Etravirine for HIV-I: addressing the limitations of the nonnucleoside reverse transcriptase inhibitor class.
Etravirine (ETR) is a second-generation nonnucleoside reverse transcriptase inhibitor (NNRTI) specifically designed for treatment-experienced patients infected with HIV-1. Its unique strength over other, older agents in the NNRTI class is its higher genetic barrier to resistance, allowing it to be used effectively in patients with limited treatment options. The arrival of ETR in the market has made sequential NNRTI therapy possible for the first time in the history of HIV treatment, as it can maintain virologic activity in the presence of certain (and sometimes multiple) NNRTI mutations. Although ETR has demonstrated efficacy in treatment-experienced and NNRTI-resistant patients in large trials, further analyses on its resistance profile are ongoing. As new data emerge on the weighting of ETR's resistance-associated mutations (RAMs), investigators and clinicians will no doubt be able to further characterize its specific place in the HIV treatment armamentarium.
Grennan
Troy
T
Department of Infectious Diseases, McMaster University, St Joseph's Healthcare F506-1, Hamilton, Ontario, Canada.
Walmsley
Sharon
S
D044966:Anti-Retroviral Agents / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D001682:Biological Availability; D001798:Blood Proteins / Q000378:metabolism; D002986:Clinical Trials as Topic; D004347:Drug Interactions; D024882:Drug Resistance, Viral; D015658:HIV Infections / Q000188:drug therapy*; D015497:HIV-1 / Q000187:drug effects*; D006801:Humans; D009570:Nitriles; D011485:Protein Binding; D011724:Pyridazines / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use
D044966:Anti-Retroviral Agents; D001798:Blood Proteins; D009570:Nitriles; D011724:Pyridazines; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; C451734:etravirine