Literature DB >> 21434946

Raltegravir: the first HIV-1 integrase strand transfer inhibitor in the HIV armamentarium.

Bach-Yen T Nguyen1, Robin D Isaacs, Hedy Teppler, Randi Y Leavitt, Peter Sklar, Marian Iwamoto, Larissa A Wenning, Michael D Miller, Joshua Chen, Ramon Kemp, Wei Xu, Robert A Fromtling, Joseph P Vacca, Steven D Young, Michael Rowley, Michael W Lower, Keith M Gottesdiener, Daria J Hazuda.   

Abstract

Raltegravir is the first integrase strand transfer inhibitor approved for the treatment of HIV-1 infection. As the first agent in this new class of antiretroviral therapies, raltegravir has demonstrated safety and efficacy in treatment-naive as well as heavily pretreated HIV-infected patients failing therapy with multidrug-resistant virus. Raltegravir has a favorable drug interaction profile that permits both administration to a wide, demographically diverse patient population and coadministration with many other therapeutic agents, including antiretroviral agents and supportive medications, without restrictions or dose adjustment. Data through 96 weeks of follow-up in three phase III studies, protocol 021 (STARTMRK) in treatment-naive patients, and protocols 018 (BENCHMRK-1) and 019 (BENCHMRK-2) in treatment-experienced patients, demonstrated the potent and durable antiretroviral and immunologic effects and the favorable long-term safety profile of raltegravir in both treatment-naive and treatment-experienced patients. Raltegravir represents an important addition to the current armamentarium for the treatment of HIV infection.
© 2011 New York Academy of Sciences.

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Year:  2011        PMID: 21434946     DOI: 10.1111/j.1749-6632.2011.05972.x

Source DB:  PubMed          Journal:  Ann N Y Acad Sci        ISSN: 0077-8923            Impact factor:   5.691


  24 in total

1.  Uncommon pathways of immune escape attenuate HIV-1 integrase replication capacity.

Authors:  Mark A Brockman; Denis R Chopera; Alex Olvera; Chanson J Brumme; Jennifer Sela; Tristan J Markle; Eric Martin; Jonathan M Carlson; Anh Q Le; Rachel McGovern; Peter K Cheung; Anthony D Kelleher; Heiko Jessen; Martin Markowitz; Eric Rosenberg; Nicole Frahm; Jorge Sanchez; Simon Mallal; Mina John; P Richard Harrigan; David Heckerman; Christian Brander; Bruce D Walker; Zabrina L Brumme
Journal:  J Virol       Date:  2012-04-11       Impact factor: 5.103

2.  Double Variational Binding--(SMILES) Conformational Analysis by Docking Mechanisms for Anti-HIV Pyrimidine Ligands.

Authors:  Mihai V Putz; Nicoleta A Dudaș; Adriana Isvoran
Journal:  Int J Mol Sci       Date:  2015-08-18       Impact factor: 5.923

3.  HIV Drug Resistance and the Advent of Integrase Inhibitors.

Authors:  Peter K Quashie; Thibault Mesplède; Mark A Wainberg
Journal:  Curr Infect Dis Rep       Date:  2013-02       Impact factor: 3.725

4.  Characterization of the R263K mutation in HIV-1 integrase that confers low-level resistance to the second-generation integrase strand transfer inhibitor dolutegravir.

Authors:  Peter K Quashie; Thibault Mesplède; Ying-Shan Han; Maureen Oliveira; Diane N Singhroy; Tamio Fujiwara; Mark R Underwood; Mark A Wainberg
Journal:  J Virol       Date:  2011-12-28       Impact factor: 5.103

5.  A Mos1 transposase in vivo assay to screen new HIV-1 integrase inhibitors.

Authors:  Mariana Cancian; Elgion L S Loreto
Journal:  Genetica       Date:  2018-01-19       Impact factor: 1.082

6.  Structure and Metal Binding Properties of a Poxvirus Resolvase.

Authors:  Huiguang Li; Young Hwang; Kay Perry; Frederic Bushman; Gregory D Van Duyne
Journal:  J Biol Chem       Date:  2016-03-24       Impact factor: 5.157

7.  Treatment with suboptimal doses of raltegravir leads to aberrant HIV-1 integrations.

Authors:  Janani Varadarajan; Mary Jane McWilliams; Stephen H Hughes
Journal:  Proc Natl Acad Sci U S A       Date:  2013-08-19       Impact factor: 11.205

Review 8.  A review of the toxicity of HIV medications.

Authors:  Asa M Margolis; Harry Heverling; Paul A Pham; Andrew Stolbach
Journal:  J Med Toxicol       Date:  2014-03

9.  Mucosal tissue pharmacokinetics of the integrase inhibitor raltegravir in a humanized mouse model: Implications for HIV pre-exposure prophylaxis.

Authors:  Milena Veselinovic; Kuo-Hsiung Yang; Craig Sykes; Leila Remling-Mulder; Angela D M Kashuba; Ramesh Akkina
Journal:  Virology       Date:  2016-01-06       Impact factor: 3.616

Review 10.  Raltegravir Once-Daily Tablet: A Review in HIV-1 Infection.

Authors:  Emma D Deeks
Journal:  Drugs       Date:  2017-10       Impact factor: 9.546

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