Abstract
We compared the preclinical safety and efficacy of tenofovir (TFV) 1% gel with that of MZC gel [containing 50 μM MIV-150, 14 mM Zn(O2CCH3)2(H2O)2, and 3% carrageenan] through a series of in vitro, ex vivo, and in vivo assays. The two gels showed good antiviral therapeutic indexes (50% cytotoxic concentration/50% effective concentration ratios; range, >25 to 800). MZC showed greater anti-simian-human immunodeficiency virus reverse transcriptase (SHIV-RT) activity than TFV 1% gel in rhesus macaque vaginal explants. MZC protected mice from vaginal herpes simplex virus 2 (HSV-2) challenge (P < 0.0001), but the TFV 1% gel did not.
Copyright © 2016 Jean-Pierre et al.
Publication types
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Research Support, U.S. Gov't, Non-P.H.S.
MeSH terms
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Administration, Intravaginal
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Animals
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Anti-Retroviral Agents / administration & dosage
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Anti-Retroviral Agents / pharmacology*
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Carrageenan / chemistry
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Drug Combinations
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Female
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Gels / administration & dosage
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Gels / chemistry
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HIV-1 / drug effects
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Herpesvirus 2, Human / drug effects
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Herpesvirus 2, Human / pathogenicity
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Macaca mulatta
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Mice, Inbred BALB C
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Pyridines / pharmacology
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Simian Acquired Immunodeficiency Syndrome / prevention & control
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Simian Immunodeficiency Virus / drug effects
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Tenofovir / pharmacology*
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Urea / analogs & derivatives
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Urea / pharmacology
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Vagina / drug effects
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Vagina / virology
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Zinc Acetate / administration & dosage
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Zinc Acetate / pharmacology*
Substances
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Anti-Retroviral Agents
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Drug Combinations
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Gels
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MIV 150
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Pyridines
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Urea
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Carrageenan
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Tenofovir
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Zinc Acetate