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.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Administration, Intravaginal
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Animals
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Anti-HIV Agents / pharmacology
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Body Weight / drug effects
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Contraceptive Agents, Male / chemistry
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Contraceptive Agents, Male / pharmacology*
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Dideoxynucleotides
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Emulsions
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Female
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Fertility / drug effects
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Gels
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Insemination, Artificial
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Litter Size
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Male
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Pregnancy
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Rabbits
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Spermatocidal Agents / chemistry
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Spermatocidal Agents / pharmacology*
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Survival
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Thymidine Monophosphate / analogs & derivatives*
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Thymidine Monophosphate / chemistry
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Thymidine Monophosphate / pharmacology*
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Zidovudine / analogs & derivatives*
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Zidovudine / chemistry
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Zidovudine / pharmacology*
Substances
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5-Bromo-6-methoxy-5,6-dihydro-3'-azidothymidine-5'-(p-methoxyphenyl)methoxyalaninyl phosphate
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Anti-HIV Agents
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Contraceptive Agents, Male
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Dideoxynucleotides
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Emulsions
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Gels
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Spermatocidal Agents
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Thymidine Monophosphate
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Zidovudine