Literature DB >> 25092710

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

Rima Kulkarni1, Rebecca Hluhanich2, Damian M McColl2, Michael D Miller2, Kirsten L White2.   

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.
Copyright © 2014, American Society for Microbiology. All Rights Reserved.

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Year:  2014        PMID： 25092710      PMCID： PMC4187912          DOI： 10.1128/AAC.03591-14

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  45 in total

1.  A randomized, double-blind comparison of single-tablet regimen elvitegravir/cobicistat/emtricitabine/tenofovir DF versus single-tablet regimen efavirenz/emtricitabine/tenofovir DF for initial treatment of HIV-1 infection: analysis of week 144 results.

Authors:  David A Wohl; Calvin Cohen; Joel E Gallant; Anthony Mills; Paul E Sax; Edwin Dejesus; Andrew Zolopa; Hui C Liu; Andrew Plummer; Kirsten L White; Andrew K Cheng; Martin S Rhee; Javier Szwarcberg
Journal:  J Acquir Immune Defic Syndr       Date:  2014-03-01       Impact factor: 3.731

2.  Antiviral activity, pharmacokinetics, and dose response of the HIV-1 integrase inhibitor GS-9137 (JTK-303) in treatment-naive and treatment-experienced patients.

Authors:  Edwin DeJesus; Daniel Berger; Martin Markowitz; Calvin Cohen; Trevor Hawkins; Peter Ruane; Richard Elion; Charles Farthing; Lijie Zhong; Andrew K Cheng; Damian McColl; Brian P Kearney
Journal:  J Acquir Immune Defic Syndr       Date:  2006-09       Impact factor: 3.731

3.  Drug combinations and effect parameters of zidovudine, stavudine, and nevirapine in standardized drug-sensitive and resistant HIV type 1 strains.

Authors:  Q Y Zhu; A Scarborough; B Polsky; T C Chou
Journal:  AIDS Res Hum Retroviruses       Date:  1996-04-10       Impact factor: 2.205

4.  Dead-end complexes contribute to the synergistic inhibition of HIV-1 RT by the combination of rilpivirine, emtricitabine, and tenofovir.

Authors:  Rima Kulkarni; Joy Y Feng; Michael D Miller; Kirsten L White
Journal:  Antiviral Res       Date:  2013-11-28       Impact factor: 5.970

5.  Co-formulated elvitegravir, cobicistat, emtricitabine, and tenofovir disoproxil fumarate versus ritonavir-boosted atazanavir plus co-formulated emtricitabine and tenofovir disoproxil fumarate for initial treatment of HIV-1 infection: a randomised, double-blind, phase 3, non-inferiority trial.

Authors:  Edwin DeJesus; Jürgen K Rockstroh; Keith Henry; Jean-Michel Molina; Joseph Gathe; Srinivasan Ramanathan; Xuelian Wei; Kitty Yale; Javier Szwarcberg; Kirsten White; Andrew K Cheng; Brian P Kearney
Journal:  Lancet       Date:  2012-06-30       Impact factor: 79.321

6.  Rapid and durable antiretroviral effect of the HIV-1 Integrase inhibitor raltegravir as part of combination therapy in treatment-naive patients with HIV-1 infection: results of a 48-week controlled study.

Authors:  Martin Markowitz; Bach-Yen Nguyen; Eduardo Gotuzzo; Fernando Mendo; Winai Ratanasuwan; Colin Kovacs; Guillermo Prada; Javier O Morales-Ramirez; Clyde S Crumpacker; Robin D Isaacs; Lucinda R Gilde; Hong Wan; Michael D Miller; Larissa A Wenning; Hedy Teppler
Journal:  J Acquir Immune Defic Syndr       Date:  2007-10-01       Impact factor: 3.731

7.  Decay dynamics of HIV-1 depend on the inhibited stages of the viral life cycle.

Authors:  Ahmad R Sedaghat; Jason B Dinoso; Lin Shen; Claus O Wilke; Robert F Siliciano
Journal:  Proc Natl Acad Sci U S A       Date:  2008-03-24       Impact factor: 11.205

8.  Ribavirin antagonizes inhibitory effects of pyrimidine 2',3'-dideoxynucleosides but enhances inhibitory effects of purine 2',3'-dideoxynucleosides on replication of human immunodeficiency virus in vitro.

Authors:  M Baba; R Pauwels; J Balzarini; P Herdewijn; E De Clercq; J Desmyter
Journal:  Antimicrob Agents Chemother       Date:  1987-10       Impact factor: 5.191

9.  New tetrahydroimidazo[4,5,1-jk][1,4]-benzodiazepin-2(1H)-one and -thione derivatives are potent inhibitors of human immunodeficiency virus type 1 replication and are synergistic with 2',3'-dideoxynucleoside analogs.

Authors:  R Pauwels; K Andries; Z Debyser; M J Kukla; D Schols; H J Breslin; R Woestenborghs; J Desmyter; M A Janssen; E De Clercq
Journal:  Antimicrob Agents Chemother       Date:  1994-12       Impact factor: 5.191

10.  The triple combination of tenofovir, emtricitabine and efavirenz shows synergistic anti-HIV-1 activity in vitro: a mechanism of action study.

Authors:  Joy Y Feng; John K Ly; Florence Myrick; Derrick Goodman; Kirsten L White; Evguenia S Svarovskaia; Katyna Borroto-Esoda; Michael D Miller
Journal:  Retrovirology       Date:  2009-05-13       Impact factor: 4.602
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  12 in total

1.  Seminal Tenofovir Concentrations, Viral Suppression, and Semen Quality With Tenofovir Alafenamide, Compared With Tenofovir Disoproxil Fumarate (Spanish HIV/AIDS Research Network, PreEC/RIS 40).

Authors:  Arkaitz Imaz; Jordi Niubó; Mackenzie L Cottrell; Emilia Perez; Angela D M Kashuba; Juan M Tiraboschi; Sandra Morenilla; Benito Garcia; Daniel Podzamczer
Journal:  Clin Infect Dis       Date:  2019-09-27       Impact factor: 9.079

2.  Reduced viral fitness and lack of cross-class resistance with integrase strand transfer inhibitor and nucleoside reverse transcriptase inhibitor resistance mutations.

Authors:  Kristen N Andreatta; Derrick D Goodman; Michael D Miller; Kirsten L White
Journal:  Antimicrob Agents Chemother       Date:  2015-03-30       Impact factor: 5.191

3.  An Enhanced Emtricitabine-Loaded Long-Acting Nanoformulation for Prevention or Treatment of HIV Infection.

Authors:  Subhra Mandal; Michael Belshan; Ashley Holec; You Zhou; Christopher J Destache
Journal:  Antimicrob Agents Chemother       Date:  2016-12-27       Impact factor: 5.191

Review 4.  Elvitegravir: a review of its use in adults with HIV-1 infection.

Authors:  Emma D Deeks
Journal:  Drugs       Date:  2014-04       Impact factor: 9.546

5.  Antiretroviral Hydrophobic Core Graft-Copolymer Nanoparticles: The Effectiveness against Mutant HIV-1 Strains and in Vivo Distribution after Topical Application.

Authors:  Anita Leporati; Suresh Gupta; Elijah Bolotin; Gerardo Castillo; Joshua Alfaro; Marina B Gottikh; Alexei A Bogdanov
Journal:  Pharm Res       Date:  2019-03-27       Impact factor: 4.200

6.  Early HIV RNA decay during raltegravir-containing regimens exhibits two distinct subphases (1a and 1b).

Authors:  Adriana Andrade; Jeremie Guedj; Susan L Rosenkranz; Darlene Lu; John Mellors; Daniel R Kuritzkes; Alan S Perelson; Ruy M Ribeiro
Journal:  AIDS       Date:  2015-11-28       Impact factor: 4.177

Review 7.  Genetic Consequences of Antiviral Therapy on HIV-1.

Authors:  Miguel Arenas
Journal:  Comput Math Methods Med       Date:  2015-06-10       Impact factor: 2.238

8.  Topical Delivery of Tenofovir Disoproxil Fumarate and Emtricitabine from Pod-Intravaginal Rings Protects Macaques from Multiple SHIV Exposures.

Authors:  Priya Srinivasan; John A Moss; Manjula Gunawardana; Scott A Churchman; Flora Yang; Chuong T Dinh; James M Mitchell; Jining Zhang; Rob Fanter; Christine S Miller; Irina Butkyavichene; Janet M McNicholl; Thomas J Smith; Marc M Baum; James M Smith
Journal:  PLoS One       Date:  2016-06-08       Impact factor: 3.240

9.  Inhibition of Plasmodium Hepatic Infection by Antiretroviral Compounds.

Authors:  Marta Machado; Margarida Sanches-Vaz; João P Cruz; António M Mendes; Miguel Prudêncio
Journal:  Front Cell Infect Microbiol       Date:  2017-07-19       Impact factor: 5.293

10.  Structural Basis of Nanobodies Targeting the Prototype Norovirus.

Authors:  Kerstin Ruoff; Turgay Kilic; Jessica Devant; Anna Koromyslova; Alessa Ringel; Alexander Hempelmann; Celina Geiss; Juliane Graf; Michelle Haas; Imme Roggenbach; Grant Hansman
Journal:  J Virol       Date:  2019-03-05       Impact factor: 5.103
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