title: The combined anti-HIV-1 activities of emtricitabine and tenofovir plus the integrase inhibitor elvitegravir or raltegravir show high levels of synergy in vitro.
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.
authors.affiliation: Gilead Sciences, Inc., Foster City, California, USA rima.kulkarni@gilead.com.
authors.forename: Rima
authors.initials: R
authors.lastname: Kulkarni
authors.affiliation: Gilead Sciences, Inc., Foster City, California, USA.
authors.forename: Rebecca
authors.initials: R
authors.lastname: Hluhanich
authors.affiliation: Gilead Sciences, Inc., Foster City, California, USA.
authors.forename: Damian M
authors.initials: DM
authors.lastname: McColl
authors.affiliation: Gilead Sciences, Inc., Foster City, California, USA.
authors.forename: Michael D
authors.initials: MD
authors.lastname: Miller
authors.affiliation: Gilead Sciences, Inc., Foster City, California, USA.
authors.forename: Kirsten L
authors.initials: KL
authors.lastname: White
mesh_terms: D000225:Adenine / Q000031:analogs & derivatives* / Q000494:pharmacology; D019380:Anti-HIV Agents / Q000494:pharmacology*; D003841:Deoxycytidine / Q000031:analogs & derivatives* / Q000494:pharmacology; D004357:Drug Synergism; D000068679:Emtricitabine; D019429:Integrase Inhibitors / Q000494:pharmacology*; D063065:Organophosphonates / Q000494:pharmacology*; D011760:Pyrrolidinones / Q000494:pharmacology*; D015363:Quinolones / Q000494:pharmacology*; D000068898:Raltegravir Potassium; D018894:Reverse Transcriptase Inhibitors / Q000494:pharmacology; D000068698:Tenofovir
chemical_list: D019380:Anti-HIV Agents; D019429:Integrase Inhibitors; D063065:Organophosphonates; D011760:Pyrrolidinones; D015363:Quinolones; D018894:Reverse Transcriptase Inhibitors; D003841:Deoxycytidine; D000068898:Raltegravir Potassium; C509700:elvitegravir; D000068698:Tenofovir; D000068679:Emtricitabine; D000225:Adenine
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