Shifting paradigms: the resistance profile of etravirine.
The raised genetic barrier of etravirine relative to first-generation compounds indicates that it may now be possible to sequence drugs within the non-nucleoside reverse transcriptase inhibitor (NNRTI) class. Available evidence from clinical trials provides guidance for the use of etravirine in NNRTI-experienced persons, with sustained virological suppression demonstrated in combination with other active drugs in the background regimen, most commonly including a ritonavir-boosted protease inhibitor with or without enfuvirtide. Cross-resistance occurs however, and the drug is vulnerable to loss of activity in the absence of a supportive background regimen. In order to optimize the use of etravirine in clinical practice, it is important to understand how current predictors of virological activity in NNRTI-experienced persons were developed, how they can be applied, and the adjustments and improvements they require.
Geretti
Anna Maria
AM
Department of Virology, Royal Free Hospital and Royal Free and University College Medical School, Pond Street, London NW3 2QG, UK. a.geretti@medsch.ucl.ac.uk
D024882:Drug Resistance, Viral; D015658:HIV Infections / Q000188:drug therapy; D006801:Humans; D009570:Nitriles; D011724:Pyridazines / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*
D009570:Nitriles; D011724:Pyridazines; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; C451734:etravirine