New Anti-HIV Spermicide  
Parker Hughes Institute scientists have recently developed microbicide compounds which have shown potential in preventing the sexual transmission of HIV as well as providing fertility control. These compounds may be useful as dual-function vaginal contraceptives for women who are at high risk for HIV by heterosexual vaginal transmission. The anti-HIV spermicide was developed by Dr. Osmond D’Cruz and has already been heralded by the reproductive science community as a major research breakthrough. A clinical paper describing the anti-HIV spermicide was named the winner of the prestigious Prize Paper Award for the Plenary Session of the Conjoint 16th World Congress on Fertility and Sterility and the 54th Annual Meeting of the American Society for Reproductive Medicine The results of Dr. D’Cruz’s research are reported in Biology of Reproduction, the official journal of the Society for the Study of Reproduction (ref. 1).

Dr. D’Cruz recently received a grant worth more than $700,000 from the National Institutes of Health. Issued on December 14, 1998, the grant is in support of the development of dual function vaginal spermicides which protect against HIV transmission and pregnancy. The research conducted under this grant will be essential to further explore the utility of these novel drugs for clinical studies in patients. This is a three-year grant for the period December, 1998 to December, 2001.

Because HIV/AIDS is the fastest growing cause of death in women of reproductive age and more than 75% of all new HIV infections worldwide are caused by heterosexual transmission, the development of a female controlled anti-HIV vaginal agent has become an area of intense investigation in contemporary HIV research.

Currently, the only topical microbicide under consideration for protection against sexually transmitted HIV infection in women contains nonoxynol-9 (N-9). N-9 is a detergent ingredient which has been widely used for more than 30 years in the form of gels, foams, aerosols, creams, sponges, suppositories, films and foaming tablets. Although N-9 exerts both spermicidal and antibacterial/antiviral activities against pathogens responsible for sexually transmitted disease including HIV recent clinical studies have shown it ineffective in protecting from HIV and other sexually transmitted diseases (ref. 2). In addition, it disrupts the cell membrane, damages cervicovaginal epithelium, and causes an acute tissue inflammatory response, thereby enhancing the likelihood of HIV infection. Therefore, there is an urgent need for new, effective, safe, and easy-to-use microbicides with anti-HIV activity lacking detergent-type membrane toxicity.

In a systematic effort to develop such microbicides, Parker Hughes Institute scientists synthesized several novel compounds that exhibit both anti-HIV and spermicidal properties. The lead compound is 400-times more potent than N-9 as an anti-HIV agent and at least 10-fold more potent than N-9 as a spermicidal agent. These dual-function compounds are non-inflammatory by their nature and will have clinical potential as vaginal microbicides for women who are at high risk of acquiring HIV/AIDS by heterosexual transmission. The lead anti-HIV spermicidal compound is expected to enter human clinical trials within 12 months

1. D’Cruz OJ, Venkatachalam TK, Zhu Z, Shih MJ, Uckun FM. Aryl Phosphate derivatives of Bromo-methoxy-azidothymidine are dual-function spermicides with potent anti-human immunodeficiency virus activity. Biology of Reproduction 59:503-515, 1998
2.Roddy RE, Zekeng L, Ryan KA, Tamoufe U, Weir SS, Wong EL. A controlled trial of nonoxynol 9 film to reduce male-to-female transmission of sexually transmitted diseases. The New England Journal of Medicine, 339(8):504-510, 1998