An Update on Vaginal Microbicides

Overview

Journal Curr Infect Dis Rep

Specialty Infectious Diseases

Date 2001 Nov 28

PMID 11722815

Citations 3

Authors

Christine Mauck

Gustavo Doncel

Affiliations

Soon will be listed here.

Abstract

In response to an increasing prevalence of sexually transmitted diseases, especially AIDS, efforts to prevent further infections have been heightened. One of those approaches has been the development of topical microbicidal agents or microbicides. These are compounds designed to protect the body's mucosal surfaces from infection by sexually transmitted disease-causing pathogens. Numerous candidates are currently in preclinical stages; however, only a handful have been tested for safety, and even fewer are ready for clinical efficacy trials. In this update, we describe some of the specific features of microbicide research and development, including preclinical screening algorithms, candidate's ideal properties, examples of compounds presently in the pipeline, and future prospects.

Citing Articles

Synthesis and Biological Evaluation of 5'--Dicarboxylic Fatty Acyl Monoester Derivatives of Anti-HIV Nucleoside Reverse Transcriptase Inhibitors.

Pemmaraju B, Agarwal H, Oh D, Buckheit K, Buckheit Jr R, Tiwari R Tetrahedron Lett. 2014; 55(12):1983-1986.

PMID: 24791029 PMC: 4001930. DOI: 10.1016/j.tetlet.2014.02.001.

Sophorolipids, microbial glycolipids with anti-human immunodeficiency virus and sperm-immobilizing activities.

Shah V, Doncel G, Seyoum T, Eaton K, Zalenskaya I, Hagver R Antimicrob Agents Chemother. 2005; 49(10):4093-100.

PMID: 16189085 PMC: 1251511. DOI: 10.1128/AAC.49.10.4093-4100.2005.

Vaginal microbicides: a novel approach to preventing sexual transmission of HIV.

Doncel G, Mauck C Curr HIV/AIDS Rep. 2005; 1(1):25-32.

PMID: 16091220 DOI: 10.1007/s11904-004-0004-0.

References

Mauck C, Rosenberg Z, Van Damme L . Recommendations for the clinical development of topical microbicides: an update. AIDS. 2001; 15(7):857-68. DOI: 10.1097/00002030-200105040-00006. View

Koomey M . Implications of molecular contacts and signaling initiated by Neisseria gonorrhoeae. Curr Opin Microbiol. 2001; 4(1):53-7. DOI: 10.1016/s1369-5274(00)00164-8. View

Dell A, Morris H, Easton R, Patankar M, Clark G . The glycobiology of gametes and fertilization. Biochim Biophys Acta. 1999; 1473(1):196-205. DOI: 10.1016/s0304-4165(99)00179-8. View

Risso A . Leukocyte antimicrobial peptides: multifunctional effector molecules of innate immunity. J Leukoc Biol. 2000; 68(6):785-92. View

Bourne N, Bernstein D, Ireland J, Sonderfan A, Profy A, Stanberry L . The topical microbicide PRO 2000 protects against genital herpes infection in a mouse model. J Infect Dis. 1999; 180(1):203-5. DOI: 10.1086/314853. View

Bellm L, Lehrer R, Ganz T . Protegrins: new antibiotics of mammalian origin. Expert Opin Investig Drugs. 2000; 9(8):1731-42. DOI: 10.1517/13543784.9.8.1731. View

Kreiss J, Ngugi E, Holmes K, Ndinya-Achola J, Waiyaki P, Roberts P . Efficacy of nonoxynol 9 contraceptive sponge use in preventing heterosexual acquisition of HIV in Nairobi prostitutes. JAMA. 1992; 268(4):477-82. View

Stephens R, Lammel C . Chlamydia outer membrane protein discovery using genomics. Curr Opin Microbiol. 2001; 4(1):16-20. DOI: 10.1016/s1369-5274(00)00158-2. View

Bourinbaiar A, Lee-Huang S . Comparative in vitro study of contraceptive agents with anti-HIV activity: gramicidin, nonoxynol-9, and gossypol. Contraception. 1994; 49(2):131-7. DOI: 10.1016/0010-7824(94)90088-4. View

10.

Mahmoud E, Svensson L, OLSSON S, Mardh P . Antichlamydial activity of vaginal secretion. Am J Obstet Gynecol. 1995; 172(4 Pt 1):1268-72. DOI: 10.1016/0002-9378(95)91491-9. View

11.

Herold B, Siston A, Bremer J, Kirkpatrick R, Wilbanks G, Fugedi P . Sulfated carbohydrate compounds prevent microbial adherence by sexually transmitted disease pathogens. Antimicrob Agents Chemother. 1998; 41(12):2776-80. PMC: 164209. DOI: 10.1128/AAC.41.12.2776. View

12.

Zheng H, Alcorn T, Cohen M . Effects of H2O2-producing lactobacilli on Neisseria gonorrhoeae growth and catalase activity. J Infect Dis. 1994; 170(5):1209-15. DOI: 10.1093/infdis/170.5.1209. View

13.

McClure M, Moore J, Blanc D, Scotting P, Cook G, Keynes R . Investigations into the mechanism by which sulfated polysaccharides inhibit HIV infection in vitro. AIDS Res Hum Retroviruses. 1992; 8(1):19-26. DOI: 10.1089/aid.1992.8.19. View

14.

Barnhart K, Pretorius E, Stolpen A, Malamud D . Distribution of topical medication in the human vagina as imaged by magnetic resonance imaging. Fertil Steril. 2001; 76(1):189-95. DOI: 10.1016/s0015-0282(01)01822-2. View

15.

Stafford M, Cain D, Rosenstein I, Fontaine E, McClure M, Flanagan A . A placebo-controlled, double-blind prospective study in healthy female volunteers of dextrin sulphate gel: a novel potential intravaginal virucide. J Acquir Immune Defic Syndr Hum Retrovirol. 1997; 14(3):213-8. DOI: 10.1097/00042560-199703010-00003. View

16.

Bulut A, Ortayli N, Ringheim K, Cottingham J, Farley T, Peregoudov A . Assessing the acceptability, service delivery requirements, and use-effectiveness of the diaphragm in Colombia, Philippines, and Turkey. Contraception. 2001; 63(5):267-75. DOI: 10.1016/s0010-7824(01)00204-9. View

17.

Barnhart K, Stolpen A, Pretorius E, Malamud D . Distribution of a spermicide containing Nonoxynol-9 in the vaginal canal and the upper female reproductive tract. Hum Reprod. 2001; 16(6):1151-4. DOI: 10.1093/humrep/16.6.1151. View

18.

Campbell S, Crowe S, Mak J . Lipid rafts and HIV-1: from viral entry to assembly of progeny virions. J Clin Virol. 2001; 22(3):217-27. DOI: 10.1016/s1386-6532(01)00193-7. View

19.

Jan S, Shih M, Venkatachalam T, DCruz O, Chen C, Uckun F . Synthesis of dual function (5R,6R)- and (5S,6S)-5-bromo-6-methoxy-5,6-dihydro-AZT-5'-(para-bromophenyl methoxyalaninyl phosphate) as novel spermicidal and anti-HIV agents. Antivir Chem Chemother. 1999; 10(1):39-46. DOI: 10.1177/095632029901000105. View

20.

Herold B, Bourne N, Marcellino D, Kirkpatrick R, Strauss D, Zaneveld L . Poly(sodium 4-styrene sulfonate): an effective candidate topical antimicrobial for the prevention of sexually transmitted diseases. J Infect Dis. 2000; 181(2):770-3. DOI: 10.1086/315228. View