In vitro Activity of Stampidine against Primary Clinical Human Immunodeficiency Virus Isolates

Arzneimittel-Forschung/Drug Research

Volumn 54, Issue 1, 2004, Pages 69-77

  Uckun, Fatih M ^a   Pendergrass, Sharon ^a   Qazi, Sanjive ^a   Venkatachalam, Taracad K ^a  

^a Parker Hughes Cancer Center   (United States)

Author keywords

Antiviral agents; CAS 217178 62 6; HI 113; Stampidine, effect on HIV isolates, in vitro studies

Indexed keywords

ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; ENZYME INHIBITOR; LAMIVUDINE; NELFINAVIR; NEVIRAPINE; RNA DIRECTED DNA POLYMERASE INHIBITOR; STAMPIDINE; STAVUDINE; UNCLASSIFIED DRUG; ZIDOVUDINE;

ARTICLE; CONTROLLED STUDY; DRUG ACTIVITY; DRUG EFFICACY; DRUG POTENCY; GENOTYPE; HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS 1; IC 50; IN VITRO STUDY; INHIBITION KINETICS; NONHUMAN; PHENOTYPE; VIRUS ISOLATION; VIRUS REPLICATION;

EID: 0742322029     PISSN: 00044172     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0031-1296939     Document Type: Article

References (44)

1. Gottlieb, M. S., AIDS - past and future. N. Engl. J. Med. 344 1788 (2001)
2. Sepkowitz, K. A., AIDS - the first 20 years. N. Engl. J. Med. 344, 1764 (2001)
3. Freedberg, K. A., Losina, E., Weinstein, M. C. et al., The cost effectiveness of combination antiretroviral therapy for HIV disease. N. Engl. J. Med. 344, 824 (2001)
4. Richman, D. D., HIV chemotherapy. Nature 410, 995 (2001)
5. Shafer, R. W., Vuitton, D. A., Highly active antiretroviral therapy (HAART) for the treatment of infection with human immunodeficiency virus type 1. Biomed. Pharmacother. 53, 73 (1999)
6. Starr, S. E., Fletcher, C. V., Spector, S. A. et al., Combination therapy with efavirenz, nelfinavir, and nucleoside reverse-transcriptase inhibitors in children infected with human immunodeficiency virus type 1. Pediatric AIDS Clinical Trials Group 382 Team. N. Engl. J. Med. 341, 1874 (1999)
7. Rey, D., Schmitt, M. P., Partisani, M. et al. Efavirenz as a substitute for protease inhibitors in HIV-1-infected patients with undetectable plasma viral load on HAART: a median follow-up of 64 weeks. J. Acquir. Immune Defic. Syndr. 27, 459 (2001)
8. Miller, V., Ait-Khaled, M., Stone, C. et al., HIV-1 reverse transcriptase (RT) genotype and susceptibility to RT inhibitors during abacavir monotherapy and combination therapy. AIDS 14, 163 (2000)
9. Johnson, V. A., Nucleoside reverse transcriptase inhibitors and resistance of human immunodeficiency virus type 1. J. Infect. Dis. 171 (Suppl. 2), S140 (1995)
10. Lin, P. F., Gonzalez, C. J., Griffith, B. et al., Stavudine resistance: an update on susceptibility following prolonged therapy. Antivir. Ther. 4, 21 (1999)
11. Coakley, E. P., Gillis, J. M., Hammer, S. M., Phenotypic and genotypic resistance patterns of HIV-1 isolates derived from individuals treated with didanosine and stavudine. AIDS 14, F9 (2000)
12. Ross, L., Scarsella, A., Raffanti, S. et al., Thymidine analog and multinucleoside resistance mutations are associated with decreased phenotypic susceptibility to stavudine in hiv type 1 isolated from zidovudine-naive patients experiencing viremia on stavudine-containing regimens. AIDS Res. Hum. Retroviruses 17, 1107 (2001)
13. Suzuki, K., Kaufmann, G. R., Mukaide, M. et al., Novel deletion of HIV type 1 reverse transcriptase residue 69 conferring selective high-level resistance to nevirapine. AIDS Res. Hum. Retroviruses 17, 1293 (2001)
14. Picard, V., Angelini, E., Maillard, A. et al., Comparison of Genotypic and Phenotypic Resistance Patterns of Human Immunodeficiency Virus Type 1 Isolates from Patients Treated with Stavudine and Didanosine or Zidovudine and Lamivudine. J. Infect. Dis. 184, 781 (2001)
15. Miller, M. D., Margot, N. A., Lamy, P. D. et al., Adefovir and tenofovir susceptibilities of HIV-1 after 24 to 48 weeks of adefovir dipivoxil therapy: genotypic and phenotypic analyses of study GS-96-408. J. Acquir. Immune Defic. Syndr. 27, 450 (2001)
16. Shulman, N. S., Machekano, R. A., Shafer, R. W. et al., The AIDS Clinical Trials Group 302 Study Team. Genotypic correlates of a virologic response to stavudine after zidovudine monotherapy. J. Acquir. Immune Defic. Syndr. 27, 377 (2001)
17. Izopet, J., Bicart-See, A., Pasquier, C. et al., Mutations conferring resistance to zidovudine diminish the antiviral effect of stavudine plus didanosine. J. Med. Virol. 59, 507 (1999)
18. Venturi, G., Romano, L., Catucci, M. et al., Genotypic resistance to zidovudine as a predictor of failure of subsequent therapy with human immunodeficiency virus type-1 nucleoside reverse-transcriptase inhibitors. Eur. J. Clin. Microbiol. Infect. Dis. 18, 274 (1999)
19. Kuritzkes, D. R., Sevin, A., Young, B. et al., Effect of zidovudine resistance mutations on virologic response to treatment with zidovudine-lamivudine-ritonavir: genotypic analysis of human immunodeficiency virus type 1 isolates from AIDS clinical trials group protocol 315.ACTG Protocol 315 Team. J. Infect. Dis. 181, 491 (2000)
20. O'Brien, W. A., Resistance against reverse transcriptase inhibitors. Clin. Infect. Dis. 30 (Suppl. 2), S185 (2000)
21. Pillay, D., Taylor, S., Richman, D. D., Incidence and impact of resistance against approved antiretroviral drugs. Rev. Med. Virol. 10, 231 (2000)
22. Briones, C., Soriano, V., Gonzalez-Lahoz, J., Prevalence of drug-resistant HIV-1 genotypes in heavily pre-treated patients on current virological failure. AIDS 14, 1659 (2000)
23. Rousseau, M. N., Vergne, L., Montes, B. et al., Patterns of resistance mutations to antiretroviral drugs in extensively treated HIV-1-infected patients with failure of highly active antiretroviral therapy. J. Acquir. Immune Defic. Syndr. 26, 36 (2001)
24. Gutierrez, F., Molto, J., Escolano, C. et al., Genotypic resistance to antiretroviral drugs in patients with therapeutic failure to highly active antiretroviral therapy. Med. Clin. (Barcelona) 115, 401 (2000)
25. Palmer, S., Shafer, R. W., Merigan, T. C., Highly drug-resistant HIV-1 clinical isolates are cross-resistant to many antiretroviral compounds in current clinical development. AIDS 13, 661 (1999)
26. Duwe, S., Brunn, M., Altmann, D. et al., Frequency of genotypic and phenotypic drug-resistant HIV-1 among therapy-naive patients of the German Seroconverter Study. J. Acquir. Immune Defic. Syndr. 26, 266 (2001)
27. Salomon, H., Wainberg, M. A., Brenner, B. et al., Prevalence of HIV-1 resistant to antiretroviral drugs in 81 individuals newly infected by sexual contact or injecting drug use. Investigators of the Quebec Primary Infection Study. AIDS 14, F17 (2000)
28. Rana, K. Z., Dudley, M. N., Clinical pharmacokinetics of stavudine. Clin. Pharmacokinet. 33, 276 (1997)
29. Uckun, F. M., Vig, R., United States Patent No. 6,030,957: Aryl Phosphate Derivatives of d4T Having Anti-HIV Activity. Issue Date: 2-29-2000
30. Venkatachalam, T. K., Tai, H.-L., Vig, R. et al., Enhancing Effects of a Mono-Bromo Substitution at the Para Position of the Phenyl Moiety on the Metabolism and Anti-HIV Activity of D4T-Phenyl Methoxyalaninyl Phosphate Derivatives. Bioorg. & Med. Chem. Lett. 8, 3121 (1998)
31. Vig, R., Venkatachalam, T. K., Uckun, F. M., D4T-5′[p-Bromo- Phenylmethoxyalaninyl Phosphate] As A Potent And Non-Toxic Anti-HIV Agent. Antiviral Chem. & Chemother. 9, 445 (1998)
32. Chen, C., Venkatachalam, T., Zhu, Z. et al., In vivo pharmacokinetics and metabolism of stampidine, a novel aryl phosphate derivative of d4T with potent anti-HIV activity. Drug Metab. Dispos. 29, 1035 (2001)
33. Uckun, F. M., Chen, C., Lisowski, E. et al., Toxicity and Pharmacokinetics of Stampidine in Mice and Rats. Arzneim.-Forsch./Drug Res. 53, 357 (2003)
34. Uckun, F. M., Qazi, S., Pendergrass, S. et al., In vivo Toxicity, Pharmacokinetics, and anti-HIV Activity of D4T-5′[P-Bromophenyl Methoxyalaninyl Phosphate], Stampidine, in Mice. Antimicrob. Agents Chemother. 46 (II), 3428 (2002)
35. Richman, D. D., Johnson, V. A., Mayers, D. L. et al., In vitro evaluation of experimental agents for anti-HIV activity. In: Current Protocols in Immunology, J. E. Coligan, A. M. Kruisbeek, D. H. Margulies (eds.), Suppl 8, Unit 12.9, pp. 1-21, John Wiley & Sons, Inc., Brooklyn, NY (1993)
36. Uckun, F. M., Chelstrom, L. M., Tuel-Ahlgren, L., Txu (anti-CD7) -pokeweed antiviral protein as a potent inhibitor of human immunodeficiency virus. Antimicrob. Agents Chemother. 42, 383 (1998)
37. Erice, A., Balfour, H. H. Jr., Myers, D. E., Anti-human immunodeficiency virus type I activity of an anti-CD4 immunoconjugate containing pokeweed antiviral protein. Antimicrob. Agents Chemother. 37, 835 (1993)
38. Palmer, S., Alaeus, A., Albert, J., Drug susceptibility of subtypes A,B,C,D, and E human immunodeficiency virus type 1 primary isolates. AIDS Res. Hum. Retroviruses 14, 157 (1998)
39. Mao, C., Sudbeck, E. A., Venkatachalam, T. K. et al., Structure-based drug design of non-nucleoside inhibitors for wild-type and drug-resistant HIV reverse transcriptase. Biochem. Pharmacol. 60, 1251 (2000)
40. Hu, D. J., Dondero, T. J., Rayfield, M. A. et al., The emerging genetic diversity of HIV: The importance of global surveillance for diagnostics, research and prevention. JAMA 275, 210 (1996)
41. Kuiken, C. L., Foley, B., Hahn, B., Human retroviruses and AIDS: A compilation and analysis of nucleic acid and amino acid sequences. Los Alamos National Laboratory, Los Alamos, New Mexico (1999)
42. Palmer, S., Alaeus, A., Albert, J. et al., Drug susceptibility of subtypes A,B,C,D, and E human immunodeficiency virus type 1 isolates. AIDS Res. Hum. Retroviruses 14, 157 (1998)
43. Shafer, R. W., Eisen, J. A., Merigan, T. C. et al., Sequence and drug susceptibility of subtype C reverse transcriptase from human immunodeficiency virus type 1 seroconverters in Zimbabwe. J. Virol. 71, 5441 (1997)
44. Palmer, S., Margot, N., Gilbert, H. et al., Tenofovir, adefovir, and zidovudine susceptibilities of primary human immunodeficiency virus type 1 isolates with non-B subtypes or nucleoside resistance. AIDS Res. Hum. Retroviruses 17, 1167 (2001)