Etravirine

Abstract

Etravirine is a next-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) that demonstrates potent in vitro activity against wild-type strains of HIV type 1 (HIV-1), as well as against numerous strains resistant to available NNRTIs. Furthermore, the potential for resistance to etravirine developing appears to be lower than for first-generation NNRTIs. In treatment-experienced patients infected with HIV-1 with NNRTI resistance, HIV-1 RNA levels of <50 copies/mL (primary endpoint) and <400 copies/mL were achieved by a significantly greater proportion of patients receiving etravirine 200 mg twice daily plus background therapy (BT) than placebo plus BT, according to the planned pooled and individual 24-week analyses of two large, well designed, continuing phase III trials (DUET-1 and DUET-2). In the pooled 24-week analysis, patients receiving etravirine plus BT achieved a significantly greater mean reduction in viral load from baseline and a significantly greater mean increase in CD4+ cell counts from baseline than patients receiving placebo plus BT. The pooled and individual findings of the DUET studies at 48 weeks indicate that the efficacy of etravirine is maintained with regard to these endpoints. In the DUET studies, etravirine was generally well tolerated in treatment-experienced patients infected with HIV-1, with a tolerability profile generally similar to that of placebo. Adverse events were mostly of mild or moderate severity.