Literature DB >> 19249947

Etravirine and rilpivirine: nonnucleoside reverse transcriptase inhibitors with activity against human immunodeficiency virus type 1 strains resistant to previous nonnucleoside agents.

Patricia Pecora Fulco1, Ian R McNicholl.   

Abstract

Etravirine and rilpivirine are two new nonnucleoside reverse transcriptase inhibitors (NNRTIs) that have the distinct advantage of being able to be used in patients with exposure to previous NNRTIs (e.g., nevirapine or efavirenz). Etravirine was approved by the United States Food and Drug Administration to be used twice/day in treatment-experienced patients infected with the human immunodeficiency virus. The approval was based on phase III clinical studies in which 61% of etravirine-treated patients reached an undetectable viral load of less than 50 copies/ml compared with 40% of patients who received the optimized background regimen. Etravirine was well tolerated with a self-limiting skin rash being the most common toxicity, reported in 19% of patients. Rilpivirine, a once-daily NNRTI, is entering phase III studies; the drug appears to be effective against a broad range of NNRTI-resistant viruses including etravirine-resistant strains.

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Year:  2009        PMID: 19249947     DOI: 10.1592/phco.29.3.281

Source DB:  PubMed          Journal:  Pharmacotherapy        ISSN: 0277-0008            Impact factor:   4.705


  11 in total

1.  Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.

Authors:  Lian-Qi Sun; Bingjie Qin; Li Huang; Keduo Qian; Chin-Ho Chen; Kuo-Hsiung Lee; Lan Xie
Journal:  Bioorg Med Chem Lett       Date:  2012-02-24       Impact factor: 2.823

2.  Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

Authors:  Xingtao Tian; Bingjie Qin; Zhiyuan Wu; Xiaofeng Wang; Hong Lu; Susan L Morris-Natschke; Chin Ho Chen; Shibo Jiang; Kuo-Hsiung Lee; Lan Xie
Journal:  J Med Chem       Date:  2010-11-04       Impact factor: 7.446

3.  In vitro and in vivo activities of AIC292, a novel HIV-1 nonnucleoside reverse transcriptase inhibitor.

Authors:  Steffen Wildum; Daniela Paulsen; Kai Thede; Helga Ruebsamen-Schaeff; Holger Zimmermann
Journal:  Antimicrob Agents Chemother       Date:  2013-08-19       Impact factor: 5.191

4.  Etravirine: a guide to its use in treatment-experienced pediatric patients with HIV-1 infection in the US.

Authors:  Katherine A Lyseng-Williamson
Journal:  Paediatr Drugs       Date:  2012-10-01       Impact factor: 3.022

5.  Development and validation of a simple and isocratic reversed-phase HPLC method for the determination of rilpivirine from tablets, nanoparticles and HeLa cell lysates.

Authors:  Abhijit A Date; Annemarie Shibata; Patrick Bruck; Christopher J Destache
Journal:  Biomed Chromatogr       Date:  2014-10-09       Impact factor: 1.902

6.  Structural and Preclinical Studies of Computationally Designed Non-Nucleoside Reverse Transcriptase Inhibitors for Treating HIV infection.

Authors:  Shalley N Kudalkar; Jagadish Beloor; Albert H Chan; Won-Gil Lee; William L Jorgensen; Priti Kumar; Karen S Anderson
Journal:  Mol Pharmacol       Date:  2017-02-06       Impact factor: 4.436

Review 7.  Etravirine: a review of its use in the management of treatment-experienced patients with HIV-1 infection.

Authors:  Jamie D Croxtall
Journal:  Drugs       Date:  2012-04-16       Impact factor: 9.546

8.  Emtricitabine/rilpivirine/tenofovir disoproxil fumarate single-tablet regimen: a guide to its use in HIV-1 infection.

Authors:  Katherine A Lyseng-Williamson; Lesley J Scott
Journal:  Clin Drug Investig       Date:  2012-10-01       Impact factor: 2.859

9.  Design, synthesis, and preclinical evaluations of novel 4-substituted 1,5-diarylanilines as potent HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) drug candidates.

Authors:  Lian-Qi Sun; Lei Zhu; Keduo Qian; Bingjie Qin; Li Huang; Chin Ho Chen; Kuo-Hsiung Lee; Lan Xie
Journal:  J Med Chem       Date:  2012-08-10       Impact factor: 7.446

10.  Pharmacotherapy of pediatric and adolescent HIV infection.

Authors:  Susan J Schuval
Journal:  Ther Clin Risk Manag       Date:  2009-06-22       Impact factor: 2.423

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