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PubMed · 16499282

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

Lawrence R Boone
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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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AnimalsAnti-HIV AgentsAzepinesClinical Trials as TopicDrug DesignDrug Evaluation, PreclinicalDrug Resistance, ViralHIV InfectionsHIV Reverse TranscriptaseHIV-1HumansMutationNitrilesPyridazinesPyrimidinesReverse Transcriptase InhibitorsRilpivirineJournal ArticleReview

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Lawrence R Boone. 2006. Next-generation HIV-1 non-nucleoside reverse transcriptase inhibitors.. https://pubmed.ncbi.nlm.nih.gov/16499282/

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