Literature DB >> 31957507

Evaluating emtricitabine + rilpivirine + tenofovir alafenamide in combination for the treatment of HIV-infection.

Ying Mu1, Michelle Pham2, Anthony T Podany2, Theodore J Cory1.   

Abstract

Introduction: Antiretroviral therapy (ART) is recommended for all people who are living with HIV to suppress viral load and to stop the progression and transmission of HIV-1. Fixed-dose combinations of antiretrovirals largely reduce pill burden.Areas covered: The authors first provide an overview of the use of non-nucleoside reverse transcriptase inhibitor (NNRTI) based therapy in HIV care. They then summarize the properties of each drug in the fixed-dose combination of tenofovir alafenamide/emtricitabine/rilpivirine/(TAF/FTC/RPV). The efficacy and safety of each component and the combination as a whole are reviewed: FTC is non-inferior to lamivudine (3TC) at assessed dosages; TAF was non-inferior to tenofovir disoproxil fumarate (TDF); the viral efficacy of RPV is non-inferior with EFV at the assessed dosage; TAF/FTC/RPV is non-inferior in efficacy but shows less of a decline in bone mineral density and renal function compared to TDF/FTC/RPV. Finally, adverse effects and drug-drug interaction data with FTC/RPV/TAF are discussed.Expert opinion: TAF/FTC/RPV can be used as an initial regimen for people living with HIV whose HIV RNA <100,000 copies/ml and CD4 cell count > 200 cells/mm3 when INSTI-based regimens are not a treatment option. Future antiretroviral therapy development may focus on dual therapy-based regimens containing RPV, particularly as long-acting formulations.

Entities:  

Keywords:  Antiretroviral therapy; emtricitabine; rilpivirine; tenofovir alafenamide

Mesh:

Substances:

Year:  2020        PMID: 31957507      PMCID: PMC7061289          DOI: 10.1080/14656566.2020.1713096

Source DB:  PubMed          Journal:  Expert Opin Pharmacother        ISSN: 1465-6566            Impact factor:   3.889


  41 in total

1.  Antiviral activity, safety, and pharmacokinetics/pharmacodynamics of tenofovir alafenamide as 10-day monotherapy in HIV-1-positive adults.

Authors:  Peter J Ruane; Edwin DeJesus; Daniel Berger; Martin Markowitz; U Fritz Bredeek; Christian Callebaut; Lijie Zhong; Srini Ramanathan; Martin S Rhee; Marshall W Fordyce; Kitty Yale
Journal:  J Acquir Immune Defic Syndr       Date:  2013-08-01       Impact factor: 3.731

2.  Metabolism of GS-7340, a novel phenyl monophosphoramidate intracellular prodrug of PMPA, in blood.

Authors:  E J Eisenberg; G X He; W A Lee
Journal:  Nucleosides Nucleotides Nucleic Acids       Date:  2001 Apr-Jul       Impact factor: 1.381

3.  Switching from efavirenz, emtricitabine, and tenofovir disoproxil fumarate to tenofovir alafenamide coformulated with rilpivirine and emtricitabine in virally suppressed adults with HIV-1 infection: a randomised, double-blind, multicentre, phase 3b, non-inferiority study.

Authors:  Edwin DeJesus; Moti Ramgopal; Gordon Crofoot; Peter Ruane; Anthony LaMarca; Anthony Mills; Claudia T Martorell; Joseph de Wet; Hans-Jürgen Stellbrink; Jean-Michel Molina; Frank A Post; Ignacio Pérez Valero; Danielle Porter; YaPei Liu; Andrew Cheng; Erin Quirk; Devi SenGupta; Huyen Cao
Journal:  Lancet HIV       Date:  2017-03-02       Impact factor: 12.767

4.  Pharmacokinetic and pharmacodynamic characteristics of emtricitabine support its once daily dosing for the treatment of HIV infection.

Authors:  Laurene H Wang; John Begley; Robert L St Claire; Jeanette Harris; Charles Wakeford; Franck S Rousseau
Journal:  AIDS Res Hum Retroviruses       Date:  2004-11       Impact factor: 2.205

5.  Selective intracellular activation of a novel prodrug of the human immunodeficiency virus reverse transcriptase inhibitor tenofovir leads to preferential distribution and accumulation in lymphatic tissue.

Authors:  William A Lee; Gong-Xin He; Eugene Eisenberg; Tomas Cihlar; Swami Swaminathan; Andrew Mulato; Kenneth C Cundy
Journal:  Antimicrob Agents Chemother       Date:  2005-05       Impact factor: 5.191

6.  Plasma and intracellular population pharmacokinetic analysis of tenofovir in HIV-1-infected patients.

Authors:  Gautam Baheti; Jennifer J Kiser; Peter L Havens; Courtney V Fletcher
Journal:  Antimicrob Agents Chemother       Date:  2011-09-06       Impact factor: 5.191

7.  Prospective randomized trial of emtricitabine versus lamivudine short-term monotherapy in human immunodeficiency virus-infected patients.

Authors:  Franck S Rousseau; Charles Wakeford; Herve Mommeja-Marin; Ian Sanne; Cary Moxham; Jeanette Harris; Laura Hulett; Laurene H Wang; Joseph B Quinn; David W Barry
Journal:  J Infect Dis       Date:  2003-10-31       Impact factor: 5.226

8.  Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro.

Authors:  Eve-Irene Lepist; Truc K Phan; Anupma Roy; Leah Tong; Kelly Maclennan; Bernard Murray; Adrian S Ray
Journal:  Antimicrob Agents Chemother       Date:  2012-07-30       Impact factor: 5.191

9.  Safety, efficacy, and pharmacokinetics of rilpivirine: systematic review with an emphasis on resource-limited settings.

Authors:  Nathan Ford; Janice Lee; Isabelle Andrieux-Meyer; Alexandra Calmy
Journal:  HIV AIDS (Auckl)       Date:  2011-04-28

10.  Pharmacokinetics, Pharmacodynamics, and Safety of Entospletinib, a Novel pSYK Inhibitor, Following Single and Multiple Oral Dosing in Healthy Volunteers.

Authors:  Srini Ramanathan; Julie A Di Paolo; Feng Jin; Lixin Shao; Shringi Sharma; Michelle Robeson; Brian P Kearney
Journal:  Clin Drug Investig       Date:  2017-02       Impact factor: 2.859

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  1 in total

Review 1.  Tenofovir, Another Inexpensive, Well-Known and Widely Available Old Drug Repurposed for SARS-COV-2 Infection.

Authors:  Isabella Zanella; Daniela Zizioli; Francesco Castelli; Eugenia Quiros-Roldan
Journal:  Pharmaceuticals (Basel)       Date:  2021-05-11
  1 in total

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