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

Drug Discovery Program, Department of Reproductive Biology, Parker Hughes Institute, Paradigm Pharmaceuticals, LLC, St. Paul, MN, USA. odcruz@ih.org

Arzneimittel-Forschung 2003

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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.

Citation

Osmond J D'Cruz, Fatih M Uckun. Contraceptive activity of a spermicidal aryl phosphate derivative of bromo-methoxy zidovudine (compound WHI-05) in rabbits. Arzneimittel-Forschung. 2003;53(7):515-21