Antiviral efficacy in vivo of the anti-human immunodeficiency virus bicyclam SDZ SID 791 (JM 3100), an inhibitor of infectious cell entry

Antimicrobial Agents and Chemotherapy

Volumn 40, Issue 3, 1996, Pages 750-754

  Datema, Roelf ^a   Rabin, Linda ^a,b   Hincenbergs, Mara ^a,b   Moreno, Mary Beth ^a,b   Warren, Suzette ^a,b   Linquist, Valerie ^a,b   Rosenwirth, Brigitte ^a   Seifert, Jan ^a   McCune, Joseph M ^a,b  

^a NOVARTIS PHARMA AG   (Switzerland)

^b UNIVERSITY OF CALIFORNIA   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1,1' [1,4 PHENYLENEBIS(METHYLENE)]BIS(1,4,8,11 TETRAAZACYCLOTETRADECANE); ANTIVIRUS AGENT; CYCLAM DERIVATIVE; DIDANOSINE; UNCLASSIFIED DRUG; ZIDOVUDINE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG EFFICACY; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; MOUSE; NONHUMAN; PRIORITY JOURNAL; SUBCUTANEOUS DRUG ADMINISTRATION; VIREMIA; VIRUS INHIBITION; VIRUS REPLICATION;

EID: 0029976181     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/aac.40.3.750     Document Type: Article

References (20)

1. Aldrovandi, G., G. Feuer, L. Gao, B. Jamieson, M. Kristeva, I. S. Chen, and J. A. Zack. 1993 The SCID-hu mouse as a model ofor HIV-1 infection. Nature (London) 363:732-736.
2. Bean, B. 1992. Antiviral therapy current concepts and practices Clin Microbiol. Res. 5:146-182.
3. Bonyhadi, M. L., L. Rabin, S. Salimi, D. A. Brown, J. Kosek, J. M. McCune, and H. KaDeshima. 1993. HIV induces thymus depletion in vivo. Nature (London) 363:728-732.
4. Bridger, G. J., R. T. Skerlj, D. Thornton, S. Padmanabhan, S. A. Martellucci, G. W. Henson, M. J. Abrams, N. Yamamoto, K. De Vreese, R. Paawels, and E. De Clercq. 1995. Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-tetraazamacrocycles that inhibit HIV replication. Effects of macrocyclic ring size and substituents on the aromatic linker. J. Med. Chem. 38:366-377.
5. Cheeseman, S. H., S. E. Hattox, M. M. McLaughlin, R. A. Koup, C. Andrews, C. A. Bova, J. W. Pav, T. Roy, J. L. Sullivan, and J. J. Keirns. 1993. Pharmacokinetics of nevirapine: initial single-rising-dose study in humans. Antimicrob. Agents Chemother. 37:178-182.
6. De Clercq, E., N. Yamamato, R. Pauwels, J. Balzarini, M. Witvrouw, K. De Vreese, Z. Debyser, B. Rosenwirth, P. Peichl, R. Datema, D. Thornton, R. Skerlj, F. Gaul, S. Padmanabhan, G. Bridger, G. Henson, and M. Abrams. 1994. Highly potent and selective inhibition of human immunodeficiency virus by the bicyclam derivative JM 3100. Antimicrob. Agents Chemother 38:668-674.
7. De Clercq, E., N. Yamamoto, R. Pauwels, M. Baba, D. Schols, H. Nakashima, J. Balzarini, Z. Debyser, B. A. Murrer, D. Schwartz, D. Thornton, G. Bridger, S. Fricker, G. Henson, M. Abrams, and D. Picker. 1992. Potent and selective inhibition of human immunodeficiency virus (HIV)-1 and HIV-2 replication by a class of bicyclams interacting with a viral uncoating event. Proc. Natl. Acad Sci. USA 89:5286-5290.
8. De Vreese, K., V. Kofler-Mongold, C. Leutgeb, V. Weber, K. Vermeire, S. Schacht, J. Anne, E. De Clercq, R. Datema, and G. Werner. 1996. The molecular target of bicyclams, potent inhibitors of human immunodeficiency virus replication. J. Virol. 70:689-696.
9. De Vreese, K., D. Reymen, P. Griffin, A. Steinkasserer, G. Werner, G. J. Bridger, J. Esté, W. James, G. W. Henson, J. Desmyter, J. Anne, and E. De Clercq. The bicyclam, a new class of potent human immunodeficiency virus inhibitors, block viral entry after binding. Antiviral Res., in press.
10. Hauck, C., A. Schweitzer, V. Pflimlin, M. Piaget, and A. Wach. Unpublished data
11. Havlir, D., and The ACTG 164 and 168 Study Teams. 1993. Antiviral activity of nevirapine at 400 mg in p24 antigen positive adults, abstr. WS-B26-1, p 69. IXth In Abstract, of the International Conference on AIDS.
12. Havlir, D., S. H. Cheeseman, M. McLaughlin, R. Murphy, A. Erice, S. A. Spector, T. C. Greenough, J. L. Sullivan, D. Hall, M. Myers, M. Lamson, and D. D. Richman. 1995. High-dose nevirapine: safety, pharmacokinetics. and antiviral effect in patients with human immunodeficiency virus infection. J Infect. Dis. 171:537-545.
13. Joao, H. C., K. De Vreese, R. Pauwels, E. De Clercq, G. W. Henson, and G. J. Bridger. 1995. Quantitative structural activity relationship study of bis-tetraazacyclic compounds. A novel series of HIV-1 and HIV-2 inhibitors. J. Med. Chem. 38:3865-3873.
14. Kaneshima, H., L. Su, M. Bonyhadi, R. Conner, D. Ho, and J. M. McCune. 1994. Rapid-high, syncytium-inducing isolates of human immunodeficiency virus type 1 induce cytopathicity in the human thymus of the SCID-hu mouse. J. Virol. 68:8188-8192.
15. Krowka, J., S. Sarin, R. Namikawa, J. M. McCune, and H. Kaneshima. 1991. The human T cells of the SCID-hu mouse are phenotypically normal and functionally competent. J. Immunol. 145:3751-3756
16. Namikawa, R., K. N. Weilbaecher, H. Kaneshima, E. J. Yee, and J. M. McCune. 1990. Long-term human hematopoiesis in the SCID-hu mouse. J. Exp. Med. 172:1055-1063.
17. Rabin, L., M. Hincenbergs, M. B. Moreno, S. Warren, V. Linquist, R. Datema, B. Charpiot, J. Seifert, H. Kaneshima, and J. M. MeCune. 1996. Use of a standardized SCID-hu Thy/Liv mouse model for preclinical efficacy testing of anti-human immunodeficiency virus type 1 compounds. Antimicrob. Agents Chemother. 40:755-762.
18. Stanley, S. K., J. M. McCune, H. Kaneshima, J. S. Justement, M. Sullivan, E. Boone, M. Baseler, J. Adelsberger, M. Bonyhadi, J. Orenstein, C. F. Fox, and A. S. Fauci. 1993. Human immunodeficiency virus (HIV)-related damage to the human thymus: HIV infects thymocyte subsets and thymic epithelial cells in human thymus xenografts in the SCID-hu mouse. J. Exp. Med. 178:1151-1163.
19. Vandekerckhove, B. A. E., J. F. Krowka, J. M. McCune, J. E. de Vries, H. Spits, and M. G. Roncarolo. 1991 Clonal analysis of the peripheral T cell compartment of the SCID-hu mouse. J. Immunol. 146:4173-4179.
20. Witvrouw, M., J. Seifert, G. W. Henson, S. A. Martellucci, J. Desmyter, and E. De Clercq. 1996. Pharmacokinetics of the anti-HIV bicyclam SID 791 (JM 3100) in rabbits, as determined by both analytical and broassay methods Antiviral Chem. Chemother 7:27-30