A 24-week open-label phase I/II evaluation of the HIV protease inhibitor MK-639 (indinavir)

AIDS

Volumn 10, Issue 5, 1996, Pages 485-492

  Stein, Daniel S ^a   Fish, Douglas G ^a   Bilello, John A ^a   Preston, Sandra L ^b   Martineau, Gisele L ^a   Drusano, George L ^a  

^a ALBANY MEDICAL COLLEGE   (United States)

^b ALBANY COLLEGE OF PHARMACY AND HEALTH SCIENCES   (United States)

Author keywords

Antiviral therapy; Clinical trial; HIV; Mathematical modelling; Protease inhibitors

Indexed keywords

ANTIVIRUS AGENT; CD4 ANTIGEN; INDINAVIR; PROTEINASE INHIBITOR; TUMOR NECROSIS FACTOR RECEPTOR; VIRUS RNA;

ADULT; ANTIVIRAL ACTIVITY; ARTICLE; CLINICAL ARTICLE; CLINICAL TRIAL; COMPARTMENT MODEL; DRUG SAFETY; DRUG TOLERABILITY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; LYMPHOCYTE COUNT; MALE; MATHEMATICAL MODEL; NAUSEA; ORAL DRUG ADMINISTRATION; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; PRIORITY JOURNAL; RASH;

EID: 0029872589     PISSN: 02699370     EISSN: None     Source Type: Journal    
DOI: 10.1097/00002030-199605000-00006     Document Type: Article

References (27)

1. Debouck C: The HIV-1 protease as a therapeutic target for AIDS. AIDS Res Hum Retroviruses 1992, 8:153-160.
2. Dorsey BD, Levin RB, McDaniel SL, et al.: L-735524: the design of a potent and orally bioavailable HIV protease inhibitor. J Med Chem 1994, 37:3443-3451.
3. 3. 2nd Annual National Conference on Human Retroviruses and Related Infections. Washington, DC, January-February 1995 [abstract 183].
4. Jacobsen H, Yasargil K, Winslow DL, et al.: Characterization of human immunodeficiency virus type 1 mutants with decreased sensitivity to proteinase Ro 31-8959. Virology 1995, 206:527 534.
5. Markowitz M, Mo H, Kempf DJ, et al.: Selection and analysis of human immunodeficiency virus type 1 variants with increased resistance to ABT-538, a novel protease inhibitor. J Virol 1995, 69:701-706.
6. 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.
7. Gelman R, Cheng SC, Kidd P, Waxdal M, Kagan J: Assessment of the effects of instrumentation, monoclonal antibody, and fluorochrome on flow cytometric immunophemotyping: a report based on 2 years of the NIAID DAIDS flow cytometry quality assessment program. Clin Immunol Immunopathol 1993, 66:150-162.
8. Mulder J, McKinney N, Christopheron C, et al.: Rapid and simple PCR assay for quantitation of human immunodeficiency virus type 1 RNA in plasma: application to acute retroviral infection. J Clin Microbiol 1994, 32:292-300.
9. Woolf E, Au T, Haddix H, Matuszewski B: Determination of L-735524, a human immunodeficiency virus protease inhibitor, in human plasma and urine via high-performance liquid chromatography with column switching. J Chromatogr JAJ 1995, 692:45-52.
10. D'Argenio DZ, Schumitzky A: ADAPT II. A Program Package for Simulation, Identification, and Optimal Experimental Design. Users Manual. Los Angeles: Biomedical Simulations Resource, University of Southern California; 1992.
11. Drusano GL, Yuen GJ, Lambert JS, et al.: Quantitative relationships between dideoxyinosine exposure and surrogate markers of response in a phase I trial. Ann Intern Med 1992, 116:562-566.
12. Drusano GL, Balis FM, Gitterman SR, Pizzo PA: Quantitative relationships between zidovudine exposure and efficacy and toxicity. Antimicrob Agents Chemother 1994, 38:1726-1731.
13. Godfried MH, van der Poll T, Weverling GJ, et al.: Soluble receptors for tumor necrosis factor as predictors of progression to AIDS in asymptomatic human immunodeficiency virus type 1 infection. J Infect Dis 1994, 169:739-745.
14. Kahn JO, Lagakos SW, Richman DD, et al.: A controlled trial comparing continued zidovudine with didanosine in human immunodeficiency virus infection. N Engl J Med 1992, 327:581-587.
15. Abrams DI, Goldman AI, Launer C, et al.: A comparative trial of didanosine or zalcitabine after treatment with zidovudine in patients with human immunodeficiency virus infection. N Engl J Med 1994, 330:657-662.
16. Spruance SL, Pavia AT, Peterson D, et al.: Didanosine compared with continuation of zidovudine in HIV-infected patients with signs of clinical deterioration while receiving zidovudine. Ann Intern Med 1994, 120:360-368.
17. Fischl MA, Stanley K, Collier AC, et al.: Combination and monotherapy with zidovudine and zalcitabine in patients with advanced HIV disease. Ann Intern Med 1995, 122:24-32.
18. Kitchen VS, Skinner C, Ariyoshi K, et al.: Safety and activity of saquinavir in HIV infection. Lancet 1995, 345:952-955.
19. Graham NMH, Park LP, Piantadosi S, et al.: Prognostic value of combined response markers among human immunodeficiency virus-infected persons: possible aid in the decision to change zidovudine monotherapy. Clin Infect Dis 1995, 20:352-362.
20. Katzenstein DA, Winters M, Bubp J, Israelski D, Winger E, Merigan TC: Quantitation of human immunodeficiency virus by culture and polymerase chain reaction in response to didanosine after long-term therapy with zidovudine. J Infect Dis 1994, 169:416-419.
21. Lu W, Andrieu JM: Early identification of human immunodeficiency virus infected asymptomatic subjects susceptible to zidovudine by quantitative viral co-culture and reverse transcription linked polymerase chain reaction. J Infect Dis 1993, 167:1014-1020.
22. Holodniy M, Katzenstein DA, Israelski DM, Merigan TC: Reduction in plasma human immunodeficiency virus ribonucleic acid after dideoxynucleoside therapy as determined by the polymerase chain reaction. J Clin Invest 1991, 88:1755-1759.
23. Grasela TH, Sheiner LB, Rambeck B, et al.: Steady state pharmacokinetics of phenytoin from routinely collected patient data. Clin Pharmacokinet 1983, 8:355-364.
24. Ho DD, Neumann AU, Perelson AS, Chen W, Leonard JM, Markowitz M: Rapid turnover of plasma virions and CD4 lymphocytes in HIV-1 infection. Nature 1995, 373:123-126.
25. Wei X, Ghosh SK, Taylor ME, et al.: Viral dynamics in human immunodeficiency virus type 1 infection. Nature 1995, 373:117-122.
26. Hill AV: The possible effects of the aggregation of the molecules of haemoglobin on its dissociation curves. J Physiology 1910, 40:iv-vii.
27. Holford NHG, Sheiner LB: Understanding the dose-effect relationship: clinical application of pharmacokinetic-pharmacodynamic models. Clin Pharmacokinet 1981, 6:429-453.