Wild - Type and Reverse Transcriptase Inhibitor ( NNRTI ) , TMC 278 , a Next - Generation Nonnucleoside
نویسندگان
چکیده
Published Ahead of Print 23 November 2009. 10.1128/AAC.00986-09. 2010, 54(2):718. DOI: Antimicrob. Agents Chemother. Rimsky Van Craenenbroeck, Gaston Picchio and Laurence T. Béthune, Guenter Kraus, Katia Boven, Dirk Jochmans, Elke Hilde Azijn, Ilse Tirry, Johan Vingerhoets, Marie-Pierre de NNRTI-Resistant HIV-1 Active against Wild-Type and Reverse Transcriptase Inhibitor (NNRTI), TMC278, a Next-Generation Nonnucleoside
منابع مشابه
RAPID COMMUNICATION Minority Variants Associated with Transmitted and Acquired HIV-1 Nonnucleoside Reverse Transcriptase Inhibitor Resistance: Implications for the Use of Second-Generation Nonnucleoside Reverse Transcriptase Inhibitors
Objectives: K103N, the most common nonnucleoside reverse transcriptase inhibitor (NNRTI)–resistant mutation in patients with transmitted resistance and in patients receiving a failing NNRTIcontaining regimen, is fully susceptible to the new NNRTI, etravirine. Therefore, we sought to determine how often NNRTI-resistant mutations other than K103N occur as minority variants in plasma samples for w...
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INTRODUCTION Etravirine is a novel nonnucleoside reverse transcriptase inhibitor (NNRTI) specifically designed to suppress the replication of viruses resistant to the three currently approved NNRTIs efavirenz, nevirapine, and delavirdine. AIMS To assess the evidence for the place of etravirine in the treatment of HIV-1 infection. EVIDENCE REVIEW In combination with a ritonavir-boosted prote...
متن کاملShort-term randomized proof-of-principle trial of TMC278 in patients with HIV type-1 who have previously failed antiretroviral therapy.
BACKGROUND In vitro, TMC278, an investigational next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI), has shown activity against wild-type and NNRTI-resistant HIV type-1 (HIV-1) and a higher genetic barrier to the development of resistance than efavirenz or nevirapine. This Phase II open-label trial evaluated the short-term (7-day) antiviral activity of TMC278 administered at ...
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TMC278 is a diarylpyrimidine (DAPY) nonnucleoside reverse transcriptase inhibitor (NNRTI) that is highly effective in treating wild-type and drug-resistant HIV-1 infections in clinical trials at relatively low doses ( approximately 25-75 mg/day). We have determined the structure of wild-type HIV-1 RT complexed with TMC278 at 1.8 A resolution, using an RT crystal form engineered by systematic RT...
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Combination antiretroviral therapy has transformed the prognosis and life expectancy of HIV-1 infected individuals in resource-rich settings. British guidelines currently recommend the non-nucleoside reverse transcriptase inhibitor (NNRTI) efavirenz as part of first-line treatment in therapy-naive HIV-1 infected individuals. However, efavirenz is limited by its low genetic barrier to the develo...
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