Etravirine

Is the first second-generation NNRTI. It is active against many of the strains of HIV that are resistant to the first-generation NNRTIs. HIV strains with the common K103N resistance mutation to the first generation of NNRTIs are fully susceptible to etravirine. Following oral administration, etravirine is well distributed, and bioavailability is enhanced when taken with a high-fat meal. Although it has a half-life of approximately 40 hours, it is indicated for twice-daily dosing. Etravirine is extensively metabolized to inactive products. Because etravirine is a potent inducer of CYP450, the doses of CYP450 substrates may need to be increased when given with etravirine. Rash is the most common side effect.nausea, and diarrhea it is pregnancy category B. Etravirine is indicated for HIV treatment–experienced, multidrug-resistant adult patients who have evidence of ongoing viral replication.Elevations in serum cholesterol, triglycerides, and transaminase levels may occur. Etravirine is a substrate as well as an inducer of CYP3A4 and also inhibits CYP2C9 and CYP2C19 and may be involved in significant drug interactions.