM, Baseler M, Lloyd AL & Nowak MA (1997) Presence of an inducible HIV-1 latent reservoir during highly active antiretroviral therapy. Proceedings of the National Academy of Sciences, USA 94:13193-13197.
19. Collier AC, Coombs RW, Schoenfeld DA, Bassett RL, Timpone J, Baruch A, Jones M, Facey K, Whitacre C, McAuliffe VJ, Friedman HM, Merigan TC, Reichman RC, Hooper C & Corey L (1996) Treatment of human immunodeficiency virus infections with saquinavir, zidovudine and zalcitabine. New England Journal of Medicine 334:1011-1017.
20. Concorde Coordinating Committee (1994) Concorde: MRC/ANRS randomised double-blind controlled trial of immediate and deferred zidovudine in symptom-free HIV infection. Lancet 343:871-881.
21. Condra JH, Holder DJ, Schleif WA, Blahy OM, Danovich RM, Gabryelski LJ, Graham DJ, Laird D, Quintero JC, Rhodes A, Robbins HL, Roth E, Shivaprakash M, Yang T, Chodakewitz JA, Deutsch PJ, Leavitt RY, Massari FE, Mellors JW, Squires KE, Steigbigel RT, Teppler H & Emini EA (1996) Genetic correlates of in vivo viral resistance to indinavir, a human immunodeficiency virus type 1 protease inhibitor. Journal of Virology 70:8270-8276.
22. Connor EM, Sperling RS, Gelber R, Kiselev P, Scott G, O'Sullivan MJ, VanDyke R, Bey M, Shearer W & Jacobson RL (1994) Reduction of maternal-infant transmission of human immunodeficiency virus type 1 with zidovudine treatment. New England Journal of Medicine 331:1173-1180.
23. Cooley TP, Kunches LM, Saunders CA, Ritter JK, Perkins CJ, McLaren C, McCaffrey RP & Liebman HA (1990) Once-daily administration of 2′,3′-dideoxyinosine (ddl) in patients with the acquired immunodeficiency syndrome or AIDS-related complex. Results of a phase I trial. New England Journal of Medicine 322:1340-1345.
24. Craig C & Moyle G (1997) The development of resistance of HIV-1 to zalcitabine. AIDS 11:271-279.
25. Croteau G, Doyon L, Thibeault D, McKercher G, Pilote L &. Lamarre D (1997) Impaired fitness of human immunodeficiency virus type 1 variants with high-level resistance to protease inhibitors. Journal of Virology 71:1089-1096.
26. D'Aquila RT, Hughes MD, Johnson VA, Fischl MA, Sommadossi J-P, Liou S-H, Timpone J, Myers M, Basgoz N, Niu M, Hirsch MS & The National Institute of Allergy and Infectious Diseases AIDS Clinical Trials Group Protocol 241 Investigators (1996) Nevirapine, zidovudine, and didanosine compared with zidovudine and didanosine in patients with HIV-1 infection. Annals of Internal Medicine 124:1019-1030.
27. Danner SA, Carr A, Leonard JM, Lehman LM, Gudiol F, Gonzales J, Raventos A, Rubio R, Bouza E, Pintado V, Aguado AG, De Lomas JG, Delgado R, Borleffs JCC, Hsu A, Valdes JM, Boucher CAB & Cooper DA (1995) A short-term study of the safety, pharmacokinetics, and efficacy of ritonavir, an inhibitor of HIV-1 protease. New England Journal of Medicine 333:1528-1533.
28. Davey RT, Chaitt DG, Reed GF, Freimuth WW, Herpin BR, Metcalf JA, Eastman PS, Falloon J, Kovacks JA, Polis MA, Walker RE, Masur H, Boyle J, Coleman S, Cox SR, Wathen L, Daenzer CL & Lane HC (1996) Randomized, controlled phase I/II trial of combination therapy with delavirdine (U-90152S) and conventional nucleosides in human immunodeficiency virus type 1-infected patients. Antimicrobial Agents and Chemotherapy 40:1657-1664.
29. De Clercq E (1997) Virus replication: target functions and events for virus-specific inhibitors. In Antiviral Agents and Human Viral Diseases, pp 1-44. Edited by GJ Galasso, RJ Whitley and TC Merigan. Philadelphia: Lippincott-Raven.
30. de Jong MD, Veenstra J, Stilianakis NI, Schuurman R, Lange JM, de Boer RJ & Boucher CA (1996) Host-parasite dynamics and outgrowth of virus containing a single K70R amino acid change in reverse transcriptase are responsible for the loss of human immunodeficiency virus type 1 RNA load suppression by zidovudine. Proceedings of the National Academy of Sciences, USA 93:5501-5506.
31. De Bouck C (1992) The HIV-1 protease as a therapeutic target for AIDS. AIDS Research and Human Retroviruses 8:153-164.
32. Deeks SG, Smith M, Holodniy M & Kahn JO (1997) HIV-1 protease inhibitors. Journal of the American Medical Association 277:145-153.
33. Delta Coordinating Committee (1996) Delta: a randomised double-blind controlled trial comparing combinations of zidovudine plus didanosine or zalcitabine with zidovudine alone in HIV-infected individuals. Lancet 348:283-291.
34. De Noon DJ (1998) AIDS Therapies. Atlanta: Charles W Henderson.
35. Dickover RE, Garratty EM, Herman SA, Sim MS, Plaeger S, Boyer PJ, Keller M, Deveikis A, Stiehm ER & Bryson YJ (1996) Identification of levels of maternal HIV-1 RNA associated with risk of perinatal transmission. Effect of maternal zidovudine treatment on viral load. Journal of the American Medical Association 275:640-641.
36. Domingo E, Menendezarias L & Holland JJ (1997) RNA virus fitness. Review of Medical Virology 7:87-96.
37. Doyon L, Croteau G, Thibeault D, Poulin F, Pilote L & Lamarre D (1996) Second locus involved in human immunodeficiency virus type I resistance to protease inhibitors. Journal of Virology 70:3763-3769.
38. Dueweke TJ, Pushkarskaya T, Poppe SM, Swaney SM, Zhao JQ, Chen ISY, Stevenson M & Tarpley WG (1993) A mutation in reverse transcriptase of bis(heteroaryl)piperazine-resistant human immunodeficiency virus type 1 that confers increased sensitivity to other nonnucleoside inhibitors. Proceedings of the National Academy of Sciences, USA 90:4713-4717.
39. Endres MJ, Jaffer S, Haggarty B, Turner JD, Doranz BJ, O'Brien PJ, Kolson DL & Hoxie JA (1997) Targeting of HIV- and SIV-infected cells by CD4-chemokine receptor pseudotypes. Science 278:1462-1464.
40. Eron JJ, Benoit SL, Jemsek J, MacArthur RD, Santana J, Quinn JB, Kuritzkes DR, Fallon MA & Rubin M (1995) Treatment with lamivudine, zidovudine, or both in HIV-positive patients with 200 to 500 CD4+ cells per cubic millimeter. New England Journal of Medicine 333:1662-1669.
41. Fessel WJ (1997) Human immunodeficiency virus (HIV) RNA in plasma as the preferred target for therapy in patients with HIV infection: a critique. Clinical Infectious Diseases 24:116-122.
42. Finzi D, Hermankova M, Pierson T, Carruth LM, Buck C, Chaisson RE, Quinn TC, Chadwick K, Margolick J, Brookmeyer R, Gallant J, Markowitz M, Ho DD, Richman DD & Siliciano RF (1997) Identification of a reservoir for HIV-1 in patients on highly active antiretroviral therapy. Science 278:1295-1300.
43. Fischl MA, Richman DD, Grieco MH, Gottlieb MS, Volberding PA, Laskin OL, Leedom JM, Groopman JE, Mildvan D, Schooley RT, Jackson GG, Durack DT & King D (1987) The efficacy of azidothymidine (AZT) in the treatment of patients with AIDS and AIDS-related complex. New England Journal of Medicine 317:185-191.
44. Fitzgibbon JE, Farnham AE, Sperber SJ, Kim H & Dubin DT (1993) Human immunodeficiency virus type 1 pol gene mutations in and AIDS patient treated with multiple antiretroviral drugs. Journal of Virology 67:7271-7275.
45. + repertoire during antiviral therapy. Nature Medicine 4:215-221.
46. Graham NMH, Zeger SL, Park LP, Vermund SH, Detels R, Rinaldo CR & Phair JP (1992) The effects on survival of early treatment of human immunodeficiency virus infection. New England Journal of Medicine 326:1037-1042.
47. Gu ZX, Fletcher RS, Arts EJ, Wainberg MA & Parniak MA (1994) The K65R mutant reverse transcriptase of HIV-1 cross-resistant to 2′,3′-dideoxycytidine, 2′,3′-dideoxy-3′-thiacytidine, and 2′,3′-dideoxyinosine shows reduced sensitivity to specific dideoxynucleoside triphosphate inhibitors in vitro. Journal of Biological Chemistry 269:28118-28122.
48. Gulick R, Mellors JW, Havlir D, Eron JJ, Gonzalez C, McMahon D, Richman DD, Valentine FT, Jonas L, Meibohm A, Emini EA & Chodakewitz JA (1997) Treatment with indinavir, zidovudine, and lamivudine in adults with human immunodeficiency virus infection and prior antiretroviral therapy. New England Journal of Medicine 337:734-739.
49. Günthard HF, Wong JK, Ignacio CC, Guatelli JC, Riggs NL, Havlir DV & Richman DD (1998) Human immunodeficiency virus replication and genotypic resistance in blood and lymph nodes after a year of potent antiretroviral therapy. Journal of Virology 72:2422-2428.
50. Hammer SM, Katzenstein DA, Hughes MD, Gundacker H, Schooley RT, Haubrich RH, Henry WK, Lederman MM, Phair JP, Niu M, Hirsch MS &. Merigan TC (1996) A trial comparing nucleoside monotherapy with combination therapy in HIV-infected adults with CD4 cell counts from 200 to 500 per cubic millimeter. New England Journal of Medicine 335:1081-1090.
51. Hammer SM, Squires KE, Hughes MD, Grimes JM, Demeter LM, Currier JS, Eron Jr JJ, Feinberg JE, Balfour HH, Deyton LR, Chodakewitz JA & Fischl MA (1997) A controlled trial of two nucleoside analogues plus indinavir in persons with human immunodeficiency virus infection and CD4 cell counts of 200 per cubic millimeter or less. New England Journal of Midecine 337:725-733.
52. Havlir D, Cheeseman SH, McLaughlin MM, Murphy R, Erice A, Spector SA, Greenough TC, Sullivan JL, Hall D, Myers M, Lamson M & Richman DD (1995) High-dose nevirapine: safety, pharmacokinetics, and antiviral effect in patients with human immunodeficiency virus infection. Journal of Infectious Diseases 171:537-545.
53. Havlir DV & Richman DD (1996) Viral dynamics of HIV: implications for drug development and therapeutic strategies. Annals of Internal Medicine 124:984-994.
54. Hertogs K, de Béthune M-P, Miller V, Ivens T, Schel P, Van Cauwenberge A, Van Den Eynde C, Van Gerwen V, Azijn H, Van Houtte M, Peeters F, Staszewski S, Conant M, Bloor S, Kemp S, Larder B & Pauwels R (1998) A rapid method for simultaneous detection of phenotypic resistance to inhibitors of protease and reverse transcriptase in recombinant human immunodeficiency virus type 1 isolates from patients treated with antiretroviral drugs. Antimicrobial Agents and Chemotherapy 42:269-276.
55. Ho DD, Neumann AU, Perelson AS, Chen W, Leonard JM & Markowitz M (1995) Rapid turnover of plasma virions and CD4 lymphocytes in HIV-1 infection. Nature 373:123-126.
56. Iversen AKN, Shafer RW, Wehrly K, Winters MA, Mullins JI, Chesebro B & Merigan TC (1996) Multidrug-resistant human immunodeficiency virus type 1 strains resulting from combination antiretroviral therapy. Journal of Virology 70:1086-1090.
57. Jacobsen H, Hänggi M, Ott M, Duncan IB, Owen S, Andreoni M, Vella S & Mous J (1996) In vivo resistance to a human immunodeficiency virus type 1 proteinase inhibitor: mutations, kinetics, and frequencies. Journal of Infectious Diseases 173:1379-1387.
58. 138→Lys on the p51 subunit. Journal of Biological Chemistry 269:25255-25258.
59. Katlama C, Ingrand D, Loveday C, Clumeck N, Mallolas J, Staszewski S, Johnson M, Hill AM, Pearce G & McDade H (1996) Safety and efficacy of lamivudine-zidovudine combination therapy in antiretroviral-naive patients. A randomized controlled comparison with zidovudine monotherapy. Journal of the American Medical Association 276:118-125.
60. Katzenstein DA, Hammer SM, Hughes MD, Gundacker H, Jackson JB, Fiscus S, Rasheed S, Elbeik T, Reichman R, Japour A, Merigan TC & Hirsch MS (1996) The relation of virologic and immunologic markers to clinical outcomes after nucleoside therapy in HIV-infected adults with 200 to 500 CD4 cells per cubic millimeter. New England Journal of Medicine 335:1091-1098.
61. Kavlick MF, Shirasaka T, Kojima E, Pluda JM, Hui F Jr, Yarchoan R & Mitsuya H (1995) Genotypic and phenotypic characterization of HIV-1 isolated from patients receiving (-)-2′,3′,-dideoxy-3′-thiacytidine. Antiviral Research 28:133-146.
62. Kaye S, Loveday C & Tedder RS (1992) A microtitre format point mutation assay: application to the detection of drug resistance in human immunodeficiency virus type-1 infected patients treated with zidovudine. Journal of Medical Virology 37:241-246.
63. Kellam P & Larder BA (1994) Recombinant virus assay: a rapid, phenotypic assay for assessment of drug susceptibility of human immunodeficiency virus type 1 isolates. Antimicrobial Agents and Chemotherapy 38:23-30.
64. Kinloch-De Loës S, Hirschel BJ, Hoen B, Cooper DA, Tindall B, Carr A, Saurat J-H, Clumeck N, Lazzarin A, Mathiesen L, Raffi F, Antunes F, von Overbeck J, Lüthy R, Glauser M, Hawkins D, Baumberger C, Yerly S, Perneger TV & Perrin L (1995) A controlled trial of zidovudine in primary human immunodeficiency virus infection. New England Journal of Medicine 333:408-413.
65. Kozal MJ, Shafer RW, Winters MA, Katzenstein DA, Aguiniga E, Halpern J & Merigan TC (1994) HIV-1 syncytium-inducing phenotype, virus burden, codon 215 reverse transcriptase mutation and CD4 cell decline in zidovudine-treated patients. Journal of Acquired Immune Deficiency Syndromes and Human Retrovirology 7:832-838.
66. Kumar RM, Hughes PF & Khurranna A (1994) Zidovudine use in pregnancy: a report on 104 cases and the occurrence of birth defects. Journal of Acquired Immune Deficiency Syndromes and Human Retrovirology 7:1034-1039.
67. Lambert JS, Seidlin M, Reichman RC, Plank CS, Laverty M, Morse GD, Knupp C, McLaren C, Pettinelli C & Valentine FT (1990) 2′,3′-dideoxyinosine (ddI) in patients with the acquired immunodeficiency syndrome or AIDS-related complex. A phase I trial. New England Journal of Medicine 322:1333-1340.
68. Lange J (1997) Issues for the future of antiretroviral therapy. Antiviral Therapy 2 (Suppl. 4):71-83.
69. Larder BA (1992) 3′-Azido-3′-deoxythymidine resistance suppressed by a mutation conferring human immunodeficiency virus type 1 resistance to nonnucleoside reverse transcriptase inhibitors. Antimicrobial Agents and Chemotherapy 36: 2664-2669.
70. Larder BA (1994) Interactions between drug resistance mutations in human immunodeficiency virus type 1 reverse transcriptase. Journal of General Virology 75:951-957.
71. Larder BA, Darby G & Richman DD (1989) HIV with reduced sensitivity to zidovudine (AZT) isolated during prolonged therapy. Science 243:1731-1734.
72. Larder BA, Kellam P & Kemp SD (1991) Zidovudine resistance predicted by direct detection of mutations in DNA from HIV-infected lymphocytes. AIDS 5:317-144.
73. Lea AP & Faulds D (1996) Stavudine. A review of its pharmacodynamic and pharmacokinetic properties and clinical potential in HIV infection. Drugs 51:846-864.
74. Lech WJ, Wang G, Yang YL, Chee Y, Dorman K, McCrae D, Lazzeroni LC, Erickson JW, Sinsheimer JS & Kaplan AH (1996) In vivo sequence diversity of the protease of human immunodeficiency virus type 1: presence of protease inhibitor-resistant variants in untreated subjects. Journal of Virology 70:2038-2043.
75. Lorenzi P, Yerly S, Abderrakim K, Fathi M, Rutschmann OT, Vonoverbeck J, Leduc D, Perrin L, Hirschel B, Battegay M, Burgisser P, Doorly R, Egger M, Erb P, Fierz W, Flepp M, Francioli P, Grob P, Gruninger U, Ledergerber B, Luthy R, Malinverni R, Matter L, Opravil M, Paccaud F, Pichler W, Rickenbach M, Ruschmann O & Vernazza P (1997) Toxicity, efficacy, plasma drug concentrations and protease mutations in patients with advanced HIV infection treated with ritonavir plus saquinavir. AIDS 11:F95-F99.
76. Lori F, Malykh AG, Foli A, Maserati R, De Antoni A, Minoli L, Padrini D, Degli Antoni A, Barchi E, Jessen H, Wainberg MA, Gallo RC & Lisziewicz J (1997) Combination of a drug targeting the cell with a drug targeting the virus controls human immunodeficiency virus type 1 resistance. AIDS Research and Human Retroviruses 13:1403-1409.
77. Markowitz M, Saag M, Powderly WG, Hurley AM, Hsu A, Valdes JM, Henry D, Sattler F, La Marca A, Leonard JM & Ho DD (1995) A preliminary study of ritonavir, an inhibitor of HIV-1 protease, to treat HIV-1 infection. New EnglandJournal of Medicine 333:1534-1539.
78. Maschera B, Furfine E &. Blair ED (1995) Analysis of resistance to human immunodeficiency virus type 1 protease inhibitors by using matched bacterial expression and proviral infection vectors. Journal of Virology 69:5431-5436.
79. Mayers DL, Japour AJ, Arduino J-M, Hammer SM, Reichman R, Wagner KF, Chung R, Lane J, Crumpacker CS, McLeod GX, Beckett LA, Roberts CR, Winslow D, Burke D & The RV43 Study Group (1994) Dideoxynucleoside resistance emerges with prolonged zidovudine monotherapy. Antimicrobial Agents and Chemotherapy 38:307-314.
80. Mellors JW, Munoz A, Giorgi JV, Margolich JB, Tassoni CJ, Gupta P, Kingsley LA, Todd JA, Saad AJ, Detels R, Phair JP & Rinaldo CR (1997) Plasma viral load and CD4+ lymphocytes as prognostic markers of HIV-1 infection. Annals of Internal Medicine 126:946-954.
81. Merigan TC & Skowron G (1990) Safety and tolerance of dideoxycytidine as a single agent. Results of early-phase studies in patients with acquired immunodeficiency syndrome (AIDS) or advanced AIDS-related complex. American Journal of Medicine 88:11S-15S.
82. Merigan TC, Skowron G, Bozzette SA, Richman D, Uttamchandani R, Fischl M, Schooley R, Hirsch M, Soo W & Pettinelli C (1989) Circulating p24 antigen levels and responses to dideoxycytidine in human immunodeficiency virus (HIV) infections. A phase I and II study. Annals of Internal Medicine 110:189-194.
83. Miles SA (1997) Long-term therapeutic strategies in HIV. Journal of Acquired Immune Deficiency Syndromes and Human Retrovirology 16 (Suppl. 1):S36-S41.
84. Miller V, Staszewski S, Boucher CAB & Phair JP (1997) Clinical experience with non-nucleoside reverse transcriptase inhibitors. AIDS 11 (Suppl. A):S157-S164.
85. Misson J, Clark W & Kendall MJ (1997) Therapeutic advances: protease inhibitors for the treatment of HIV-1 infection. Journal of Clinical Pharmacy Therapy 22:109-117.
86. Mitsuya H & Yarchoan R (1997) Development of antiretroviral therapy for AIDS and related disorders. In Textbook of AIDS Medicine, pp. 721-742. Edited by S Broder, TC Merigan and D Bolognesi. Philadelphia: Williams & Wilkins.
87. Molla A & Japour A (1997) HIV protease inhibitors. Current Opinion in Infectious Diseases 10:491-495.
88. Molla A, Korneyeva M, Gao Q, Vasavanonda S, Schipper PJ, Mo H-M, Markowitz M, Chernyavskiy T, Niu P, Lyons N, Hsu A, Granneman GR, Ho DD, Boucher CAB, Leonard JM, Norbeck DW & Kempf DJ (1996) Ordered accumulation of mutations in HIV protease confers resistance to ritonavir. Nature Medicine 2:760-766.
89. Mulato AS, Lamy PL, Li W, Miller MD & Cherrington JM (1997) Genotypic characterization of HIV-1 variants isolated from AIDS patients treated with adefovir dipivoxil (bis-POM PMEA). Antiviral Therapy 2 (Suppl. 5):29-30.
90. Najera I, Richman DD, Olivares I, Rojas JM, Peinado MA, Perucho M, Najera R & Lopez-Galindez C (1994) Natural occurence of drug resistance mutations in the reverse transcriptase of human immunodeficiency virus type 1 isolates. AIDS Research and Human Retroviruses 10:1479-1488.
91. Nakano T, Morozumi H, Inuzuka S, Nagata M, Taguchi Y, Mizokami M & Okamoto T (1997) Clonal selection of HIV type 1 variants associated with resistance to foscarnet in vitro: confirmation by molecular evolutionary analysis. AIDS Research and Human Retroviruses 13:563-573.
92. Navia MA, Fitzgerald PM, McKeever BM, Leu CT, Heimbach JC, Herber WK, Sigal IS, Darke PL & Springer JP (1989) Three-dimensional structure of aspartyl protease from human immunodeficiency virus HIV-1. Nature 337:615-620.
93. Nijhuis M, Schuurman R, de Jong D, van Leeuwen R, Lange J, Danner S, Keulen W, de Groot T & Boucher CAB (1997) Lamivudine-resistant human immunodeficiency virus type 1 variants (184V) require multiple amino acid changes to become co-resistant to zidovudine in vivo. Journal of Infectious Diseases 176:398-405.
94. O'Brien WA, Hartigan PM, Daar ES, Simberkoff MS & Hamilton JD (1997) Changes in plasma HIV RNA levels and CD4 lymphocyte counts predict both response to antiretroviral therapy and therapeutic failure. Annals of Internal Medicine 126:939-945.
95. Pantaleo G, Graziosi C, Demarest JF, Butini L, Montroni M, Fox CH, Orenstein JM, Kotler DP & Fauci AS (1993) HIV infection is active and progressive in lymphoid tissue during the clinically latent stage of disease. Nature 362:355-358.
96. Pennisi E & Cohen J (1996) Eradicating HIV from a patient: not just a dream? Science 272:1884.
97. Perelson AS, Essunger P, Cao Y, Vesanen M, Hurley A, Saksela K, Markowitz M & Ho DD (1997) Decay characteristics of HIV-1-infected compartments during combination therapy. Nature 387:188-191.
98. Perrin L &. Hirschel B (1996) Combination therapy in primary HIV infection. Antiviral Research 29:87-89.
99. Peter K & Gambertoglio JG (1996) Zidovudine phosphorylation after short-term and long-term therapy with zidovudine in patients infected with the human immunodeficiency virus. Clinical Pharmacology and Therapeutics 60:168-176.
100. Pluda JM, Cooley TP, Montaner JS, Shay LE, Reinhalter NE, Warthan SN, Ruedy J, Hirst HM, Vicary CA & Qyinn JB (1995) A phase I/II study of 2′-deoxy-3′-thiacytidine (lamivudine) in patients with advanced human immunodeficiency virus infection. Journal of Infectious Diseases 171:1438-1447.
101. Rayner MM, Cordova B & Jackson DA (1997) Population dynamics studies of wild-type and drug-resistant mutant HIV in mixed infections. Virology 236:85-94.
102. Richman DD, Fischl MA, Grieco MH, Gottlieb MS, Volberding PA, Laskin OL, Leedom JM, Groopman JE, Mildvan D, Hirsch MS et al. (1987) The toxicity of azidothymidine (AZT) in the treatment of patients with AIDS and AIDS-related complex. A double-blind, placebo-controlled trial. New England Journal of Medicine 317:192-197.
103. Richman DD, Havlir D, Corbeil J, Looney D, Ignacio C, Spector SA, Sullivan J, Cheeseman S, Barringer K, Pauletti D, Shih C-K, Myers M & Griffin J (1994) Nevirapine resistance mutations of human immunodeficiency virus type 1 selected during therapy. Journal of Virology 68:1660-1666.
104. Rowe PM (1997) Breaking the mother-to-child transmission of HIV-1. Lancet 350:788.
105. Rubio R, Leal M, Pineda JA, Caruz A, Luque F, Rey C, Sanchezquijano A & Lissen E (1997) Increase in the frequency of mutation at codon 215 associated with zidovudine resistance in HIV-1 infected antiviral naive patients from 1989 to 1996. AIDS 11:1184-1186.
106. Saag MS, Emini EA, Laskin OL, Douglas J, Lapidus WI, Schleif WA, Whitley RJ, Hildebrand C, Byrnes VW, Kappes JC, Anderson KW, Massari FE, Shaw GM & The L-697 6W (1993) A short-term clinical evaluation of L-697,661, a non-nucleoside inhibitor of HIV-1 reverse transcriptase. New England Journal of Medicine 329:1065-1072.
107. Saag MS, Holodniy M, Kuritzkes DR, O'Brien WA, Coombs R, Poscher ME, Jacobsen DM, Shaw GM, Richman DD & Volberding PA (1996) HIV viral load markers in clinical practice. Nature Medicine 2:625-629.
108. Sanford JP, Gilbert DN, Moellering RC & Sande MA (1997) The Sanford Guide to HIV/AIDS Therapy. Dallas & Vienna, USA: Antimicrobial Therapy.
109. Schapiro JM, Winters MA, Stewart F, Efron B, Norris J, Kozal MJ & Merigan TC (1996) The effect of high-dose saquinavir on viral load and CD4(+) T-cell counts in HIV-infected patients. Annals of Internal Medicine 124:1039-1050.
110. Schinazi RF, Larder BA & Mellors JW (1997) Mutations in retroviral genes associated with drug resistance. International Antiviral News 5:129-142.
111. Schmit J-C, Clotet B, Ruiz L, Hermans P, Sprecher S, Arendt V, Leal M, Lissen E, Harrer T, De Clercq E, Witvrouw M & Vandamme A-M (1997) Multiple dideoxynucleoside analogue-resistant HIV-1 in Europe. Antiviral Therapy 2 (Suppl. 5):39.
112. Schmit J-C, Cogniaux J, Hermans P, Van Vaeck C, Sprecher S, Van Remoortel B, Witvrouw M, Balzarini J, Desmyter J, De Clercq E & Vandamme A-M (1996b) Multiple drug resistance to nucleoside analogues and nonnucleoside reverse transcriptase inhibitors in an efficiently replicating human immunodeficiency virus type 1 patient strain. Journal of Infectious Diseases 174:1-7.
113. Schmit J-C, Martinez-Picado J, Ruiz L, Tural C, Van Laethem K, Cabrera C, Ibanez A, Puig T, Witvrouw M, Desmyter J, De Clercq E, Clotet B & Vandamme A-M (1998a) Evolution of HIV drug resistance in zidovudine/zalcitabine- and zidovudine/didanosine-experienced patients receiving lamivudine-containing combination therapy. Antiviral Therapy (in press).
114. Schmit J-C, Ruiz L, Clotet B, Raventos A, Tor J, Leonard J, Desmyter J, De Clercq E & Vandamme A-M (1996a) Resistance-related mutations in the HIV-1 protease gene of patients treated for 1 year with the protease inhibitor ritonavir (ABT-538). AIDS 10:995-999.
115. Schmit JC, Ruiz L, Stuyver L, Van Laethem K, Van der Linden I, Puig T, Rossau R, Desmyter J, De Clercq E, Clotet B & Vandamme A-M (1998b) Comparison of the LiPA HIV-1 RT test, selective PCR and direct solid phase sequencing for the detection of HIV-1 drug resistance mutations. Journal of Virological Methods (in press).
116. Schooley RT (1997) Changing treatment strategies and goals. Antiviral Therapy 2 (Suppl. 4):59-70.
117. Schuurman R (1997) State of the art of genotypic HIV-1 drug resistance. Current Opinion in Infectious Diseases 10:480-484.
118. Schuurman R, Nijhuis M, van Leeuwen R, Schipper P, de Jong D, Collis P, Danner SA, Mulder J, Loveday C & Christopherson C (1995) Rapid changes in human immunodeficiency virus type 1 RNA load and appearance of drug-resistant virus populations in persons treated with lamivudine (3TC). Journal of Infectious Diseases 171:1411-1419.
119. Seligmann M, Warrel DA, Aboulker JP, Carbon C, Darbyshire JH, Dormont J, Eschwege E, Girling DJ, James DR, Levy JP, Peto TEA, Schwarz D, Stone AB, Weller IVD, Withnall R, Gelmon K & Lafon E (1994) Concorde-MRC/ANRS randomized double-blind controlled trial of immediate and deferred zidovudine in symptom-free HIV infection. Lancet 343:871-881.
120. Shafer RW, Kozal MJ, Winters MA, Iversen AKN, Katzenstein DA, Ragni MV, Meyer III WA, Gupta P, Rasheed S, Coombs R, Katzman M, Fiscus S & Merigan TC (1994) Combination therapy with zidovudine and didanosine selects for drug-resistant human immunodeficiency virus type 1 strains with unique patterns of pol gene mutations. Journal of Infectious Diseases 169:722-729.
121. Shao W, Everitt L, Manchester M, Loeb DD, Hutchison CA & Swanstrom R (1997) Sequence requirements of the HIV-1 protease flap region determined by saturation mutagenesis and kinetic analysis of flap mutants. Proceedings of the National Academy of Sciences, USA 94:2243-2248.
122. Sharma PL & Crumpacker CS (1997) Attenuated replication of human immunodeficiency virus type 1 with a didanosine-selected reverse transcriptase mutation. Journal of Virology 71:8846-8851.
123. Shirasaka T, Kavlick MF, Ueno T, Gao W-Y, Kojima E, Alcaide ML, Chokekijchai S, Roy BM, Arnold E, Yarchoan R & Mitsuya H (1995) Emergence of human immunodeficiency virus type 1 variants with resistance to multiple dideoxynucleosides in patients receiving therapy with dideoxynucleosides. Proceedings of the National Academy of Sciences, USA 92:2398-2402.
124. Siegrist CA, Yerly S, Kaiser L, Wyler CA & Perrin L (1994) Mother to child transmission of zidovudine-resistant HIV-1. Lancet 344:8939-8944.
125. Staszewski S, Loveday C, Picazo JJ, Dellarnonica P, Skinhoj P, Johnson MA, Danner SA, Harrigan PR, Hill AM, Verity L & McDade H (1996) Safety and efficacy of lamivudine-zidovudine combination therapy in zidovudine-experienced patients. A randomized controlled comparison with zidovudine monotherapy. Journal of the American Medical Association 276:111-117.
126. St Clair MH, Martin JL, Tudor-Williams G, Bach MC, Vavro CL, King DM, Kellam P, Kemp SD & Larder BA (1991) Resistance to ddI and sensitivity to AZT induced by a mutation in HIV-1 reverse transcriptase. Science 253:1557-1559.
127. Stein DS, Fish DG, Bilello JA, Preston SL, Martineau GL & Drusano GL (1996) A 24-week open-label phase I/II evaluation of the HIV protease inhibitor MK-639 (indinavir). AIDS 10:485-492.
128. Stephenson J (1997) The art of 'HAART': researchers probe the potential and limits of aggressive HIV treatments. Journal of the American Medical Association 277:614-616.
129. Stuyver L, Wyseur A, Rombout A, Louwagie J, Scarcez T, Verhofstede C, Rimland D, Schinazi RF & Rossau R (1997) Line probe assay for rapid detection of drug-selected mutations in the human immunodeficiency virus type 1 reverse transcriptase gene. Antimicrobial Agents and Chemotherapy 41:284-291.
130. Tachedjian G, Mellors J, Bazmi H, Birch C & Mills J (1996) Zidovudine resistance is suppressed by mutations conferring resistance of human immunodeficiency virus type 1 to foscarnet. Journal of Virology 70:7171-7181.
131. Tantillo C, Ding J, Jacobo-Molina A, Nanni RG, Boyer PL, Hughes SH, Pauwels R, Andries K, Janssen PAJ & Arnold E (1994) Locations of anti-AIDS drug binding sites and resistance mutations in the three-dimensional structure of HIV-1 reverse transcriptase. Journal of Molecular Biology 243:369-387.
132. Tozser J, Yin FH, Cheng YSE, Bagossi P, Weber IT, Harrison RW & Oroszlan S (1997) Activity of tethered human immunodeficiency virus 1 protease containing mutations in the flap region of one subunit. European Journal of Biochemistry 244:235-241.
133. Tseng AL & Foisy MM (1997) Management of drug interactions in patients with HIV. Annals of Pharmacotherapy 31:1040-1058.
134. Ueno T, Shirasaka T & Mitsuya H (1995) Enzymatic characterization of human immunodeficiency virus type 1 reverse transcriptase resistant to multiple 2′,3′-dideoxynucleoside 5′-triphosphates. Journal of Biological Chemistry 270:23605-23611.
135. van Leeuwen R, Katlama C, Kitchen V, Boucher CA, Tubiana R, McBride M, Ingrand D, Weber J, Hill A & McDade H (1995) Evaluation of safety and efficacy of 3TC (lamivudine) in patients with asymptomatic or mildly symptomatic human immunodeficiency virus infection: a phase I/II study. Journal of Infectious Diseases 171:1166-1171.
136. Vandamme A-M, Debyser Z, Pauwels R, De Vreese K, Goubau P, Youle M, Gazzard B, Stoffels A, Cauwenbergh G, Anné J, Andries K, Janssen PAJ, Desmyter J & De Clercq E (1994) Characterization of HIV-1 strains isolated from patients treated with TIBO R82913. AIDS Research and Human Retroviruses 10:39-45.
137. Vandamme A-M, Harrer T, Van Laethem K, De Vroey V, Rascu A, Grunke M, Low P, Kalden JR, Desmyter J & De Clercq E (1997) Lack of resistance mutations (including M184V) in treatment-naive HIV-1 seropositives for up to 7 months after initiation of a lamivudine-containing three-or four-drug combination therapy, except for one patient with previous zidovudine resistance. Antiviral Therapy 2 (Suppl. 5):123.
138. Vandamme A-M, Witvrouw M, Pannecouque C, Balzarini J, Schmit J-C, Desmyter J & De Clercq E (1998) Evaluating clinical isolates for their phenotypic and genotypic resistance against anti-HIV drugs. In Methods in Cellular and Molecular Biology: Antiviral Evaluation (in press). Edited by D Kinchington and RF Schinazi. Totowa: Humana Press.
139. Volberding PA (1994) Treatment dilemmas in HIV infection. Hospital Practice 27:49-60.
140. von der Helm K, Seelmeier S, Kisselev A & Nitschko H (1994) Identification, purification and cell culture assays of retroviral proteases. In Retroviral Proteases, pp. 89-105. Edited by LC Kuo and JA Shafer. New York: Academic Press.
141. Wei X, Ghosh SK, Taylor ME, Johnson VA, Emini EA, Deutsch P, Lifson JD, Bonhoeffer S, Nowak MA, Hahn BH, Saag MS & Shaw GM (1995) Viral dynamics in human immunodeficiency virus type 1 infection. Nature 373:117-121.
142. Wilde MI & Langtry HD (1993) Zidovudine in perspective. Drugs 46:515-578.
143. Wilson SI, Phylip LH, Mills JS, Gulnik SV, Erickson JW, Dunn BM & Kay J (1997) Escape mutants of HIV-1 proteinase: enzymic efficiency and susceptibility to inhibition. Biochimica et Biophysica Acta 1339:113-125.
144. Wilson JE, Aulabaugh A, Caligan B, McPherson S, Wakefield JK, Jablonski S, Morrow CD, Reardon JE & Furman PA (1996) Human immunodeficiency virus type-1 reverse transcriptase. Contribution of Met-184 to binding of nucleoside 5′-triphosphate. Journal of Biological Chemistry 271:13656-13662.
145. Winters MA, Schapiro JM, Lawrence J & Merigan TC (1997) Genotypic and phenotypic analysis of the protease gene in HIV-1-infected patients that failed long-term saquinavir therapy and switched to other protease inhibitors. Antiviral Therapy 2 (Suppl. 5):25-26.
146. Wlodawer A, Miller M, Jaskolski M, Sathyanarayana BK, Baldwin E, Weber IT, Selk LM, Clawson L, Schneider J & Kent SB (1989) Conserved folding in retroviral proteases: crystal structure of a synthetic HIV-1 protease. Science 245:616-621.
147. Yarchoan R, Klecker RW, Weinhold KJ, Markham PD, Lyerly HK, Durack DT, Gelmann E, Lehrman SN, Blum RM & Barry DW (1986) Administration of 3′-azido-3′-deoxythymidine, an inhibitor of HTLV-III/LAV replication, to patients with AIDS or AIDS-related complex. Lancet i:575-580.
148. Yarchoan R, Perno CF, Thomas RV, Klecker RW, Allain JP, Wills RJ, McAtee N, Fischl MA, Dubinsky R, McNeely MC, et al. (1988) Phase I studies of 2′,3′-dideoxycytidine in severe human immunodeficiency virus infection as a single agent and alternating with zidovudine (AZT). Lancet i:76-81.
149. Zhang Y-M, Imamichi H, Imamichi T, Lane HC, Falloon J, Vasudevachari MB & Salzman NP (1997) Drug resistance during indinavir therapy is caused by mutations in the protease gene and in its Gag substrate cleavage sites. Journal of Virology 71:6662-6670.