PR Newswire; Friday August 21, 1998

Sexually active women represent the fastest growing human immunodeficiency virus/acquired immunodeficiency syndrome (HIV/AIDS) risk group. Heterosexual transmission accounts for more than 75% of all HIV infections worldwide and constitutes a growing proportion of new HIV infections in the United States. In the absence of an effective prophylactic anti-HIV vaccine or antiretroviral therapy, female-controlled vaginal contraceptives which curb HIV transmission and protect against sexually transmitted diseases are being sought.

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, 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.

Reference:

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.

SOURCE: Hughes Institute

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