Protease inhibitors: A therapeutic breakthrough for the treatment of patients with human immunodeficiency virus

Clinical Therapeutics

Volumn 19, Issue 2, 1997, Pages 187-214

  Lewis II, James S ^a   Tariff, Colleen M ^a,b   Coulston, Daniel R ^b   Garrison, Mark W ^a  

^a WASHINGTON STATE UNIVERSITY   (United States)

^b Deaconess Medical Center Spokane   (United States)

Author keywords

human immunodeficiency virus; indinavir; nelfinavir; protease inhibitors; ritonavir; saquinavir

Indexed keywords

ANTIRETROVIRUS AGENT; INDINAVIR; KETOCONAZOLE; LAMIVUDINE; NELFINAVIR; PHENOBARBITAL; PROTEINASE INHIBITOR; RIFABUTIN; RIFAMPICIN; RITONAVIR; RNA DIRECTED DNA POLYMERASE INHIBITOR; SAQUINAVIR; ZALCITABINE; ZIDOVUDINE;

ABDOMINAL DISCOMFORT; CLINICAL TRIAL; DIARRHEA; DRUG FORMULATION; DRUG INHIBITION; DRUG METABOLISM; DRUG RESISTANCE; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; LACTATION; MAXIMUM PERMISSIBLE DOSE; NAUSEA; NEPHROLITHIASIS; OPPORTUNISTIC INFECTION; ORAL DRUG ADMINISTRATION; PARESTHESIA; PREGNANCY; REVIEW; SIDE EFFECT;

EID: 8244248789     PISSN: 01492918     EISSN: 1879114X     Source Type: Journal    
DOI: 10.1016/S0149-2918(97)80110-5     Document Type: Article

References (89)

1. Food and Drug Administration, US Department of Health and Human Services. FDA approvals in 1996 set new records. FDA Talk Paper. 1997; 14 January. http://www.fda.gov/bbs/topics/ANSWERS/ ANS00781.html.
2. Collier AC, Coombs RW, Schoenfeld DA, et al. Treatment of human immunodeficiency virus infection with saquinavir, zidovudine and zalcitabine. NEJM. 1996; 334:1011-1017.
3. Mathez D, Bagnarelli P, De Truchis P, et al. A triple combination of ritonavir + AZT + ddC as a first line treatment of patients with AIDS: Update. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract Mo.B.175.
4. Stein DS, Fish DG, Bilello JA, et al. A 24-week open-label phase I/II evaluation of the HIV protease inhibitor MK-639 (indinavir). AIDS. 1996; 10:485-492.
5. Markowitz M, Cao Y, Hurley A, et al. Triple therapy with AZT and 3TC in combination with nelfinavir mesylate in 12 antiretroviral naive subjects chronically infected with HIV-1. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract LB.B.6031.
6. Cameron DW, Heath-Chiozzi M, Kravcik S, et al. Prolongation of life and prevention of AIDS complications in advanced HIV immunodeficiency with ritonavir: Update. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract Mo.B.411.
7. Carpenter CC, Fischl MA, Hammer SM, et al. Recommendations of an international panel: Antiretroviral therapy for HIV infection in 1996. JAMA. 1996;276: 146-154.
8. Larder BA, Darby G, Richman DD. HIV with reduced sensitivity to zidovudine isolated during prolonged therapy. Science. 1989;243:1731-1734.
9. Condra JH, Schleif WA, Blahy OM, et al. In vivo emergence of HIV-1 variants resistant to multiple protease inhibitors. Nature. 1995;374:569-571.
10. How the protease inhibitors work: Their mechanism of action, with schematic color illustrations. HIV Newsline. 1996;2:Insert.
11. Mellors JW. HIV-1 protease inhibitors: Historical perspective and basic science. Infect Med. 1996;13(Suppl F):9-15.
12. Kitchen VS, Skinner C, Ariyoshi K, et al. Safety and activity of saquinavir in HIV infection. Lancet. 1995;345:952-955.
13. Invirase® (saquinavir) package insert. Nutley, NJ: Roche Laboratories Inc.
14. Schapiro JM, Winters MA, Stewart F, et al. The effect of high-dose saquinavir on viral load and CD4+ T-cell counts in HIV infected patients. Ann Intern Med. 1996; 124:1039-1050.
15. Lalezari J, Haubrich R, Burger HU, et al. Improved survival and decreased progression of HIV in patients treated with saquinavir plus Hivid. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract LB.B.6033.
16. Salgo MP, Beattie D, Bragman K, et al. Saquinavir vs. Hivid vs. combination as treatment for advanced HIV infection in patients discontinuing/unable to take Retrovir. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract Mo.B.410.
17. Testa MA, Lenderking WR, Fischer L, et al. Effects of combination therapy with saquinavir, zidovudine, and zalcitabine on quality of life. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract Tu.B.542.
18. Workman C, Downie J, Sutherland D, et al. Rapid viral load decrease in primary infection associated with aggressive therapy. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract LB.B.6021.
19. Kravcik S, Sahai J, Kerr B, et al. Nelfinavir mesylate increases saquinavir soft gel capsule exposure in HIV+ patients. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 389.
20. McCrea J, Buss N, Stone J, et al. Indinavir-saquinavir single dose pharmacokinetic study. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 432.
21. Hsu A, Granneman GR, Sun E, et al. Assessment of single- and multiple-dose interactions between ritonavir and saquinavir. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract LB.B.6041.
22. Cox SR, Batts DH, Stewart F, et al. Evaluation of the pharmacokinetic interaction between saquinavir and delavirdine in healthy volunteers. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 381.
23. Sahai J, Cameron W, Salgo M, et al. Drug interaction study between saquinavir and nevirapine. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 496.
24. Sahai J, Stewart F, Swick L, et al. Rifabutin reduces saquinavir plasma levels in HIV-infected patients. In: Program and Abstracts of the 36th Interscience Conference on Antimicrobial Agents and Chemotherapy, American Society for Microbiology; September 15-18, 1996; New Orleans. Abstract A027.
25. Norvir® (ritonavir) package insert. Abbott Park, Ill: Abbott Laboratories, Pharmaceutical Products Division.
26. Barnett AA. Protease inhibitors fly through FDA. Lancet. 1996;347:678.
27. Danner SA, Carr A, Leonard JM, et al. A short term study of the safety, pharmacokinetics, and efficacy of ritonavir, an inhibitor of HIV-1 protease. NEJM. 1995; 333;1528-1533.
28. Markowitz M, Saag M, Powderly WG, et al. A preliminary study of ritonavir, an inhibitor of HIV-1 protease, to treat HIV-1 infection. NEJM. 1995;333:1534-1539.
29. Kumar GN, Rodrigues AD, Buko AM, Denissen JF. Cytochrome P450-mediated metabolism of the HIV-1 protease inhibitor ritonavir in human liver microsomes. J Pharmacol Exp Ther. 1996;277: 423-431.
30. Kelleher AD, Carr A, Zaunders J, Cooper DA. Alterations in the immune response of human immunodeficiency virus-infected subjects treated with an HIV-specific protease inhibitor, ritonavir. J Infect Dis. 1996;173:321-329.
31. Markowitz M, Cao Y, Hurley A, et al. Triple therapy with AZT, 3TC, and ritonavir in 12 subjects newly infected with HIV-1. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract Th.B.933.
32. Bertz R, Shi H, Cavanaugh J, Hsu A. Effects of three vehicles, Advera®, Ensure®, and chocolate milk, on the bioavailability of an oral liquid formulation of Norvir™. In: Program and Abstracts of the 36th Interscience Conference on Antimicrobial Agents and Chemotherapy, American Society for Microbiology; September 15-18, 1996; New Orleans. Abstract A025.
33. Duong M, Sgro C, Grappin M, et al. Renal failure after treatment with ritonavir. Lancet. 1996;348:693-694.
34. Chugh S, Bird R, Alexander EA. Ritonavir and renal failure. NEJM. 1997;336: 138.
35. Lamson M, Gagnier P, Greguski R, et al. Effect of nevirapine on pharmacokinetics of ritonavir in HIV-1 patients. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 556.
36. Ferry JJ, Schneck DW, Carlson GF, et al. Evaluation of the pharmacokinetic interaction between ritonavir and delavirdine in healthy volunteers. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 385.
37. Gerber JG. Drug interactions with HIV protease inhibitors. Improving the Management of HIV Disease. 1996;4:20-23.
38. Sun E, Heath-Chiozzi M, Cameron DW, et al. Concurrent ritonavir and rifabutin increase risk of rifabutin associated adverse events. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract Mo.B.171.
39. Bertz RJ, Cao G, Cavanaugh JH, et al. Effect of ritonavir on the pharmacokinetics of trimethoprim/sulfamethoxazole. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract Mo.B.1197.
40. Mars ME, Loi S, Suzan V, Gallais H. Indinavir, saquinavir, ritonavir: A comparative trial. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 537.
41. Gulick R, Mellors J, Havlir D, et al. Potent and sustained antiretroviral activity of indinavir, zidovudine and lamivudine. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract Th.B.931.
42. 3. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract LB.B.6019.
43. Crixivan® (indinavir sulfate) package insert. West Point, Pa: Merck & Co, Inc.
44. Stein D, Drusano G, Steigbigel R, et al. Two year follow-up of patients treated with indinavir 800 mg q8h. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 410.
45. Tashima KT, Horowitz JD, Rosen S. Indinavir nephropathy. NEJM. 1997;336: 138-139.
46. Chodakewitz JA, Leavitt R, Massari F, et al. Crixivan: Summary of 24-week experience with Crixivan at 2.4 g/d in phase II trials. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract Mo.B.1144.
47. Yuen G, Anderson R, Daniels R, Kerr B. Investigations of nelfinavir mesylate pharmacokinetic interactions with indinavir and ritonavir. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 428.
48. Ferry JJ, Herman BD, Cox SR, et al. Delavirdine and indinavir: A pharmacokinetic drug-drug interaction study in healthy adult volunteers. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 121.
49. Murphy R, Gagnier P, Lamson M, et al. Effect of nevirapine on pharmacokinetics of indinavir and ritonavir in HIV-1 patients. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 374.
50. The Indinavir Pharmacokinetic Study Group. Indinavir drug interaction studies. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract Mo.B.174.
51. De Wit S, Turner D, Debier M, et al. Absence of interaction between indinavir and fluconazole: A pharmacokinetic study in HIV patients. In: Program and Abstracts of the 36th Interscience Conference on Antimicrobial Agents and Chemotherapy, American Society for Microbiology; September 15-18, 1996; New Orleans. Abstract A026.
52. PRNewswire. Agouron Pharmaceuticals, Inc. Agouron Files New Drug Application for Anti-HIV Drug Viracept®. 12/23/96 09:01 EST. http://www.prnewswire.com.
53. Conant MA, Markowitz M, Hurley A, et al. A randomized phase II dose range-finding study of the HIV protease inhibitor Viracept™ as monotherapy in HIV positive patients. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract Tu.B.2129.
54. Pedneault L, Elion R, Adler M, et al. Stavudine, didanosine, and nelfinavir combination therapy in HIV-infected subjects: Antiviral effect and safety in an ongoing pilot study. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 406.
55. Viracept® (nelfinavir mesylate) package insert. La Jolla, Calif: Agouron Pharmaceuticals, Inc.
56. Viracept® (nelfinavir mesylate) physician information brochure. La Jolla, Calif: Agouron Pharmaceuticals, Inc. 1996.
57. Henry K, Lamarca A, Myers R, Chapman S. The safety of Viracept in pivotal phase II/III double-blind randomized controlled trials as monotherapy and in combination with either d4T or AZT/3TC. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 384.
58. Kerr B, Yuen G, Daniels R, et al. Strategic approach to nelfinavir mesylate drug interactions involving CYP3A metabolism. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 429.
59. Lee CA, Liang B, Wu EY, et al. Prediction of nelfinavir mesylate clinical drug interactions based on in vitro human P450 metabolism studies. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 523.
60. Richman DD. HIV drug resistance. AIDS Res Hum Retroviruses. 1992;8;1065-1071.
61. Molla A, Korneyeva M, Gao Q, et al. Ordered accumulation of mutations in HIV protease confers resistance to ritonavir. Nat Med. 1996;2:760-766.
62. Erickson JW, Bhat TN, Yu B, et al. Mechanisms of drug resistance for HIV-1 protease mutants. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 50.
63. Jacobsen H, Hänggi M, Ott M, et al. In vivo resistance to a human immunodeficiency virus type 1 proteinase inhibitor: Mutations, kinetics, and frequencies. J Infect Dis. 1996;173:1379-1387.
64. Jacobsen H, Hänggi M, Ott M, et al. Reduced sensitivity to saquinavir: An update on genotyping from phase I/II trials. Antiviral Res. 1996;29:95-97.
65. Vella S, Galluzzo C, Giannini G, et al. Saquinavir/zidovudine combination in patients with advanced HIV infection and no prior antiretroviral therapy: CD4+ lymphocyte/plasma RNA changes, and emergence of HIV strains with reduced phenotypic sensitivity. Antiviral Res. 1996; 29:91-93.
66. Condra JH, Schleif WA, Blahy OM, et al. In vivo evolution of resistance to the HIV-1 protease inhibitor indinavir. In: Program and Abstracts of the Third Conference on Retroviruses and Opportunistic Infections; January 28-February 1, 1996; Washington, DC. Abstract 145.
67. Condra JH, Holder DJ, Schleif WA, et al. Genetic correlates of in vivo viral resistance to indinavir, a human immunodeficiency virus type 1 protease inhibitor. J Virol. 1996;70:8270-8276.
68. Patick AK, Duran M, Cao Y, et al. Genotypic and phenotypic characterization of HIV-1 variants isolated from in vitro selection studies and from patients treated with the protease inhibitor, nelfinavir. In: Abstracts of the Fifth International Workshop on HIV Drug Resistance; July 3-6, 1996; Whistler, British Columbia. Abstract 29.
69. Patick AK, Mo H, Markowitz M, et al. Antiviral and resistance studies of AG 1343, an orally bioavailable inhibitor of human immunodeficiency virus protease. Antimicrob Agents Chemother. 1996;40: 292-297.
70. Flexner C. HIV protease inhibitors: Plasma protein binding and pharmacodynamics. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 48.
71. Cohen C, Sun E, Cameron W, et al. Ritonavir-saquinavir combination treatment in HIV-infected patients. In: Program and Abstracts of the 36th Interscience Conference on Antimicrobial Agents and Chemotherapy, American Society for Microbiology; September 15-18, 1996; New Orleans. Abstract LB07B.
72. Rose RE, Gong Y, Greytok JA, et al. Human immunodeficiency virus type 1 viral background plays a major role in development of resistance to protease inhibitors. Proc Natl Acad Sci. 1996;93: 1648-1653.
73. Paulous S, Clavel F. Sequential selection by protease inhibitors: Effects of ritonavir resistance on further selection for HIV resistance to saquinavir. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 483.
74. Granneman GR, Hsu A, Sun E, et al. Pharmacokinetics/pharmacodynamics of ritonavir-saquinavir combination therapy. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 521.
75. Angel JB, Parato K, Kumar A, et al. Rapid improvement in cell mediated immune function with initiation of ritonavir plus saquinavir in HIV immune deficiency. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 147.
76. Hirschel BJ, Rutschmann O, Fathi M, et al. Treatment of advanced HIV infection with ritonavir plus saquinavir. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract LB.B.6030.
77. Steinhart CR, George SA, Mann RD. Salvage therapy using the combination of ritonavir and saquinavir in patients with advanced HIV infection. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 492.
78. Hirschel B, Lorenzi P, Yerly S, et al. Escape of viremia and rapid development of protease mutations in advanced HIV infection treated with saquinavir plus ritonavir. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 524.
79. Merrill DP, Manion DJ, Chou T, Hirsch MS. Protease inhibitor combination regimens against HIV in vitro. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 370.
80. PRNewswire. Agouron Pharmaceuticals, Inc. Agouron Reports Positive Results from Pivotal Clinical Trials of Viracept. Thursday January 23 6:47 pm EDT. http://www.prnewswire.com.
81. Mueller BU, Zuckerman J, Nelson RP Jr, et al. A phase I/II study of the protease inhibitor ritonavir in children with HIV infection. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract We.B.551.
82. Mueller BU, Zuckerman J, Nelson RP Jr, et al. Update on the pediatric phase I/II study of the protease inhibitor ritonavir. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 394.
83. Mueller BU, Smith S, Sleasman J, et al. A phase I/II study of the protease inhibitor indinavir in children with HIV infection. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract We.B.554.
84. Krogstad P, Kerr B, Anderson R, et al. Phase I study of the HIV-protease inhibitor nelfinavir mesylate in HIV+ children. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 392.
85. Zingman BS. Resolution of refractory AIDS-related mucosal candidiasis after initiation of didanosine plus saquinavir. NEJM. 1996;334:1674-1675.
86. Workman C, Lewis C, Smith DO. Resolution of Kaposi's sarcoma associated with saquinavir therapy - case report. In: Program and Abstracts of the XI International Conference on AIDS; July 7-12, 1996; Vancouver, British Columbia. Abstract Tu.B.2217.
87. Henry K, Worley J, Sullivan C, et al. Documented improvement in late stage manifestations of AIDS after starting ritonavir in combination with two reverse transcriptase inhibitors. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 697.
88. Benhamou Y, Bochet MV, Carriere J, et al. Effects of triple antiretroviral therapies including a HIV protease inhibitor on chronic intestinal cryptosporidiosis and microsporidiosis in HIV-infected patients. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 499.
89. Mileno MD, Tashima K, Farrar D, et al. Resolution of AIDS-related opportunistic infections with addition of protease inhibitor treatment. In: Program and Abstracts of the Fourth Conference on Retroviruses and Opportunistic Infections; January 22-26, 1997; Washington, DC. Abstract 657.