Journal of Pharmaceutics / 2014 / Article / Tab 2

Review Article

Microbicides for the Treatment of Sexually Transmitted HIV Infections

Table 2

Mechanism of action of different generations of microbicide candidates.

Mechanism of actionCandidates

First-generation microbicide (GEN-1)
Viral disrupting agentsC-31G (savvy), nonoxynol-9, octoxynol-9, benzalkonium chloride, octyl glycerol/milk lipids, polybiguanides, sodium dodecyl sulphate, Z-14 (acylcarnitine analogue), and so forth.

Second-generation microbicide (GEN-2)
Blocking HIV bindingCarrageenan, cellulose sulfate, naphthalene sulfonate, PRO 2000/5, dextrin-2-sulfate, heparan sulfate/cholic acid, polyanionic Gp120 inhibitors, polystyrene sulfonate, and so forth.

New-generation microbicide
gp120-binding agentsmAb b12, CD IgG2, and BMS-806
Gp41-binding agentsT-20 (enfuvirtide), mAb 2F5, 4E10, and T1249
Targeting soluble CD4 receptormAb (TNX-355), soluble CD4-IgG
Targeting CXCR4 coreceptorAMD3100, AMD070 small molecules antagonists
Targeting CCR5 coreceptorPRO-140, PSC-RANTES
Dendritic cell uptake inhibitorDC-SIGN and macrophage mannose binding receptor
NNRTI (nonnucleoside reverse transcriptase inhibitors)MIV-150, TMC120, UC781, and S-DABO
NtRTIs (nucleotide reverse transcriptase inhibitors)PMPA (tenofovir)
Integrase inhibitorsS-1360, C-731

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