Antiviral and resistance studies of AG1343, an orally bioavailable inhibitor of human immunodeficiency virus protease

Antimicrobial Agents and Chemotherapy

Volumn 40, Issue 2, 1996, Pages 292-297

  Patick, A K ^a   Mo, H ^b   Markowitz, M ^b   Appelt, K ^a   Wu, B ^a   Musick, L ^a   Kalish, V ^a   Kaldor, S ^c   Reich, S ^a   Ho, D ^b   Webber, S ^a  

^a AGOURON PHARMACEUTICALS INC   (United States)

^b AARON DIAMOND AIDS RESEARCH CENTER   (United States)

^c ELI LILLY AND COMPANY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

GAG PROTEIN; NELFINAVIR; PROTEINASE INHIBITOR; PYRIDONE DERIVATIVE; SAQUINAVIR; ZIDOVUDINE;

AMINO ACID SUBSTITUTION; ANTIVIRAL ACTIVITY; ARTICLE; CELL PROTECTION; DRUG SENSITIVITY; ENZYME INHIBITION; HUMAN; HUMAN CELL; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS 2; PRIORITY JOURNAL; T LYMPHOCYTE; VIRUS INHIBITION; VIRUS RECOMBINANT;

EID: 13344275873     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/aac.40.2.292     Document Type: Article

References (45)

1. Adachi, A., H. E. Gendelman, S. Koenig, T. Folks, R. Willey, A. Rabson, and M. A. Martin. 1986. Production of acquired immunodeficiency syndrome-associated retrovirus in human and nonhuman cells transfected with an infectious molecular clone. J. Virol. 59:284-291.
2. Alley, M. C., D. A. Scudiero, A. Monks, M. L. Hursey, M. J. Czerwinski, D. L. Fine, B. J. Abbott, T. G. Mayo, R. H. Shoemaker, and M. R. Boyd. 1988. Feasibility of drug screening with panels of human tumor cell lines using microculture tetrazolium assay Cancer Res 48:589-601.
3. Ashorn, P., T. J. McQuade, S. Thaisrivongs, A. G. Tomasselli, W. G. Tarpley, and B. Moss. 1990. An inhibitor of the protease blocks maturation of human and simian immunodeficiency virus and spread of infection. Proc Natl. Acad. Sci. USA 87:7472-7476.
4. Bechtold, C. M., A. K. Patick, M. Alam, J. Greytok, J. A. Tino, P. Chen, E. Gordon, S. Ahmad, J. C. Barrish, R. Zahler, P. F.-Lin, and R. Colonno. 1995. Antiviral properties of aminodiol inhibitors against human immunodeficiency virus and protease. Antimicrob. Agents Chemother 39:374-379.
5. Bowdon, B. (Southern Research Institute). 1995. Personal communication.
6. Chen, C., and H. Okayama. 1987. High-efficiency transformation of mammalian cells by plasmid DNA. Mol. Cell. Biol 7:2745-2752.
7. Condra, J. H., W. A. Schleif, O. M. Blahy, L. J. Gabryelski, D. J. Graham, J. C. Quintero, A. Rhodes, H. L. Robbins, E. Roth, and M. Shivaprakash. 1995. In vivo emergence of HIV-1 variants resistant to multiple protease inhibitors Nature (London) 374:569-571
8. Craig, J. C., I. B. Duncan, D. Hockley, C. Grief, N. A. Roberts, and J. S. Mills. 1991. Antiviral properties of Ro 31-8959, an inhibitor of human immunodeficiency virus (HIV) proteinase. Antiviral Res. 16:295-305.
9. Debouck, C. 1992. The HIV-1 protease as a therapeutic target for AIDS. AIDS Res. Hum. Retroviruses 8:153-164.
10. El-Farrash, M. A., M. J. Kuroda, T. Kitazaki, T. Masuda, K. Kato, M. Hatanaka, and S. Harada. 1994 Generation and characterization of human immunodeficiency virus type 1 (HIV-1) mutant resistant to an HIV-1 protease inhibitor. J. Virol. 68:233-239.
11. Fontenot, G., K. Johnston, J. C. Cohen, W. R. Gallaher, J. Robinson, and R. B. Luftig. 1992 PCR amplification of HIV-1 proteinase sequences directly from lab isolates allows determination of five conserved domains. Virology 190:1-10.
12. 2-symmetric protease inhibitor. J Virol. 68:2016-2020
13. Hostomsky, Z., K. Appelt, and R. C. Ogden. 1989 High-level expression of self-processed HIV-1 protease in Escherichia coli using a synthetic gene. Biochem Biophys Res. Commun 161:1056-1063
14. Jacobsen, H., F. Brun-Vezinet, I. Duncan, M. Hänggi, M. Ott, S. Vella, J. Weber, and J. Mous. 1994. Genotypic characterisation of HIV-1 from patients after prolonged treatment with protease inhibitor saquinavir, p. 16. In Abstracts of the 3rd International Workshop on HIV Drug Resistance. MediTech Media Ltd., London.
15. Jacobsen, H., K. Yasargil, D. L. Winslow, J. C. Craig, A. Krohn, I. B. Duncan, and J. Mous. 1995. Characterization of human immunodeficiency virus type 1 mutants with decreased sensitivity to proteinase inhibitor R0 31-8959. Virology 206:527-534
16. Kaldor, S. W., V. J. Kalish, J. F. Davies, II, B. V. Sherry, J. E. Fritz, B. A. Dressman, J. H. Tatlock, K. Appelt, K. S. Su, K. M. Campanale, J. A. Burgess, P. L. Lubbehusen, M. A. Muesing, S. D. Hatch, N. Y. Chirgadze, D. A. Clawson, A. K. Patick, M. B. Kosa, and D. A. Khalil. AG1343: a potent, orally bioavailable inhibitor of HIV-1 protease. Submitted for publication.
17. Kaplan, A. H., S. F. Michael, R. S. Wehbie, M. F. Knigge, D. A. Paul, L. Everitt, D. J. Kempf, D. W. Norbeck, J. W., Erickson, and R. Swanstrom, R. 1994. Selection of multiple human immunodeficiency virus type 1 variants that encode viral proteases with decreased sensitivity to an inhibitor of the viral protease. Proc. Natl. Acad. Sci. USA 91:5597-5601.
18. Kaplan, A. H., J. A. Zack, M. Knigge, D. A. Paul, D. J. Kempf, D. W. Norbeck, and R. Swanstrom. 1993. Partial inhibition of the human immunodeficiency virus type 1 protease results in aberrant virus assembly and the formation of noninfectious particles. J Virol. 67:4050-4055
19. Kempf, D. J., K. C. Marsh, J. Denissen, E. McDonald, S. Vasavanonda, C. Flentge, B. G. Green, L. Fino, C. Park, X. Kong, N. E. Wideburg, A. Saldivar, L. Ruiz, W. M. Kati, H. L. Sham, T. Robins, K. D. Stewart, J. J. Plattner, J. Leonard, and D. Norbeck. ABT-538 is a potent inhibitor of human immunodeficiency virus protease with high oral bioavailability. Submitted for publication.
20. Lambert, D. M., S. R. Petteway, C. E. McDanal, T. K. Hart, J. J. Leary, G. B. Dreyer, T. D. Meek, P. J. Bugelski, D. P. Bolognesi, B. W. Metcalf, and T. J. Matthews. 1992 Human immunodeficiency virus type 1 protease inhibitors irreversibly block infectivity of purified virions from chronically infected cells. Antimicrob. Agents Chemother 36:982-988.
21. Larder, B. A., G. Darby, and D. D. Richman. 1989. HIV with reduced sensitivity to zidovudine (AZT) isolated during prolonged therapy. Science 243:1731-1734
22. Larder, B. A., and S. D. Kemp. 1989. Multiple mutations in HIV-1 reverse transcriptase confer high-level resistance to zidovudine (AZT). Science 246: 1155-1158.
23. Markowitz, M., L. Jalil, A. Hurley, C. Farthing, Y. Cao, M. Saag, W. Powderly, J. Valdes, L. Leonard, and D. D. Ho. 1995. Evaluation of the antiviral activity of orally administered ABT-538, an inhibitor of HIV-1 protease, abstr. 185, p. 88. In Abstracts of 2nd National Conference on Human Retroviruses and Related Infections. American Society for Microbiology, Washington, D.C.
24. Markowitz, M., H. Mo, D. J. Kempf, D. W. Norbeck, T. Narayana Bhat, J. W. Erickson, and D. D. Ho. 1995. Selection and analysis of human immunodeficiency virus type 1 variants with increased resistance to ABT-538, a novel protease inhibitor. J. Virol. 69:701-706.
25. McQuade, T. J., A. G. Tomasselli, L. Liu, V. Karacostas, B. Moss, T. K. Sawyer, R. L. Heinrikson, and W. G. Tarpley. 1990. A synthetic HIV-1 protease inhibitor with antiviral activity arrests HIV-like particle maturation. Science 247:454-456
26. Mo, H., M. Markowitz, and D. D. Ho. 1995. Patterns of specific mutations in HIV-1 protease that confer resistance to a panel of protease inhibitors, abstr. 188, p 89. In Abstracts of the 2nd National Conference on Human Retroviruses and Related Infections American Society for Microbiology. Washington, D.C.
27. Morrison, J. F. 1969. Kinetics of the reversible inhibition of enzyme-catalysed reactions by tight binding inhibitors. Biochim. Biophys. Acta 185:269-286.
28. Nunberg, J. H., W. A. Scheif, E. J. Boots, J. A. O'Brien, J. C. Quintero, J. M. Hoffmann, E. A. Emini, and M. E. Goldman. 1991. Viral resistance to human immunodeficiency virus type 1-specific pyridinone reverse transcriptase inhibitors. J. Virol. 65:4887-4892
29. Otto, M. J., S. Garber, D. L. Winslow, C. D. Reid, P. Aldrich, P. K. Jadhav, C. E. Patterson, C. N. Hodge, and Y.-S. E. Cheng. 1993. In vitro isolation and identification of human immunodeficiency virus (HIV) variants with reduced sensitivity to C-2 symmetrical inhibitor of HIV type 1 protease. Proc. Natl. Acad Sci. USA 90:7543-7547.
30. Otto, M. J., C. D. Reid, S. Garber, P. Y.-S. Lam, H. Scarnati, L. T. Bacheler, M. M. Rayner, and D. L. Winslow. 1993. In vitro anti-human immunodeficiency virus (HIV) activity of XM323, a novel HIV protease inhibitor. Antimicrob. Agents Chemother. 37:2606-2611.
31. Patick, A. K., R. Rose, J. Greytok, C. M. Bechtold, M. A. Hermsmeier, P. T. Chen, J. C. Barrish, R. Zahler, R. J. Colonno, and P.-F. Lin. 1995. Characterization of a human immunodeficiency virus type 1 variant with reduced sensitivity to an aminodiol protease inhibitor. J. Virol. 69:2148-2152
32. Peng, C., B. K. Ho, T. W. Chang, and N. T. Chang. 1989. Role of human immunodeficiency virus type 1-specific protease in core protein maturation and viral infectivity. J. Virol. 63:2550-2556.
33. Potts, K. E., M. L. Smidt, W. C. Stallings Jr., M. Clare, D. Pillay, D. D. Richman, M. Bryant, and G. D. Searle. 1994. In vitro selection and characterization of human immunodeficiency virus type 1 (HIV-1) variants with decreased sensitivity to hydroxyethlurea isostere containing protease inhibitors, p 4. In Abstracts of the 3rd International Workshop on HIV Drug Resistance. MediTech Media Ltd., London.
34. Quart, B. D., S. K. Chapman, J. Peterkin, S. Webber, and S. Oliver. 1995 Phase I safety, tolerance, pharmacokinetics and food effect studies of AG1343 - a novel HIV protease inhibitor, abstr. LB3, p. 167. In Abstracts of the 2nd National Conference on Human Retroviruses and Related Infections. American Society for Microbiology, Washington, D.C.
35. Richards, A. D., L. H. Phylip, W. G. Farmerie, P. E. Scarborough, A. Alvarez, B. M. Dunn, P. H. Hirel, J. Konvalinka, P. Strop, L. Pavlickova, et al. 1990 Sensitive, soluble chromogenic substrates for HIV-1 proteinase. J. Biol. Chem. 265:7733-7736.
36. Richman, D. D. 1993. Resistance of clinical isolates of human immunodeficiency virus to antiretroviral agents. Antimicrob. Agents Chemother. 37: 1207-1213.
37. Schapiro, J. M., M. A. Winters, and T. C. Merigan. 1995. First efficacy and safety results of the high dose Saquinavir monotherapy trials, abstract LB2, p 167. In Abstracts of the 2nd National Conference on Human Retroviruses and Related Infections. American Society for Microbiology, Washington, D.C.
38. Shetty, B. V., M. B. Kosa, D. A. Khalil, and S. Webber. Preclinical studies of pharmacokinetics and distribution in tissue of AG1343, an inhibitor of human immunodeficiency virus type 1 protease. 40:110-114.
39. Stein, D. S., D. G. Fish, J. Chodakewitz, E. Emini, C. Hildebrand, S. L. Preston, G. L. Martineau, and G. L. Drusano. 1995. A 24 week open label phase I evaluation of the HIV protease inhibitor L735524, abstr. LB1, p. 167. In Abstracts of the 2nd National Conference on Human Retroviruses and Related Infections American Society for Microbiology, Washington, D.C
40. Tisdale, M., R. Myers, N. R. Parry, N. Oliver, B. Maschera, and E. Blair. 1994. Comprehensive analysis of HIV-1 variants individually selected for resistance to six HIV protease inhibitors, p. 14. In Abstracts of the 3rd International Workshop on HIV Drug Resistance. MediTech Media Ltd, London.
41. Vacca, J. P., B. D. Dorsey, W. A. Schleif, R. B. Levin, S. L. McDaniel, P. L. Darke, J. Zugay, J. C. Quintero, O. M. Blahy, E. Roth, V. V. Sardana, A. J. Schlabach, P. I. Graham, J. H. Condra, L. Gotlib, M. K. Holloway, J. Lin, I.-W. Chen, K. Vastag, D. Ostovic, P. S. Anderson, E. A. Emini, and J. R. Huff. 1994. L-735.524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor Proc Natl. Acad. Sci. USA 91:4096-4100.
42. Vasavanoda, S., J. Clement, and T. Robins. 1993 Selection and characterization of HIV-1 mutants that arc resistant to HIV-1 protease inhibitors, poster 39 In Program and abstracts of the 33rd Third Interscience Conference on Antimicrobial Agents and Chemotherapy. American Society for Microbiology, Washington, D.C.
43. Webber, S., D. Khalil, M. Kosa, A. Patick, and B. Shetty. 1995. Preclinical toxicokinetic studies with AG1343, an orally bioavailable HIV-1 protease inhibitor, abstr 93, p. 71. In Abstracts of the 2nd National Conference on Human Retroviruses and Related Infections. American Society for Microbiology, Washington, D.C.
44. Winslow, D. W., C. D. Reid, S. Garber, P. Aldrich, H. Scarnati, E. Anton, and M. J. Otto. 1995. DMP450, a new cyclic urea inhibitor of HIV protease with potent in vitro antiviral activity. Antiviral Res. 26:A237. (Abstract 22.)
45. Wlodawer, A., and J. W. Erickson. 1993. Structure-based inhibitors of HIV-1 protease. Annu Rev. Biochem. 62:543-585