Dual action microbicides: Reappraisal of their roles in contraceptive research

Reproductive BioMedicine Online

Volumn 20, Issue 1, 2010, Pages 103-113

  Chandran, Poornima ^a   Kabir, Syed N ^a  

^a INDIAN INSTITUTE OF CHEMICAL BIOLOGY   (India)

Author keywords

Contraception; Dual action microbicides; Fertility control; HIV AIDS; Spermicide

Indexed keywords

ABACAVIR; ACIDIFORM; ANTIRETROVIRUS AGENT; BEVIRIMAT; CARBOPOL 974P; CARBOXYMETHYLCELLULOSE; CARRAGEENAN; CELLACEFATE; CELLULOSE SULFATE; CHEMOKINE RECEPTOR CCR5; CONTRACEPTIVE AGENT; CYANOVIRIN N; ELVITEGRAVIR; EMTRICITABINE; IBALIZUMAB; LOVIRIDE; MARAVIROC; MICROBICIDE; MIV 150; N [3 [4 (3 BENZYL 1 ETHYL 5 PYRAZOLYL) 1 PIPERIDINYLMETHYL] 4 (3 FLUOROPHENYL)CYCLOPENTYL] N METHYLVALINE; NEVIRAPINE; PRO 140; PRO 2000; PSC RANTES; RALTEGRAVIR; RILPIVIRINE; STAMPIDINE; TENOFOVIR; TERAMEPROCOL; UNCLASSIFIED DRUG; UNINDEXED DRUG; VICRIVIROC; VIVAGEL; ZIDOVUDINE;

ACQUIRED IMMUNE DEFICIENCY SYNDROME; ANTIVIRAL ACTIVITY; ANTIVIRAL THERAPY; ANUS INTERCOURSE; CHLAMYDIA TRACHOMATIS; CLINICAL TRIAL; DISEASE TRANSMISSION; DRUG MECHANISM; DRUG SAFETY; EPIDEMIC; HERPES SIMPLEX VIRUS; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; INTESTINE LYMPHATIC TISSUE; LACTOBACILLUS; REVIEW; RISK FACTOR; SEXUAL TRANSMISSION; SEXUALLY TRANSMITTED DISEASE; VAGINA CONTRACEPTION; VIRUS TRANSMISSION;

EID: 77349105934     PISSN: 14726483     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.rbmo.2009.10.018     Document Type: Review

References (81)

1. Alkhatib, G., Combadiere, C., Broder, C.C., et al., 1996. CC CKR5: a RANTES, MIP-1alpha, MIP-1beta receptor as a fusion cofactor for macrophage-tropic HIV-1. Science 272, 1955-1958.
2. Alliance for microbicide development, http://www.microbicide.org/cs/ micribicide-pipetine (will be available at www.a-vac.org from 2010 onward).
3. Bernstein, I., Stanberry, L.R., Sacks, S., 2003. Evaluations of unformulated and formulated dendrimer-based microbicide candidates in mouse and guinea pig models of genital herpes D. Antimicrob. Agents Chemother. 47, 3784-3788.
4. Bomsel, M., 1997. Transcytosis of infectious human immunodeficiency virus across a tight human epithelial cell line barrier. Nature Med. 3, 42-47.
5. + T cell depletion during all stages of HIV disease occurs predominantly in the gastrointestinal tract. J. Experiment. Med. 200, 749-759.
6. Centers for Disease Control and Prevention, 2005. HIV/AIDS Surveillance Report, 2004 16, 1-46. Also available at: http://www.cdc.gov/ hiv/stats/hasrlink.htm.
7. Clayton, F., Snow, G., Reka, S., Kotler, D.P., 1997. Selective depletion of rectal lamina propria rather than lymphoid aggregate CD4 lymphocytes in HIV infection. Clin. Experiment. Immunol. 107, 288-292.
8. Cook, R.L., Rosenberg, M.J., 1998. Do spermicides containing nonoxynol-9 prevent sexually transmitted infections? A meta-analysis. Sex. Trans. Dis. 25, 144-150.
9. D'Cruz, O.J., Uckun, F.M., 2004. Clinical development of microbicides for the prevention of HIV infection. Curr. Pharmaceut. Des. 10, 315-336.
10. D'Cruz, O.J., Zhu, Z., Yiv, S.H., et al., 1999. Wh-05, a novel bromo-methoxy substituted phenyl phosphate derivative of zidovudine, is a dual action spermicide with potent anti-HIV activity. Contraception 59, 319-331.
11. Deng, H., Liu, R., Ellmeier, W., et al., 1996. Identification of a major co-receptor for primary isolates of HIV-1. Nature 381, 661-666.
12. Dragic, T., Litwin, V., Allaway, G.P., et al., 1996. HIV-1 entry into CD4+ cells is mediated by the chemokine receptor CC-CKR-5. Nature 381, 667-673.
13. Elias, C., Coggins, C., 2001. Acceptability research on female controlled methods to prevent heterosexual transmission of HIV: where have we been? Where are we going? J. Women's Health Gender Based Med. 10, 163-173.
14. Esser, M.T., Mori, T., Mondor, I., et al., 1999. Cyanovirin-N binds to gp120 to interfere with CD4-dependent human immunodeficiency virus type 1 virion binding, fusion, and infectivity but does not affect the CD4 binding site on gp120 or soluble CD4-induced conformational changes in gp120. J. Virol. 73, 4360-4371.
15. European Study Group on Heterosexual Transmission of HIV, 1992. Comparison of female-to-male and male-to-female transmission of HIV in 563 stable couples. Br. Med. J. 304, 809-813.
16. Fernàndez-Romero, J.A., Thorn, M., Turville, S.G., et al., 2007. Carrageenan/MIV-150 (PC-815), a combination microbicide. Sex. Trans. Dis. 34, 9-14.
17. Fichorova, R.N., Tucker, L.D., Anderson, D.J., et al., 2001. The molecular basis of nonoxynol-9-induced vaginal inflammation and its possible relevance to human immunodeficiency virus type 1 transmission. J. Infect. Dis. 184, 418-428.
18. Fischl, M., Richman, D., Grieco, M., et al., 1987. The efficacy of azidothymidine (AZT) in the treatment of patients with AIDS and AIDS-related complex. A double-blind, placebo-controlled trial. New England J. Med. 317, 185-191.
19. Fletcher, P., Kiselyeva, Y., Wallace, G., et al., 2005. The nonnucleoside reverse transcriptase inhibitor UC-781 inhibits human immunodeficiency virus type 1 infection of human cervical tissue and dissemination by migratory cells. J. Virol. 79, 11179-11186.
20. Geijtenbeek, T.B., Kwon, D.S., Torensma, R., et al., 2000. DC-SIGN, a dendritic cell-specific HIV-1-binding protein that enhances transinfection of T cells. Cell 100, 587-597.
21. Guo, Q., Ho, H.T., Dicker, I., et al., 2003. Biochemical and genetic characterizations of a novel human immunodeficiency virus type 1 inhibitor that blocks gp120-CD4 interactions. J. Virol. 77, 10528-10536.
22. Gyotoku, T., Aurelian, L., Neurath, A.R., et al., 1999. Cellulose acetate phthalate (CAP): an 'inactive' pharmaceutical excipient with antiviral activity in the mouse model of genital herpesvirus infection. J. Antiviral Chem. Chemother. 10, 327-332.
23. Haase, A.T., 2005. Perils at the mucosal frontlines for HIV and SIV and their hosts. Nature Rev. Immunol. 5, 783-792.
24. Haineault, C., Gourde, P., Perron, S., et al., 2003. Thermoreversible gel formulation containing sodium lauryl sulfate as a potential contraceptive device. Biol. Reprod. 69, 687-694.
25. Harman, S., Watts, P., Shattock, R., et al., 2004. TMC120 blocks HIV-1 infection in cellular and human cervical tissue models. Abstract # 02591, Presented at: Microbicides 2004 Conference; London.
26. Heise, L., 1997. Beyond acceptability: reorienting research on contraceptive choice. In: Ravindran, T.K.S., Berer, M., Cottingham, J. (Eds.), Beyond Acceptability: Users' Perspectives on Contraception. Reproductive Health Matters, London, pp. 6-14.
27. Hermonat, P.L., Daniel, R.W., Shah, K.V., et al., 1992. The spermicide nonoxynol-9 does not inactivate papilloma virus. Sex. Trans. Dis. 19, 203-205.
28. Hicks, D.R., Martin, L.S., Getchell, J.P., et al., 1985. Inactivation of HTLV-III/LAV-infected cultures of normal human lymphocytes by nonoxynol-9 in vitro. Lancet 2, 1422-1423.
29. Hossain, M.M., Parniak, M.A., 2006. In vitro microbicidal activity of the nonnucleoside reverse transcriptase inhibitor (NNRTI) UC781 against NNRTI-resistant human immunodeficiency virus type 1. J. Virol. 80, 4440-4446.
30. Jennings, R., Clegg, A., 1993. The inhibitory effect of spermicidal agents on replication of HSV-2 and HIV-1 in vitro. J. Antimicrob. Agents Chemother. 32, 71-82.
31. Judson, F.N., Ehret, J.M., Bodin, G.F., et al., 1989. In vitro evaluations of condoms with and without nonoxynol 9 as physical and chemical barriers against Chlamydia trachomatis, herpes simplex virus type 2 and human immunodeficiency virus. Sex. Trans. Dis. 16, 51-55.
32. Kabir, S.N., Ray, H., Pal, B.C., et al., 2008. Pharmaceutical composition having virucidal and spermicidal activity. US patent No. 20080300197.
33. Kaul, R., Nagelkerke, N.J., Kimani, J., et al., 2007. Prevalent herpes simplex virus type 2 infection is associated with altered vaginal flora and an increased susceptibility to multiple sexually transmitted infections. J. Infect. Dis. 196, 1692-1697.
34. Kawamura, T., Bruse, S.E., Abraha, A., et al., 2004. PSC-RANTES blocks R5 human immunodeficiency virus infection of Langerhans cells isolated from individuals with a variety of CCR5 diplotypes. J. Virol. 78, 7602-7609.
35. Kawamura, T., Gulden, F.O., Sugaya, M., et al., 2003. R5 HIV productively infects Langerhans cells, and infection levels are regulated by compound CCR5 polymorphisms. Proc. Natl. Acad. Sci. USA 100, 8401-8406.
36. Krebs, F.C., Catalone, B.J., et al., 2000. Sodium dodecyl sulfate and C31G as microbicidal alternatives to nonoxynol-9: comparative sensitivity of primary human vaginal keratinocytes. Antimicrob. Agents Chemother. 44, 1954-1960.
37. Lederman, M.M., Veazey, R.S., Offord, R., et al., 2004. Prevention of vaginal SHIV transmission in rhesus macaques through inhibition of CCR5. Science 306, 485-487.
38. LeGoff, J., Weiss, H.A., Gresenguet, G., et al., 2007. Cervicovaginal HIV-1 and herpes simplex virus type 2 shedding during genital ulcer disease episodes. Acq. Immunodef. Synd. 12, 1569-1578.
39. Lin, P.F., Blair, W., Wang, T., et al., 2003. A small molecule HIV-1 inhibitor that targets the HIV-1 envelope and inhibits CD4 receptor binding. Proc. Natl. Acad. Sci. USA 100, 11013-11018.
40. Lu M. 2004. Stabilizing peptides and their use in the preparation of stabilized HIV inhibitors. World Intellectual Property Organization patent WO-04/106364A1.
41. Manson, K.H., Wyand, M.S., Miller, C, et al., 2000. Effect of a cellulose acetate phthalate topical cream on vaginal transmission of simian immunodeficiency virus in rhesus monkeys. Antimicrob. Agents Chemother. 44, 3199-3202.
42. Mantell, J.E., Myer, L., Carballo-Dieuguez, A., et al., 2005. Microbicide acceptability research: current approaches and future directions. Soc. Sci. Med. 60, 319-330.
43. Martin, H.L., Richardson, B.A., Nyange, P.M., et al., 1999. Vaginal lactobacilli, microflora, and risk of human immunodeficiency virus type 1 and sexually transmitted disease acquisition. J. Infect. Dis. 180, 1863-1868.
44. Mauck, C.K., Frezieres, R.G., Walsh, T.L., et al., 2004. A male tolerance study of 1% C31G. Contraception 70, 221-225.
45. Mayer, K.H., Maslankowski, L.A., Gai, F., et al., 2006. Safety and tolerability of tenofovir vaginal gel in abstinent and sexually active HIV-infected and uninfected women. Acq. Immunodef. Synd. 20, 543-551.
46. Mosher WD, Chandra A, Jones J. 2005. Sexual behavior and selected health measures: men and women 15-44 years of age in 2002, United States. Report 362, Hyatsville, MD: National Center for Health Statistics.
47. Newman MC. 2004. Women and HIV. HIV InSite Knowledge Base Chapter. UCSF Center for HIV information. Available from: http://hivinsite.ucsf.edu/lnSite. jsp?page=kb-03-01-12.
48. Nicolosi, A., Correa Leite, M.L., Musicco, M., et al., 1994. The efficiency of male-to-female and female-to-male sexual transmission of the human immunodeficiency virus: a study of 730 stable couples. Italian Study Group on HIV Heterosexual Transmission. Epidemiology 5, 570-575.
49. Oberg B, Zhang H, Vrang L, Bottinger D. 2004. MIV-150, a potent HIV-1 inhibitor suitable for use in microbicides. Abstract # 02451, Presented at: Microbicides 2004 Conference; London.
50. O'Connor, T.J., Kinchington, D., Kangro, H.D., et al., 1995. The activity of candidate virucidal agents, low pH and genital secretions against HIV-1 in vitro. Int. J. Sex. Trans. Dis. Acq. Immunodef. Synd. 6, 267-272.
51. Patton, D.L., Sweeney, Y.C., Rabe, L.K., et al., 1999. Effects of multiple applications of benzalkonium chloride and nonoxynol-9 on the vaginal epithelium in the pigtailed macaque (Macaca nemestrina). Amer. J. Obstet. Gynecol. 180, 1080-1087.
52. Pauwels, R., De Clercq, E., 1996. Development of vaginal microbicides for the prevention of heterosexual transmission of HIV. J. Acq. Imm. Def. Synd. Human Retrovirol. 11, 211-221.
53. Perotti, M.E., Pirovano, A., Phillips, D.M., 2003. Carrageenan formulation prevents macrophage trafficking from vagina: implications for microbicide development. Biol. Reprod. 69, 933-939.
54. Peterson, L., Nanda, K., Opoku, B.K., et al., 2007. SAVVY® (C31G) Gel for prevention of HIV infection in women: a phase 3, double-blind, randomized, placebo-controlled trial in Ghana. Pub. Lib. Sci. One J. 2, e1312.
55. Pohlmann, S., Baribaud, F., Doms, R.W., et al., 2001. DC-SIGN and DC-SIGNR: helping hands for HIV. Trends Immunol. 22, 643-646.
56. Profy, A.T., Sonderfan, A.J., Bernstein, D.I., et al., 2000. PRO 2000 gel, a potential topical microbicide for HIV prevention, can block infection by other sexually transmitted disease pathogens. Int. Conf. AIDS 12, 620-621 (Abstract No. 33146).
57. Roddy, R.E., Zekeng, L., Ryan, K.A., et al., 1998. A controlled trial of nonoxynol 9 film to reduce male-to-female transmission of sexually transmitted diseases. New England J. Med. 339, 504-510.
58. Roy, S., Gourde, P., Piret, J., et al., 2001. Thermoreversible gel formulations containing sodium lauryl sulfate or n-lauroylsarcosine as potential topical microbicides against sexually transmitted diseases. Antimicrob. Agents Chemother. 45, 1671-1681.
59. Scordi-Bello, I.A., Mosoian, A., et al., 2005. Candidate sulfonated and sulfated topical microbicides: comparison of anti-human immunodeficiency virus activities and mechanisms of action. Antimicrob. Agents Chemother. 49, 3607-3615.
60. Severy, L.J., Tolley, E., Woodsong, C., et al., 2005. A frame work for examining the sustained susceptibility of microbicides. AIDS Behav. 9, 121-131.
61. Sexton, A., Drake, P.M., Mahmood, N., et al., 2006. Transgenic plant production of cyanovirin-N, an HIV microbicide. Fed. Amer. Soc. Experiment. Biol. J. 20, 356-358.
62. Smith, R.J., Bodine, E.N., Wilson, D.P., et al., 2005. Evaluating the potential impact of vaginal microbicides to reduce the risk of acquiring HIV in female sex workers. Acq. Immunodef. Synd. 19, 413-421.
63. Smolewski, P., 2008. Terameprocol, a novel site-specific transcription inhibitor with anti-cancer activity. Invest. Drugs 11, 204-214.
64. Soledad, B., Barbés, C., 2000. Role played by lactobacilli in controlling the population of vaginal pathogens. Micro. Infect. 2, 543-546.
65. Stafford, M.K., Ward, H., Flanagan, A., et al., 1998. Safety study of nonoxynol-9 as a vaginal microbicide: evidence of adverse effects. J. Acq. Imm. Def. Synd. Human Retroviral. 17, 327-331.
66. Stein, Z., Myer, Land, Susser, M., 2003. The design of prophylactic trials for HIV: the case of microbicides. Epidemiology 14, 80-83.
67. Taha, T.E., Hoover, D.R., Dallabetta, L.A., et al., 1998. Bacterial vaginosis and disturbances of vaginal flora; association with increased acquisition of HIV. Acq. Immunodef. Synd. 12, 1699-1706.
68. Talwar, G.P., Raghuvanshi, P., Mishra, R., et al., 2000. Polyherbal formulations with wide spectrum antimicrobial activity against reproductive tract infections and sexually transmitted pathogens. Amer. J. Reprod. Immunol. 43, 144-151.
69. Tobacman, J.K., 2001. Review of harmful gastrointestinal effects of carrageenan in animal experiments. Environ. Health Perspect. 109, 983-994.
70. Torre, V.S., Marozsan, A.J., Albright, J.L., et al., 2000. Variable sensitivity of CCR5-tropic human immunodeficiency virus type 1 isolates to inhibition by RANTES analogs. J. Virol. 74, 4868-4876.
71. Trials Network, 2006. HPTN 035: Phase II/IIb Safety and effectiveness study of the vaginal microbicides BufferGel and 0.5% PRO2000/5 Gel (P) for the prevention of HIV infection in women. Available at: http://www.hptn.org/ research-studies/hptn035.asp.
72. UNAIDS, 2008. Executive summary of Report on the Global AIDS Epidemic. Available at: http://data.unaids.org/pub/GlobalReport/2008/JC1511-GR08- ExecutiveSummary-en.pdf.
73. UNAIDS, 2005. AIDS epidemic update: December 2005 Available at: http://www.who.int/hiv/epi-update2005-en.pdf.
74. UNAIDS, WHO AIDS epidemic update 2007. UNAIDS/World Health Organization, Geneva, Switzerland. Available at: http://data.unaids.org/pub/EPISlides/2007/ 2007-epiupdate-en.pdf.
75. Van Damme, L., Ramjee, G., Alary, M., et al., 2002. Effectiveness of COL-1492, a nonoxynol-9 vaginal gel, on HIV transmission in female sex workers: a randomized control trial. Lancet 9338, 971-977.
76. Veazey, R.S., Klasse, P.J., Schader, S.M., et al., 2005. Protection of macaques from vaginal SHIV challenge by vaginally delivered inhibitors of virus-cell fusion. Nature 438, 99-102.
77. Watts, C., Kumaranayake, L., Vickerman, P., et al., 2004. Impact of an Efficacious Microbicide on Global HIV Transmission: Model Projections, a Public Health and the Environment. Microbicides, Washington, DC.
78. Woodsong, C., 2004. Covert use of topical microbicides: implications for acceptability and use. Perspect. Sex. Reprod. Health 36, 127-131.
79. Zacharopoulos, V.R., Phillips, D.M., 1997. Vaginal formulations of carrageenan protect mice from herpes simplex virus infection. Clin. Diag. Lab. Immunol. 4, 465-468.
80. Zeitlin, L., Hoen, T.E., Achilles, S.L., et al., 2001. Tests of Buffergel for contraception and prevention of sexually transmitted diseases in animal models. Sex. Trans. Dis. 28, 417-423.
81. Zekeng, L., Feldblum, P.J., Oliver, R.M., et al., 1993. Barrier contraceptive use and HIV infection among high-risk women in Cameroon. Acq. Immunodef. Synd. 7, 725-731.