Developmental safety profile of the anti-HIV agent stampidine in rabbits

Arzneimittel-Forschung/Drug Research

Volumn 56, Issue 2 A, 2006, Pages 159-166

  D'Cruz, Osmond J ^a,b   Erbeck, Douglas ^a,b   Uckun, Fatih M ^a,b,c  

^a PARKER HUGHES INSTITUTE   (United States)

^b Paradigm Pharmaceuticals   (United States)

^c Ikaros Enterprises   (United States)

Author keywords

Anti HIV agents, chemoprophylaxis; Antiretroviral therapy; CAS 217178 62 6; DDE 113; HI 113; N p (4 bromophenyl) 2',3' didehydro 3' deoxy 5' thymidylyl L alanine methyl ester; Stampidine, chemoprophylaxis, reproductive safety

Indexed keywords

CAS 217178 62 6; DDE 113; HI 113; LAMIVUDINE; RNA DIRECTED DNA POLYMERASE INHIBITOR; STAMPIDINE; STAVUDINE; UNCLASSIFIED DRUG; ZIDOVUDINE;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ANTIVIRAL ACTIVITY; ARTICLE; CONTROLLED STUDY; DRUG MECHANISM; DRUG SAFETY; FEMALE; MALE; NONHUMAN; PRENATAL DRUG EXPOSURE; RABBIT; REPRODUCTION; TERATOGENESIS;

EID: 33645110223     PISSN: 00044172     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0031-1296803     Document Type: Article

References (40)

1. Joint United Nations Programme on HIV/AIDS (UNAIDS) World Health Organization (WHO) report on AIDS epidemic update 2004, December 2004
2. Scarlatti, G., Mother-to-child transmission of HIV-1: advances and controversies of the twentieth centuries. AIDS Rev. 6, 67 (2004)
3. Clark, R. A., Dumestre, I., Women and human immunodeficiency virus: unique management issues. Am. J. Med. Sci. 328, 17 (2004)
4. Carneiro, M., Sanchez, A., Maneiro, R et al., Vertical HIV-1 transmission: prophylaxis and paediatric follow-up. Placenta 22 (Suppl. A), S13 (2001)
5. Rakhmanina, N. Y., Van den Anker, J. N., Soldin, S. J., Safety and pharmacokinetics of antiretroviral therapy during pregnancy. Ther. Drug Monit. 26, 110 (2004)
6. Fernandez, A. D., McNeeley, D. F., Management of the infant born to a mother infected with human immunodeficiency virus type 1 (HIV-1): current concepts. Am. J. Perinatol. 17, 429 (2000)
7. Cooper, E. R., Charurat, M., Mofenson, L. et al., Combination antiretroviral strategies for the treatment of pregnant HIV-1-infected women and prevention of perinatal HIV-1 transmission. J. Acquir. Immune Defic. Syndr. 29, 484 (2002)
8. Public Health Service Task Force Recommendations for use of antiretroviral drugs in pregnant HIV-1-infected women for maternal health and interventions to reduce perinatal HIV-1 transmission in the United States, November 26, 2003, Prevention. Centers for Disease Control and Prevention, Atlanta, GA, USA
9. Bhana, N., Ormrod, D., Perry, C. M. et al., Zidovudine: a review of its use in the management of vertically-acquired pediatric HFV infection. Paediatr. Drugs. 4, 515 (2002)
10. Moodley, D., Moodley, J., Coovadia, H. et al., A multicenter randomized controlled trial of nevirapine versus a combination of zidovudine and lamivudine to reduce intrapartum and early postpartum mother-to-child transmission of human immunodeficiency virus type 1. J. Infect. Dis. 187, 725 (2003)
11. Connor, E. M., Sperling, R. S., Gelber, R. et al., Reduction of maternal-infant transmission of human immunodeficiency virus type 1 with zidovudine treatment. Pediatric AIDS Clinical Trials Group Protocol 076 Study Group. N. Engl. J. Med. 331, 1173 (1994)
12. Chappuy, H., Treluyer, J. M., Jullien, V et al., Maternal-fetal transfer and amniotic fluid accumulation of nucleoside analogue reverse transcriptase inhibitors in human immunodeficiency virus-infected pregnant women. Antimicrob. Agents Chemother. 48, 4332 (2004)
13. Fowler, M. G., Prevention of perinatal HIV infection. What do we know? Where should future research go? Ann. N. Y. Acad. Sci. 918, 45 (2000)
14. Browne, M. J., Mayer, K. H., Chafee, S. B. et al., 2',3'-didehydro-3'- deoxythymidine (d4T) in patients with AIDS or AIDS-related complex: a phase I trial. J. Infect. Dis. 167, 21 (1993)
15. Spruance, S. L., Pavia, A. T., Mellors, J. W. et al., Clinical efficacy of monotherapy with STV compared with zidovudine in HIV-infected, zidovudine-experienced patients. A randomized, double-blind, controlled trial. Bristol-Myers Squibb Stavudine/019 Study Group. Ann. Intern. Med. 126, 355 (1997)
16. Balzarini, J., Herdewijn, P., De Clercq, E., Differential patterns of intracellular metabolism of 2',3'-didehydro-2',3'-dideoxythymidine and 3'-azido-2',3'-dideoxythymidine, two potent anti-human immunodeficiency virus compounds. J. Biol. Chem. 264, 6127 (1989)
17. McGuigan, C., Cahard, D., Sheeka, H. M. et al., Aryl phosphoramidate derivatives of d4T have improved anti-HIV efficacy in tissue culture and may act by the generation of a novel intracellular metabolite. J. Med. Chem. 39, 1748 (1996)
18. Vig, R., Venkatachalam, T. K., Uckun, F. M., D4T-5'-[p-bromophenyl methoxyalaninyl phosphate] as a potent and non-toxic anti-human immunodeficiency virus agent. Antivir. Chem. Chemother. 9, 445 (1998)
19. Uckun, F. M., Samuel, P., Qazi, S. et al., Effects of aryl substituents on the anti-HIV activity of the arylphosphoramidate derivatives of STV Antivir. Chem. Chemother. 13, 197 (2002)
20. Uckun, F. M., Pendergrass, S., Venkatachalam, T. K. et al., Stampidine is a potent inhibitor of Zidovudine- and nucleoside analog reverse transcriptase inhibitor-resistant primary clinical human immunodeficiency virus type 1 isolates with thymidine analog mutations. Antimicrob. Agents Chemother. 46, 3613 (2002)
21. Uckun, F. M., Pendergrass, S., Qazi, S. et al., In vitro activity of STAMP against primary clinical human immunodeficiency virus isolates. Arzneim.-Forsch./Drug Res. 54, 69 (2004)
22. Uckun, F. M., Qazi, S., Pendergrass, S. et al., In vivo toxicity, pharmacokinetics, and anti-human immunodeficiency virus activity of STV-5'-(p-bromophenyl methoxyalaninyl phosphate) (stampidine) in mice. Antimicrob. Agents Chemother. 46, 3428 (2002)
23. Chen, C. L., Yu, G., Venkatachalam, T. K. et al., Metabolism of STV-5'-[p-bromophenyl methoxyalaninyl phosphate], stampidine, in mice, dogs, and cats. Drug Metab. Dispos. 30, 1523 (2002)
24. Uckun, F. M., Chen, C. L., Lisowski, E. et al., Toxicity and pharmacokinetics of stampidine in mice and rats. Arzneim,-Forsch./Drug Res. 53, 357 (2003)
25. Uckun, F. M., Chen, C. L., Samuel, P. et al., In vivo antiretroviral activity of stampidine in chronically feline immunodeficiency virus-infected cats. Antimicrob. Agents Chemother. 47, 1233 (2003)
26. Whitaker, J., Dix, K. M., Double staining technique for rat foetus skeletons in teratological studies. Lab. Anim. 13, 309 (1979)
27. Palmer, A. K., Spontaneous malformations of the New Zealand White rabbit: The background to safety evaluation test. Lab. Anim. 2, 195 (1968)
28. Stadler, J., Kessedjian, M. J., Perraud, J., Use of the New Zealand white rabbit in teratology: incidence of spontaneous and drug-induced malformations. Food Chem. Toxicol. 21, 631 (1983)
29. D'Cruz, O. J., Erbeck, D., Uckun, F. M., Developmental toxicology studies of WHI-07, a novel nucleoside analogue-based dual-function microbicide, administered intravaginally to rabbits. Toxicol. Pathol. 31, 698 (2003)
30. Foote, R. H., Carney, E. W., The rabbit as a model for reproductive and developmental toxicity studies. Reprod. Toxicol. 14, 477 (2000)
31. D'Cruz, O. J., Uckun, F. M., Stampidine is a potential nonspermicidal broad-spectrum anti-human immunodeficiency virus microbicide. Fertil. Steril. 81 (Suppl. 1), 831 (2004)
32. D'Cruz, O. J., Samuel, P., Waurzyniak, B. et al., In vivo evaluation of a gel formulation of Stampidine, a novel non-spermicidal broad-spectrum anti-HIV microbicide. Am. J. Drug Delivery 1, 275 (2003)
33. D'Cruz, O. J., Samuel, P., Waurzyniak, B. et al., Development and evaluation of a thermoreversible ovule formulation of stampidine, a novel nonspermicidal broad-spectrum antihuman immunodeficiency virus microbicide. Biol. Reprod. 69, 1843 (2003)
34. Rana, K. Z., Dudley, M. N., Clinical pharmacokinetics of stavudine. Clin. Pharmacokinet. 33, 276 (1997)
35. Rongkavilit, C., Thaithumyanon, P., Chuenyam, T. et al., Pharmacokinetics of stavudine and didanosine coadministered with nelflnavir in human immunodeficiency virus-exposed neonates. Antimicrob. Agents Chemother. 45, 3585 (2001)
36. Wade, N. A., Unadkat, J. D., Huang, S. et al., Pharmacokinetics and safety of stavudine in HIV-infected pregnant women and their infants: Pediatric AIDS Clinical Trials Group protocol 332. J. Infect. Dis. 190, 2167 (2004)
37. Loubeyre-Unique, C., Gautier, A., Vauzelle-Gardier, C. et al., Antiretroviral agents and pregnancy: mitochondrial dysfunction and nucleoside analogs. Therapie 56, 261 (2001)
38. Alimenti, A., Burdge, D. R., Ogilvie, G. S. et al., Lactic acidemia in human immunodeficiency virus-uninfected infants exposed to perinatal antiretroviral therapy. Pediatr. Infect. Dis. J. 22, 782 (2003)
39. Shiramizu, B., Shikuma, K. M., Kamemoto, L. et al., Placenta and cord blood mitochondrial DNA toxicity in HIV-infected women receiving nucleoside reverse transcriptase inhibitors during pregnancy. J. Acquir. Immune Defic. Syndr. 32, 370 (2003)
40. 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)