Contraceptive activity of a spermicidal aryl phosphate derivative of bromo-methoxy zidovudine (compound WHI-05) in rabbits.

Abstract

WHI-05 (5-bromo-6-methoxy-5,6-dihydro-3'-azidothymidine-5'-(p-methoxyphenyl) methoxyalaninyl phosphate, CAS 213982-93-5) is a highly promising anti-viral and spermicidal agent with clinical potential as a vaginal contraceptive which can prevent the sexual transmission of AIDS. In this study, the contraceptive activity of WHI-05 in rabbits was evaluated. Exposure of semen to WHI-05 at the time of artificial insemination inhibited pregnancy and embryo implantation by 90%. Intravaginal application of 2% WHI-05 containing gel also inhibited the pregnancy rate by 90%. WHI-05 had no side effects for the offspring of rabbits who became pregnant despite WHI-05.

• Authors: Osmond J D'Cruz, Fatih M Uckun
• Journal: Arzneimittel-Forschung (Arzneimittelforschung) Vol. 53 Issue 7 Pg. 515-21 ( 2003) ISSN: 0004-4172 [Print] Germany
• PMID: 12918218 (Publication Type: Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• 5-Bromo-6-methoxy-5,6-dihydro-3'-azidothymidine-5'-(p-methoxyphenyl)methoxyalaninyl phosphate
• Anti-HIV Agents
• Contraceptive Agents, Male
• Dideoxynucleotides
• Emulsions
• Gels
• Spermatocidal Agents
• Thymidine Monophosphate
• Zidovudine

Topics

• Administration, Intravaginal
• Animals
• Anti-HIV Agents (pharmacology)
• Body Weight (drug effects)
• Contraceptive Agents, Male (chemistry, pharmacology)
• Dideoxynucleotides
• Emulsions
• Female
• Fertility (drug effects)
• Gels
• Insemination, Artificial
• Litter Size
• Male
• Pregnancy
• Rabbits
• Spermatocidal Agents (chemistry, pharmacology)
• Survival
• Thymidine Monophosphate (analogs & derivatives, chemistry, pharmacology)
• Zidovudine (analogs & derivatives, chemistry, pharmacology)