BMS-232632. Anti-HIV, HIV-1 protease inhibitor

Drugs of the Future

Volumn 24, Issue 4, 1999, Pages 375-380

  Rabasseda, X ^a   Silvestre, J ^a   Castaner J ^a  

^a PROUS SCIENCE   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

AMPRENAVIR; ATAZANAVIR; DELAVIRDINE; DIDANOSINE; INDINAVIR; KYNOSTATIN 272; LAMIVUDINE; LASINAVIR; LOPINAVIR; MOZENAVIR; NELFINAVIR; NEVIRAPINE; PROTEINASE INHIBITOR; RITONAVIR; SAQUINAVIR; STAVUDINE; TIPRANAVIR; UNCLASSIFIED DRUG; ZALCITABINE; ZIDOVUDINE;

CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DOUBLE BLIND PROCEDURE; DRUG BLOOD LEVEL; DRUG POTENTIATION; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS 1; PHASE 1 CLINICAL TRIAL; REVIEW;

EID: 0033036156     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.1999.024.04.489140     Document Type: Review

References (31)

1. Fässler, A., Bold, G., Capraro, H.-G., Lang, M., Khanna, S.C. (Novartis AG). Antivirally active heterocyclic azahexane derivs. EP 900210, US 5849911, WO 9740029.
2. Bold, G., Fässler, A., Capraro, H.-G. et al. New aza-dipeptide analogues as potent and orally absorbed HIV-1 protease inhibitors: Candidates for clinical development. J Med Chem 1998; 41 (18): 3387-401.
3. Fässler, A., Bold, G., Capraro, H.-G., Steiner, H. (Novartis AG). Process for the preparation of hydrazine derivs. useful as intermediates for the preparation of peptide analogues. WO 9746514.
4. Kohl, N.E., Emini, E.A., Schleif, W.A., Davis, L.J., Heimbach, J.C., Dixon, R.A., 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.
5. Graul, A., Silvestre, J., Castañer, J. Lodenosine. Drugs Fut 1998, 23: 1176-89.
6. Wroblewski, T., Graul, A., Castañer, J. PNU-140690. 1998, 23: 146-51.
7. Steele, F.R. New protease inhibitors, with combination drug therapy, and early intervention to reduce "viral load" show real promise in treating AIDS. Nat Med 1996, 2: 257-8.
8. Deeks, S.G., Smith, M., Holodniy, M., Kahn, J.O. HIV-1 protease inhibitors. A review for clinicians. JAMA - J Am Med Assoc 1997, 277: 145-53.
9. Phillips, K.D. Protease inhibitors: A new weapon and a new strategy against HIV. J Assoc Nurses AIDS Care 1996, 7: 57-71.
10. Boudes, P., Geiger, J.M. HIV protease inhibitors: General review. Therapie 1996, 51: 319-25.
11. FDA approves amprenavir, first new protease inhibitor in more than two years. DailyDrugNews.com (Daily Essentials) Apr 19, 1999.
12. Gong, Y., Robinson, B., Rose, R. et al. Resistance profile and drug combination studies of an HIV-1 protease inhibitor BMS-232632. 6th Conf Retroviruses Opportunistic Infect (Jan 31-Feb 4, Chicago) 1999, Abst 603.
13. Gong, Y.-F., Robinson, B., Rose, R., Deminie, C., Spicer, T., Markowitz, M., Colonno, M., Lin, P.-F. Antiviral activity and resistance profile of an HIV-1 protease inhibitor BMS-232632. 38th Intersci Conf Antimicrob Agents Chemother (Sept 24-27, San Diego) 1998, Abst I-79.
14. Robinson, B., Riccardi, K., Deminie, C., Stock, D., Djang, F., Cross, J., Colonno, R., Lin, P.-F. Two-drug combination studies on the protease inhibitor BMS-232632 on HIV-1 replication. 38th Intersci Conf Antimicrob Agents Chemother (Sept 24-27, San Diego) 1998, Abst I-20.
15. O'Mara, E.M., Smith, J., Olsen, S.J., Tanner, T., Schuster, A.E., Kaul, S. BMS-232632: Single-oral dose-safety and pharmacokinetic study in healthy volunteers. 38th Intersci Conf Antimicrob Agents Chemother (Sept 24-27, San Diego) 1998, Abst I-242.
16. O'Mara, E.M., Smith, J., Olsen, S.J., Tanner, T., Schuster, A.E., Kaul, S. BMS-232632: Single and multiple oral dose safety and pharmacokinetic study in healthy volunteers. 6th Conf Retroviruses Opportunistic Infect (Jan 31-Feb 4, Chicago) 1999, Abst 604.
17. Sham, H.L., Kempf, D.J., Molla, A. et al. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother 1998, 42: 3218-24.
18. Wilkerson, W.W., Dax, S., Cheatham, W.W. Nonsymmetrically substituted cyclic urea HIV protease inhibitors. J Med Chem 1997, 40: 4079-88.
19. Baba, M., Okamoto, M., Makino, M., Kimura, Y., Ikeuchi, T., Sakaguchi, T., Okamoto, T. Potent and selective inhibition of human immunodeficiency virus type 1 transcription by piperazinyloxoquinoline derivatives. Antimicrob Agents Chemother 1997, 41: 1250-5.
20. Kageyama, S., Mimoto, T., Murakawa, Y. et al. In vitro antihuman immunodeficiency virus (HIV) activities of transition state mimetic HIV protease inhibitors containing allophenylnorstatine. Antimicrob Agents Chemother 1993, 37: 810-7.
21. Chokekijchai, S., Shirasaka, T., Weinstein, J.N., Mitsuya, H. In vitro anti-HIV-1 activity of HIV protease inhibitor KNI-272 in resting and activated cells: Implications for its combined use with AZT or ddl. Antivir Res 1995, 28: 25-38.
22. Cozens, R.M., Bold, G., Capraro, H.-G., Fässler, A., Mestan, J., Lang, M., Poncioni, B., Stover, D., Rösel, J.L. Synthesis and pharmacological evaluation of CGP 57813 and CGP 61755, HIV-1 protease inhibitors from the Phe-c-Phe peptidomimetic class. Antivir Chem Chemother 1996, 7: 294-9.
23. Klimkait, T. et al. CGP 61755, a potential combination partner for saquinavir: A synergistic HIV-1 protease inhibitor with high antiviral potency. Antivir Res 1996, 30(1): Abst 51.
24. Kaldor, S.W., Kalish, V.J., Davies, J.F. II et al. Viracept (nelfinavir mesylate, AG1343): A potent, orally bioavailable inhibitor of HIV-1 protease. J Med Chem 1997, 40: 3979-85.
25. Patick, A.K., Mo, H., Markowitz, M., Appelt, K., Wu, B., Musick, L., Kalish, V., Kaldor, S., Reich, S., Ho, D., Webber, S. Antiviral and resistance studies of AG1343, an orally bioavailable inhibitor of human immunodeficiency virus protease. Antimicrob Agents Chemother 1996, 40: 292-7.
26. Fujiwara, T., Sato, A., El-Farrash, M. et al. S-1153 inhibits replication of known drug-resistant strains of human immunodeficiency virus type 1. Antimicrob Agents Chemother 1998, 42:1340-5.
27. Thaisrivongs, S., Skulnick, H.I., Turner, S.R. et al. Structure-based design of HIV protease inhibitors: Sulfonamide-containing 5,6-dihydro-4-hydroxy-2-pyrones as non-peptidic inhibitors. J Med Chem 1996, 39: 4349-53.
28. Chong, K.-T., Pagano, P.J. In vitro combination of PNU-140690, a human immunodeficiency virus type 1 protease inhibitor, with ritonavir against ritonavir-sensitive and -resistant clinical isolates. Antimicrob Agents Chemother 1997, 41: 2367-73.
29. Kempf, D.J., Sham, H.L., Marsh, K.C. et al. Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy. J Med Chem 1998, 41: 602-17.
30. Chen, X. et al. Evaluation of furofuran as a P2 ligand for symmetry-based HIV protease inhibitors. Bioorg Med Chem Lett 1996, 6: 2847.
31. Taylor, D.L., Ahmed, P.S., Brennan, T.M., Bridges, C.G., Tyms, A.S., Van Dorsselaer, V., Tarnus, C., Hornsperger, J.-M., Schirlin, D. Anti-human immunodeficiency virus activity, bioavailability and drug resistance profile of the novel protease inhibitor MDL 74,695. Antivir Chem Chemother 1997, 8: 205-14.