141W94 anti-HIV

Drugs of the Future

Volumn 21, Issue 4, 1996, Pages 347-350

  Painter, George R ^a   Ching, Shelley ^b   Reynolds, David ^b   St Clair, Marty ^b   Sadler, Brian M ^b   Elkins, Mary ^b   Blum, Robert ^b   Dornsife, Ronna ^b   Livingston, David J ^b   Partaledis, Judith A ^b   Pazhanisamy, S ^b   Tung, Roger D ^b   Tisdale, Margaret ^b  

^a Triangle Pharmaceuticals   (United States)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

ABACAVIR; AMPRENAVIR; ANTIVIRUS AGENT; DRUG; EMTRICITABINE; INDINAVIR; PROTEINASE INHIBITOR; RALURIDINE; RITONAVIR; RNA DIRECTED DNA POLYMERASE INHIBITOR; SAQUINAVIR; ZIDOVUDINE;

ANTIVIRAL ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CELL LINE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CYTOTOXICITY; DOSE RESPONSE; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENTIATION; DRUG SENSITIVITY; DRUG STRUCTURE; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS 2; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; INTRAVENOUS DRUG ADMINISTRATION; MOLECULAR WEIGHT; NONHUMAN; ORAL DRUG ADMINISTRATION; PHASE 1 CLINICAL TRIAL; RANDOMIZED CONTROLLED TRIAL;

EID: 0030000990     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.1996.021.04.350764     Document Type: Article

References (17)

1. Kohl, N.E., Emini, E.A., Schleif, L.J., HeimBach, J.C., Dixon, R.A.F., Scolnick, E.M., Sigal, I.S. Active human immunodeficiency virus protease is required for viral infectivity. Proc Natl Acad Sci USA 1988, 85: 4686-90.
2. Schooley, R.T. A new class: Clinical and virological perspectives on protease inhibitors. 5th Eur Conf Clin Aspects Treat HIV Infect, Satel Symp Antiretrovirals HIV Dis: Curr Emerging Ther (Sept 26-29, Copenhagen) 1995.
3. Navia, M.A., Sato, V.L., Tung, R.D. Design of VX-478, a potent inhibitor of HIV protease. Int Antivir News 1995, 9: 143-5.
4. Kim, E.E., Baker, C.T., Dwyer, M.D., Murcko, M.A., Rao, B.G., Tung, R.D., Navia, M.A. Crystal structure of HIV-1 protease in complex with VX-478, a potent and orally bioavailable inhibitor of the enzyme. J Amer Chem Soc 1995, 17: 1181-2.
5. Painter, G.R., St. Clair, M.H., DeMiranda, P., Reynolds, D., Ching, S., Dornsife, R., Livingston, D.J., Pazhanisamy, S.,Tung, R. An overview of the preclinical development of the HIV protease inhibitor VX-478 (141W94). 2nd Natl Conf Hum Retroviruses Relat Infect (Jan 29-Feb 2, Washington DC) 1995, Abst LB5.
6. St. Clair, M.H., Millard, J., Rooney, J., Tisdale, M., Parry, N., Sadler, B.M., Blum, M.R., Painter, G.R. In vitro antiviral activity of 141W94 (VX-478) in combination with other antiretroviral agents. Consensus Symp Combined Antiviral Ther (July 25-27, Lisbon) 1995.
7. St. Clair, M.H., Millard, J., Rooney, J., Tisdale, M., Parry, N., Sadler, B.M., Blum, M.R., Painter, G.R. In vitro antiviral activity of 141W94 (VX-478) in combination with other antiretroviral agents. Antivir Res 1996, 29: 53-6.
8. Larder, B.A., Kemp, S.D., Harrigan, P.R. Potential mechanism for sustained antiretroviral potency of AZT-3TC combination therapy. Science 1995, 269: 696-9.
9. Tisdale, M., Kemp, S.D., Parry, N.R., Larder, B.A. Rapid in vitro selection of human immunodeficiency virus type 1 resistant to 3′-thiacytidine inhibitors due to a mutation in the YMDD region of reverse transcriptase. Proc Natl Acad Sci USA 1993, 90: 5653-6.
10. Partaledis, J.A., Yamagouchi, K., Tisdale, M. et al. In vitro selection and characterization of human immunodeficiency virus type 1 (HIV-1) isolates with reduced sensitivity to potent sulfonamide inhibitors of HIV-1 aspartyl protease. J Virol 1995, 69: 5228-35.
11. Tisdale, M., Myers, R.E., Maschera, B., Parry, N.R., Oliver, N.M., Blair, E.D. Cross-resistance analysis of human immunodeficiency virus type 1 variants individually selected for resistance to five different protease inhibitors. Antimicrob Agents Chemother 1995, 39: 1704-10.
12. Kageyama, S.S., Anderson, B.D., Hoesterey, B.L. Protein binding of human immunodeficiency protease inhibitor KNI-272 and alteration of its in vitro antiretroviral activity in the presence of high concentrations of proteins. Antimicrob Agents Chemother 1994, 38: 1107-11.
13. 1 -acid glycoprotein. J Infect Dis 1995, 171: 546-51.
14. Kempf, D.J., Marsh, K.V., Dennissen, J.F. ABT-538 is a potent inhibitor of human immunodeficiency virus protease and has high oral bioavailability in humans. Proc Natl Acad Sci USA 1995, 92: 2484-8.
15. Markowitz, M., Jalil, L., Hurley, A. Evaluation of the antiviral activity of orally administered ABT-538, an inhibitor of HIV-1 protease. 2nd Natl Conf Hum Retroviruses Relat Infect (Jan 29-Feb2, Washington DC) 1995, Abst 185.
16. Livingston, D.J., Pazhanisamy, S., Porter, D.J.T., Partaledis, J.A., Tung, R.D., Painter, G.R. Weak binding of VX-478 to human plasma proteins and implications for anti-human immunodeficiency virus therapy. J Infect Dis 1995, 172: 1238-45.
17. Sadler, B.H., Elkins, M., Hanson, C., Rooney, J., Millard, J., Slum, M.R., Painter, G.R. The safety and pharmacokinetics of 141 W94:An HIV protease inhibitor. 5th Eur Conf Clin Aspects Treat HIV Infect (Sept 26-29, Copenhagen) 1995, Abst 564.