title: A review of the safety and tolerability profile of the next-generation NNRTI etravirine.
abstract: The next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI) etravirine (TMC125) has demonstrated durable virologic efficacy in clinical trials involving >1000 treatment-experienced, NNRTI-resistant, HIV-1-infected patients. In this clinical safety review, we show etravirine to be well tolerated with a proven safety record. The nature and magnitude of adverse events observed during treatment suggest that etravirine may offer improved tolerability over existing antiretrovirals, including NNRTIs. Notably, adverse events reported with etravirine treatment are generally mild to moderate in severity. Rash has been shown to occur with a higher incidence in etravirine-treated patients versus placebo, but cases are generally mild to moderate, occur within the first few weeks, and resolve with continued use. In addition, the rate of adverse event-related discontinuations is low with etravirine. In summary, the safety and tolerability profile of etravirine, combined with its virologic efficacy, suggest that the drug may be a valuable option for treatment-experienced patients with HIV-1 infection.
authors.affiliation: Instituto de Pesquisa Clinica Evandro Chagas-Fiocruz, Rio de Janeiro, Brazil. gbeatriz@ipec.fiocruz.br
authors.forename: Beatriz
authors.initials: B
authors.lastname: Grinsztejn
authors.forename: Giovanni
authors.initials: G
authors.lastname: Di Perri
authors.forename: William
authors.initials: W
authors.lastname: Towner
authors.forename: Brian
authors.initials: B
authors.lastname: Woodfall
authors.forename: Goedele
authors.initials: G
authors.lastname: De Smedt
authors.forename: Monika
authors.initials: M
authors.lastname: Peeters
mesh_terms: D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000009:adverse effects*; D064420:Drug-Related Side Effects and Adverse Reactions; D005076:Exanthema / Q000139:chemically induced; D015658:HIV Infections / Q000188:drug therapy*; D006801:Humans; D009570:Nitriles; D011724:Pyridazines / Q000008:administration & dosage / Q000009:adverse effects*; D011743:Pyrimidines; D013997:Time Factors; D016896:Treatment Outcome; D028761:Withholding Treatment / Q000706:statistics & numerical data
chemical_list: D019380:Anti-HIV Agents; D009570:Nitriles; D011724:Pyridazines; D011743:Pyrimidines; C451734:etravirine