Zintevir(TM). Antiviral for AIDS, HIV integrase inhibitor

Drugs of the Future

Volumn 23, Issue 3, 1998, Pages 274-277

  Silvestre, J ^a   Graul, A ^a   Castaner J ^a  

^a PROUS SCIENCE   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

AG 1717; AROMATIC AMIDE; CIBACRON BLUE F3GA; CURCUMIN; INTEGRASE INHIBITOR; NSC 158393; OLIGONUCLEOTIDE; SURAMIN; UNCLASSIFIED DRUG; ZINTEVIR;

ANIMAL EXPERIMENT; ARTICLE; CLINICAL TRIAL; CONTROLLED STUDY; DOSE RESPONSE; DRUG DISTRIBUTION; DRUG EFFECT; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; DRUG SAFETY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; INTRAVENOUS DRUG ADMINISTRATION; NONHUMAN; PHASE 1 CLINICAL TRIAL; PHASE 2 CLINICAL TRIAL; RAT;

EID: 0031899674     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.1998.023.03.449929     Document Type: Article

References (41)

1. Rando, R.F., Ojwang, J., Elbaggari, A., Reyes, G.R., Tinder, R., McGrath, M.S., Hogan, M.E. Suppression of human immunodeficiency virus type 1 activity in vitro by oligonucleotides which form intramolecular tetrads. J Biol Chem 1995, 270: 1754-60.
2. Ojwang, J., Elbaggari, A., Marshall, H.B., Jayaraman, K., McGrath, M.S., Rando, R.F. Inhibition of human immunodeficiency virus type 1 activity in vitro by oligonucleotides composed entirely of guanosine and thymidine. J Acquir Immune Defic Syndr 1994, 7: 560-70.
3. Graul, A., Rabasseda, X., Castañer, J. Efavirenz. Drugs Fut 1998, 23: 133-41.
4. Wroblewski, T., Graul, A., Castañer, J. PNU-140690. Drugs Fut 1998, 23: 146-51.
5. LaFemina, R.L., Schneider, C.L., Robbins, H.L., Callahan, P.L., LeGrow, R., Roth, E., Schleif, W.A., Emini, E.A. Requirement of active human immunodeficiency virus type 1 integrase enzyme for productive infection of human T-lymphoid cells. J Virol 1992, 66: 7414-9.
6. Sakai, H., Kawamura, M., Sakugari, S., Shibata, R., Ishimoto, A., Ono, N., Ueda, S., Adachi, A. Integration is essential for efficient gene expression of human immunodeficiency virus type 1. J Virol 1993, 67: 1169-74.
7. Katz, R.A., Skalka, A.M. The retroviral enzymes. Annu Rev Biochem 1994, 63: 133-73.
8. Letsinger, R.L., Zhang, G., Sun, D.K., Ikeuchi, T., Sarin, P.S. Cholesteryl-conjugated oligonucleotides: Synthesis, properties, and activity as inhibitors of replication of human immunodeficiency virus in cell culture. Proc Natl Acad Sci USA 1989, 86: 6553-6.
9. Lisziewicz, J., Sun, D., Metelev, V., Zamecnik, P., Gallo, R.C., Agrawal, S. Long-term treatment of human immunodeficiency virus-infected cells with antisense oligonucleotide phosphorothioates. Proc Natl Acad Sci USA 1993, 90: 3860-4.
10. Milligan, J.F., Mattenucci, M.D., Martin, J.C. Current concepts in antisense drug design. J Med Chem 1993, 36: 1923-37.
11. Gao, W., Stein, C.A., Cohen, J.S., Dutschman, G.E., Cheng, Y.C. Effect of phosphorothioate homo-oligodeoxynucleotides in herpes simplex virus type 2-induced DNA polymerase. J Biol Chem 1989, 264: 11521-6.
12. Marshall, W.S., Beaton, G., Stein, C.Y., Matsukura, M., Caruthers, M.H. Inhibition of human immunodeficiency virus activity by phosphorothioate oligodeoxycytidine. Proc Natl Acad Sci USA 1992, 89: 6265-9.
13. Ojwang, J.O., Buckheit, R.W., Pommier, Y. et al. T30177, an oligonucleotide stabilized by an intramolecular guanosine octet, is a potent inhibitor of laboratory strains and clinical isolates of human immunodeficiency virus type 1. Antimicrob Agents Chemother 1995, 39: 2426-35.
14. Wyatt, J.R., Vickers, T.A., Roberson, J.L., Buckheit, R.W., Klimkait, T., De Baets E., Davis, P.W., Rayner, B., Imbach, J.L., Ecker, D.J. Combinatorially selected guanosine-quartet structure is a potent inhibitor of human immunodeficiency virus envelope-mediated cell fusion. Proc Natl Acad Sci USA 1994, 91: 1356-60.
15. Rando, R.F., Fennewald, S., Zendegui, J.G., Ojwang, J.O., Hogan, M.E., Pommier, Y., Mazumder, A. (Aronex Pharmaceuticals, Inc.). Anti-viral guanosine-rich oligonucleotides. WO 9703997.
16. Mazumder, A., Neamati, N., Ojwang, J.O., Sunder, S., Rando, R.F., Pommier, Y. Inhibition of the human immunodeficiency virus type 1 integrase by guanosine quartet structures. Biochemistry 1996, 35: 13762-71.
17. Cherepanov, P., Est, J.A., Rando, R.F., Ojwang, J.O., Reekmans, G., Steinfeld, R., David, G., De Clercq, E., Debyser, Z. Mode of interaction of G-quartets with the integrase of human immunodeficiency virus type 1. Mol Pharmacol 1997, 52: 771-80.
18. Est, J.A., Schols, D., Witvrouw, M., Cherepanov, P., Pannecouque, C., Rando, R.F., Debyser, Z., Desmyter, J., De Clercq, E. Human immunodeficiency virus gp120 as the primary target of action of AR177 (Zintevir). Antivir Res 1997, 34(2): Abst 51.
19. Est, J.A., Proost, P., Struyf, S., Wuyts, A., Van Damme, J., De Clercq, E., Schols, D. Interaction of the HIV fusion inhibitor AR177 (Zintevir) with the HIV type 1 second receptor. Antivir Res 1997, 34(2): Abst 1.
20. 33P-labeled anti-human immunodeficiency virus oligonucleotide (AR177) after single- and multiple-dose intravenous administration to rats. J Pharmacol Exp Ther 1997, 280: 1480-8.
21. Wallace, T.L., Bazemore, S.A., Kornbrust, D.J., Cossum, P.A. I. Single-dose hemodynamic toxicity and pharmacokinetics of a partial phosphorothioate anti-HIV oligonucleotide (AR177) after intravenous infusion to cynomolgus monkeys. J Pharmacol Exp Ther 1996, 278: 1306-12.
22. Wallace, T., Kahn, J., Kennedy, B., Bazemore, S., Cossum, P. Single- and multiple-dose pharmacokinetics of AR177, an anti-HIV oligonucleotide, in humans. 37th Intersci Conf Antimicrob Agents Chemother (Sept 28-Oct 1, Toronto) 1997, Abst 1-70.
23. Zintevir development status. Aronex Pharmaceuticals, Inc. Company Communication 1998, February 24.
24. Mazumder, A., Raghavan, K., Weinstein, J., Kohn, K.W., Pommier, Y. Inhibition of human immunodeficiency virus type-1 integrase by curcumin. Biochem Pharmacol 1995, 49: 1165-70.
25. Neamati, N., Mazumder, A., Zhao, H., Sunder, S., Burke, T.R. Jr., Schultz, R.J., Pommier, Y. Diarylsufones, a novel class of human immunodeficiency virus type 1 integrase inhibitors. Antimicrob Agents Chemother 1997, 41: 385-93.
26. Farnet, C.M., Wang, B., Lipford, J.R., Bushman, F.D. Differential inhibition of HIV-1 preintegration complexes and purified integrase protein by small molecules. Proc Natl Acad Sci USA 1996, 93: 9742-7.
27. Fesen, M.R., Pommier, Y., Leteurtre, F., Hiroguchi, S., Yung, J., Kohn, K.W. Inhibition of HIV-1 integrase by flavones, caffeic acid phenetyl ester (CAPE) and related compounds. Biochem Pharmacol 1994, 48: 595-608.
28. Carteau, S., Mouscadet, J.F., Goulaounic, H., Subra, F., Auclair, C. Inhibitory effects of the polyanionic drug suramin on the in vitro HIV DNA integration reaction. Arch Biochem Biophys 1993, 305: 606-10.
29. Robinson, W.E., Reinecke, M.G., Abdel-Malek, S., Jia, Q., Chow, S.A. Inhibitors of HIV-1 replication that inhibit HIV integrase. Proc Natl Acad Sci USA 1996, 93: 6326-31.
30. Mazumder, A., Gazit, A., Levitzki, A., Nicklaus, M., Yung, J., Kohlhagen, G., Pommier, Y. Effects of tyrphostins, protein kinase inhibitors, on human immunodeficiency virus type 1 integrase. Biochemistry 1995, 34: 15111-22.
31. Hong, H., Neamati, N., Wang, S., Nicklaus, M., Pommier, Y., Milne, G.W.A. Discovery of novel HIV-1 integrase inhibitors. 212th ACS Natl Meet (Aug 25-29, Orlando) 1996, Abst MEDI 022.
32. Mazumder, A., Wang, S., Neamati, N., Nicklaus, M., Sunder, S., Chen, J., Milne, G.W.A., Rice, W.G., Burke, T.R. Jr., Pommier, Y. Antiretroviral agents as inhibitors of both human immunodeficiency virus type 1 integrase and protease. J Med Chem 1996, 39: 2472-81.
33. Wang, S., Milne, G.W.A., Yan, X., Posey, I.J., Nicklaus, M.C., Graham, L., Rice, W. Discovery of novel, non-peptide HIV-1 protease inhibitors by pharmacophore searching. J Med Chem 1996, 39: 2047-54.
34. Nicklaus, M.C., Neamati, N., Hong, H., Mazumder, A., Sunder, S., Chen, J., Milne, G.W.A., Pommier, Y. HIV-1 integrase pharmacophore: Discovery of inhibitors through three-dimensional database searching. J Med Chem 1997, 40: 920-9.
35. Gogliotti, R.D., Ellsworth, E.L., Holler, T.P., Hupe, D., Foltin, S.K., Kennedy, R.M., Sanchez, J.P., Domagala, J.M. Quinolones as novel HIV integrase inhibitors. 5th Conf Retroviruses Opportunistic Infect (Feb 1-5, Chicago) 1998, Abst 641.
36. Zhao, H., Neamati, N., Mazumder, A., Sunder, S., Pommier, Y., Burke, T.R. Jr. Arylamide inhibitors of HIV-integrase. J Med Chem 1997, 40: 1186-94.
37. Rando, R. Long term suppression of human immunodeficiency virus type 1 activity by oligonucleotides which form intramolecular tetrads. IBC 2nd Annu Antivir Conf (Nov 17-18, Washington DC) 1994.
38. Wallace, T.L., Ojwang, J.O., Buckheit, R.W., Rando, R.F., Cossum, P.A. Preclinical pharmacology of an anti-HIV oligonucleotide (AR177). 11th Int Conf AIDS (July 7-12, Vancouver) 1996, Abst Tu.B.2283.
39. Ojwang, J., Buckheit, R., Rando, R. Deoxyguanosine and thymidine containing oligonucleotide (GTO) blocks replication of HIV-1 in human peripheral blood cells. 2nd Natl Conf Hum Retroviruses Relat Infect (Jan 29-Feb 2, Washington DC) 1995, Abst 72.
40. Mazumder, A., Pommier Y., Ojwang, J.O., Rando, R.F. AR177, a guanosine tetrad containing oligonucleotide, is a potent inhibitor of HIV-1 integrase. 11th Int Conf AIDS (July 7-12, Vancouver) 1996, Abst Tu.B.2282.
41. Zintevir™. Aronex Pharmaceuticals, Inc. Company Communication 1997, October 1.