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The combined anti-HIV-1 activities of emtricitabine and tenofovir plus the integrase inhibitor elvitegravir or raltegravir show high levels of synergy in vitro.

Antimicrobial agents and chemotherapy (2014-08-06)
Rima Kulkarni, Rebecca Hluhanich, Damian M McColl, Michael D Miller, Kirsten L White
ABSTRACT

Highly active antiretroviral therapy (HAART) involves combination treatment with three or more antiretroviral agents. The antiviral effects of combinations of emtricitabine (FTC) plus tenofovir (TFV) plus antiretroviral agents of all the major drug classes were investigated. Combinations of FTC and TFV with a nonnucleoside reverse transcriptase inhibitor (NNRTI) (efavirenz or rilpivirine) or with a protease inhibitor (PI) (atazanavir, lopinavir, or darunavir) showed additive to synergistic anti-HIV-1 activity. FTC-TFV with an HIV-1 integrase strand transfer inhibitor (INSTI) (elvitegravir or raltegravir) showed the strongest synergy. Anti-HIV-1 synergy suggests enhancement of individual anti-HIV-1 activities within cells that may contribute to potent treatment efficacy and open new areas of research into interactions between reverse transcriptase (RT) and integrase inhibitors.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Ribavirin, antiviral
Sigma-Aldrich
3′-Azido-3′-deoxythymidine, ≥98% (HPLC)
Supelco
Zidovudine, Pharmaceutical Secondary Standard; Certified Reference Material
Sigma-Aldrich
Darunavir, ≥98% (HPLC)
USP
Zidovudine, United States Pharmacopeia (USP) Reference Standard
Zidovudine, European Pharmacopoeia (EP) Reference Standard
Ribavirin, European Pharmacopoeia (EP) Reference Standard