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      Profile of etravirine for the treatment of HIV infection

        1 , 2

      Therapeutics and Clinical Risk Management

      Dove Medical Press

      etravirine, review, efficacy, resistance, pharmacology

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          Abstract

          Etravirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) with the advantages of in vitro potency against many strains of virus resistant to efavirenz and nevirapine, as well as a higher genetic barrier to resistance. Etravirine is indicated for use in treatment-experienced patients, and the approved dose in adults is 200 mg twice daily. Etravirine should be administered after a meal as bioavailability is significantly reduced when taken in the fasting state. Etravirine is a substrate of CYP3A4, CYP2C9, CYP2C19, and uridine diphosphate glucuronyltransferase, and induces CYP3A4, weakly inhibits CYP2C9 and moderately inhibits CYP2C19. Etravirine may be coadministered with nucleoside/tide reverse transcriptase inhibitors, raltegravir and boosted darunavir, lopinavir, and saquinavir without dosage adjustment. Etravirine should not be given with other NNRTIs, unboosted protease inhibitors, and atazanavir/ritonavir, tipranavir/ritonavir, and fosamprenavir/ritonavir due to unfavorable drug interactions. In randomized, controlled trials, twice daily etravirine combined with darunavir/ritonavir plus optimized background therapy demonstrated better efficacy compared to darunavir/ritonavir plus optimized background therapy alone in treatment-experienced populations out to 96 weeks follow-up. The main etravirine-associated toxicity is mild to moderate self-limiting rash, although severe and sometimes fatal hypersensitivity reactions have been reported. Etravirine offers a potent sequencing option after the development of resistance to first-line NNRTIs, and is a welcome addition to this established drug class.

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          Author and article information

          Journal
          Ther Clin Risk Manag
          Therapeutics and Clinical Risk Management
          Therapeutics and Clinical Risk Management
          Dove Medical Press
          1176-6336
          1178-203X
          2010
          2010
          2 February 2010
          : 6
          : 49-58
          Affiliations
          [1 ]Toronto General Hospital, Toronto, ON, Canada;
          [2 ]Division of Infectious Diseases, Wayne State University, Detroit, Michigan, USA
          Author notes
          Correspondence: Rodger D MacArthur, Professor of Medicine, Division of Infectious Diseases, Wayne State University, Detroit, Michigan, USA 48201, Tel +1 313-993-0921, Fax +1 313-745-3638, Email rmacarthur@ 123456med.wayne.edu
          Article
          tcrm-6-049
          2817788
          20169036
          © 2010 Tseng and MacArthur, publisher and licensee Dove Medical Press Ltd.

          This is an Open Access article which permits unrestricted noncommercial use, provided the original work is properly cited.

          Categories
          Review

          Medicine

          efficacy, etravirine, pharmacology, review, resistance

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