Curr Opin Investig Drugs. 2006 Feb;7(2):128-35.

Next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors.

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GlaxoSmithKline, Discovery Virology, Research Triangle Park, NC 27709, USA. larry.r.boone@gsk.com

Abstract

This review discusses the desired attributes of a next-generation HIV-1 non-nucleoside reverse transcriptase inhibitor (NNRTI) and highlights the properties of compounds currently or recently in clinical development. TMC-125 is currently in phase III clinical trials and on track to become the first NNRTI suitable for use in NNRTI-experienced patients. TMC-278 is structurally related to TMC-125, but is more potent in vitro and has pharmacokinetics suitable for once-daily administration. It is currently undergoing phase II clinical trials. BILR-355 BS, a dipyridodiazepinone compound, is in early phase II clinical trials. It requires ritonavir as a booster and has reduced inhibitory activity against several key NNRTI-resistant HIV-1 strains. Development of the NNRTIs capravirine and GW-695634 has been discontinued because of lack of efficacy and safety issues, respectively.

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Next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors.

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