Etravirine: new drug. Multidrug-resistant HIV: another option.
(1) After failure of several successive antiretroviral regimens, HIV-infected patients are normally treated with an optimised regimen based on resistance profiling, combined with tipranavir or darunavir and also an antiretroviral belonging to another class (maraviroc, enfuvirtide or raltegravir); (2) Etravirine is a non-nucleoside reverse transcriptase inhibitor first authorized for sale in the European Union in 2008; (3) Its clinical evaluation is based on two double-blind trials of identical design in a total of 1200 patients with multiple prior treatment failures. The patients received an optimised antiretroviral regimen including darunavir and ritonavir, plus either etravirine or placebo. After 24 weeks of treatment the proportion of patients whose viral load was below 50 copies/ml was higher in the etravirine group than in the placebo group (56.3% versus 33.6%), provided enfuvirtide was not introduced at the same time as etravirine; (4) The main known adverse effect of etravirine is potentially severe skin rash; nausea, vomiting and hypercholesterolaemia can also occur; (5) Etravirine has a high potential for drug-drug interactions, due to its inducing and inhibitory effects on various cytochrome P450 isoenzymes; (6) Etravirine is an additional option for HIV-infected patients with multiple treatment failure.
D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D044966:Anti-Retroviral Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D004311:Double-Blind Method; D017277:Drug Approval; D004347:Drug Interactions; D018432:Drug Resistance, Multiple / Q000187:drug effects*; D024882:Drug Resistance, Viral / Q000187:drug effects*; D005060:Europe; D015658:HIV Infections / Q000188:drug therapy*; D006801:Humans; D009570:Nitriles; D011724:Pyridazines / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D011743:Pyrimidines; D016032:Randomized Controlled Trials as Topic; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000627:therapeutic use*; D017211:Treatment Failure; D019562:Viral Load
D019380:Anti-HIV Agents; D044966:Anti-Retroviral Agents; D009570:Nitriles; D011724:Pyridazines; D011743:Pyrimidines; D018894:Reverse Transcriptase Inhibitors; C451734:etravirine