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Resumen
Etravirina (ETR) es un inhibidor de la transcriptasa inversa no análogo de nucleósidos (ITINAN), con potente y amplia actividad in vitro frente al virus de la inmunodeficiencia humana 1 y a virus con resistencias a ITINAN, lo que permite el uso secuencial de esta familia. La potencia, eficacia y seguridad están demostradas en pacientes multitratados, pero se dispone de pocos datos en primeras líneas de tratamiento antirretroviral (TAR), sin estar definido su papel en fases iniciales. La presencia de resistencias a ITINAN primarias y adquiridas durante la primera línea de tratamiento es cada vez más frecuente. Gracias a su barrera genética y eficacia, ETR puede formar parte de un segundo régimen de TAR en pacientes que han fallado en un primer régimen. En fases iniciales, los efectos adversos siguen siendo el motivo principal por el que se modifica el TAR. ETR se ha mostrado segura y con buena tolerabilidad. No presenta efectos adversos en el sistema nervioso central y tiene un buen perfil hepático, lipídico y gastrointestinal. El efecto adverso más frecuente es el exantema, efecto adverso común al resto de ITINAN. Su buen perfil de tolerabilidad lo convierte en un fármaco que se debe considerar en la configuración de un nuevo tratamiento en cambios por tolerabilidad. Las características de ETR, posibilidad de administración 1 vez al día, posibilidad de administrar disuelta en agua y no interacción con metadona, hacen que sea un fármaco especialmente atractivo en primeras líneas de tratamiento y en pacientes a los que se les ha atribuido mala adherencia, como son los usuarios de drogas por vía parenteral en tratamiento con metadona.
Palabras clave:
VIH
Etravirina
Resistencias VIH
Tolerabilidad
Metadona
Abstract
Etravirine (ETR) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) with a potent and broad in vitro spectrum of activity against HIV-1 and viruses with NNRTI resistances, allowing sequential use of drugs of this family. The potency, efficacy and safety of etravirine have been demonstrated in multi-treated patients, but few data are available on first-line antiretroviral therapy (ART) and the role of this drug in initial treatment phases has not been defined. The presence of primary NNRTI resistances and those acquired during first-line therapy is increasingly frequent. Due to its genetic barrier and efficacy, ETR can form part of a second-line ART regimen in patients with failure to a first-line regimen. In the initial phases, adverse effects continue to be the main reason for modifying ART. ETR has demonstrated safety and tolerability, with no central nervous system adverse effects and a good liver, lipid and gastrointestinal safety profile. As with the other NNRTIs, the most common adverse effect is rash. Because of ETR good tolerability profile, this drug can be considered when a new treatment is required due to adverse effects. Because of the characteristics of ETR the possibility of once-daily administration and dissolution in water, as well as the absence of drug-drug interactions with methadone this drug is especially attractive as a firstline therapy and in patients with poor adherence, such as intravenous drug users receiving methadone treatment.
Keywords:
HIV
Etravirine
Resistances HIV
Tolerability
Methadone
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