Literature DB >> 22504027

Where rilpivirine meets with tenofovir, the start of a new anti-HIV drug combination era.

Erik De Clercq1.   

Abstract

The triple-drug once-daily combination pill containing tenofovir, emtricitabine and rilpivirine for HIV treatment was launched in 2011, both in the USA (Complera) and the E.U. (Eviplera). The active ingredients of Complera or Eviplera are the nucleotide reverse transcriptase inhibitor (NtRTI) tenofovir, the nucleoside reverse transcriptase inhibitor (NRTI) emtricitabine, and the non-nucleoside reverse transcriptase inhibitor (NNRTI) rilpivirine. Rilpivirine originated from a collaborative research I had started with Dr. Paul Janssen in 1987, whereas tenofovir emanated from a collaborative research with Dr. Antonin Holý and Gilead Sciences. Exactly twenty-five years later rilpivirine and tenofovir joined each other, together with emtricitabine, in the same "combo" pill, representing a full treatment regimen for AIDS (HIV infection) based on a single once-daily pill.
Copyright © 2012 Elsevier Inc. All rights reserved.

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Year:  2012        PMID: 22504027     DOI: 10.1016/j.bcp.2012.03.024

Source DB:  PubMed          Journal:  Biochem Pharmacol        ISSN: 0006-2952            Impact factor:   5.858


  13 in total

1.  Understanding the molecular mechanism of sequence dependent tenofovir removal by HIV-1 reverse transcriptase: differences in primer binding site versus polypurine tract.

Authors:  Pinar Iyidogan; Karen S Anderson
Journal:  Antiviral Res       Date:  2012-06-01       Impact factor: 5.970

2.  Differential activation of human constitutive androstane receptor and its SV23 and SV24 splice variants by rilpivirine and etravirine.

Authors:  Devinder Sharma; Aik Jiang Lau; Matthew A Sherman; Thomas K H Chang
Journal:  Br J Pharmacol       Date:  2015-02-10       Impact factor: 8.739

Review 3.  Three-dimensional structures in the design of therapeutics targeting parasitic protozoa: reflections on the past, present and future.

Authors:  Wim G J Hol
Journal:  Acta Crystallogr F Struct Biol Commun       Date:  2015-04-16       Impact factor: 1.056

Review 4.  Approved Antiviral Drugs over the Past 50 Years.

Authors:  Erik De Clercq; Guangdi Li
Journal:  Clin Microbiol Rev       Date:  2016-07       Impact factor: 26.132

Review 5.  Microbicides: still a long road to success.

Authors:  Christophe Vanpouille; Anush Arakelyan; Leonid Margolis
Journal:  Trends Microbiol       Date:  2012-06-15       Impact factor: 17.079

6.  Increase in single-tablet regimen use and associated improvements in adherence-related outcomes in HIV-infected women.

Authors:  David B Hanna; Nancy A Hessol; Elizabeth T Golub; Jennifer M Cocohoba; Mardge H Cohen; Alexandra M Levine; Tracey E Wilson; Mary Young; Kathryn Anastos; Robert C Kaplan
Journal:  J Acquir Immune Defic Syndr       Date:  2014-04-15       Impact factor: 3.731

7.  Theaflavin-3,3'-digallate and lactic acid combinations reduce herpes simplex virus infectivity.

Authors:  Charles E Isaacs; Weimin Xu
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8.  The connection domain mutation N348I in HIV-1 reverse transcriptase enhances resistance to etravirine and rilpivirine but restricts the emergence of the E138K resistance mutation by diminishing viral replication capacity.

Authors:  Hong-Tao Xu; Susan P Colby-Germinario; Maureen Oliveira; Yingshan Han; Yudong Quan; Veronica Zanichelli; Mark A Wainberg
Journal:  J Virol       Date:  2013-11-13       Impact factor: 5.103

9.  Enhanced activity of carbosilane dendrimers against HIV when combined with reverse transcriptase inhibitor drugs: searching for more potent microbicides.

Authors:  Enrique Vacas-Córdoba; Marta Galán; Francisco J de la Mata; Rafael Gómez; Marjorie Pion; M Ángeles Muñoz-Fernández
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Review 10.  An Odyssey in antiviral drug development-50 years at the Rega Institute: 1964-2014.

Authors:  Erik De Clercq
Journal:  Acta Pharm Sin B       Date:  2015-11-02       Impact factor: 11.413

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