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Human Reproduction Update, Vol.5, No.5 pp.506-514, 1999
© European Society of Human Reproduction and Embryology 1999; all rights reserved

Prophylactic contraceptives for HIV/AIDS

FM Uckun0,1,2 and OJ D'Cruz3

0 Drug Discovery Program, 1 Department of Virology and 3 Department of Reproductive Biology, Hughes Institute, 2665 Long Lake Road, Suite 3000, St Paul, MN 55113, USA 2 Corresponding author Tel: 651 697 9228 Fax: 651 697 1042 E-mail: fatih_uckun@mercury.ih.org

Abstract

The current pandemic of sexually transmitted human immunodeficiency virus (HIV) infection - the causative agent of acquired immunodeficiency syndrome (AIDS), has created an urgent need for a new type of contraceptive : one that is both a spermicide and a microbicide. Because most women at risk for HIV infection are of reproductive age (15-44 years), effective use of dual-function contraceptives is important to prevent HIV transmission and unintended pregnancies. In the absence of an effective prophylactic anti-HIV therapy or vaccine, new emphasis has been placed on the development of intravaginal microbicidal agents capable of reducing the transmission of HIV. Topical microbicidal spermicides would ideally provide a female-controlled method of self-protection against HIV as well as preventing pregnancy. However, several microbicides that are undergoing preclinical and human clinical trials contain detergent-type ingredients. The detergent-type spermicide, nonoxynol-9, the only recommended microbicide for protection against sexual transmission of HIV has been shown to cause lesions in vaginal and cervical epithelia leaving women more vulnerable to HIV infection. Therefore, a major challenge in microbicide research has been to design mechanism-based microbicides that are highly effective against pregnancy and HIV transmission while lacking detergent-type effects on epithelial cells and normal vaginal flora. We present an overview of current microbicide research and report on the identification and preclinical development of novel non-detergent spermicidal nucleoside and non-nucleoside inhibitors aimed at decreasing pregnancy and preventing sexual transmission of HIV.

Key words: AIDS/AZT/HIV/spermicidal contraceptives/viricidal microbicides/ZDV


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