Etravirine for the treatment of HIV/AIDS

Introduction: Etravirine (TMC125) is an orally administered second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that is approved in treatment-experienced patients as addition to an optimized background therapy (OBT). Areas covered: A Medline search was conducted of Phase II - IV clinical trials, as well as a review of abstracts from major HIV and infectious disease conferences from 2010 - 2013, involving etravirine. Expert opinion: Etravirine is a well-tolerated NNRTI with a good safety profile and a higher genetic barrier for resistance compared to first-generation NNRTIs. Rash is a potential side effect but remains mostly mild to moderate. The necessity of taking it twice daily with food (200 mg bid.), potential pharmacokinetic interactions and low concentrations in the central nervous system (CNS) represent limitations. The efficacy of once daily etravirine (400 mg qid.) and the use in treatment modification/simplification strategies requires further research. Despite its favorable profile, etravirine is currently not sufficiently investigated nor approved for use in treatment-naive patients which should be balanced against its potential as a backup NNRTI and the broad cross-resistance conferred by etravirine failure to other NNRTIs. Etravirine should be avoided following treatment failure with regimens containing rilpivirine, another second-generation NNRTI.