Neurological and psychiatric tolerability of rilpivirine (TMC278) vs. efavirenz in treatment-naïve, HIV-1-infected patients at 48 weeks

HIV Med. 2013 Aug;14(7):391-400. doi: 10.1111/hiv.12012. Epub 2013 Jan 9.

Abstract

Objectives: The aim of the study was to compare the neuropsychiatric safety and tolerability of rilpivirine (TMC278) vs. efavirenz in a preplanned pooled analysis of data from the ECHO and THRIVE studies which compared the safety and efficacy of the two drugs in HIV-1 infected treatment naïve adults.

Methods: ECHO and THRIVE were randomized, double-blind, double-dummy, 96-week, international, phase 3 trials comparing the efficacy, safety and tolerability of rilpivirine 25 mg vs. efavirenz 600 mg once daily in combination with two background nucleoside/tide reverse transcriptase inhibitors. Safety and tolerability analyses were conducted when all patients had received at least 48 weeks of treatment or discontinued earlier. Differences between treatments in the incidence of neurological and psychiatric adverse events (AEs) of interest were assessed in preplanned statistical analyses using Fisher's exact test.

Results: At the time of the week 48 analysis, the cumulative incidences in the rilpivirine vs. efavirenz groups of any grade 2-4 treatment-related AEs and of discontinuation because of AEs were 16% vs. 31% (P<0.0001) and 3% vs. 8% (P=0.0005), respectively. The incidence of treatment-related neuropsychiatric AEs was 27% vs. 48%, respectively (P<0.0001). The incidence of treatment-related neurological AEs of interest was 17% vs. 38% (P<0.0001), and that of treatment-related psychiatric AEs of interest was 15% vs. 23% (P=0.0002). Dizziness and abnormal dreams/nightmares occurred significantly less frequently with rilpivirine vs. efavirenz (P<0.01). In both groups, patients with prior neuropsychiatric history tended to report more neuropsychiatric AEs but rates remained lower for rilpivirine than for efavirenz.

Conclusions: Rilpivirine was associated with fewer neurological and psychiatric AEs of interest than efavirenz over 48 weeks in treatment-naïve, HIV-1-infected adults.

Keywords: adverse events; central nervous system; efavirenz; neuropsychiatric; rilpivirine; safety.

Publication types

  • Clinical Trial, Phase III
  • Comparative Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Aged, 80 and over
  • Alkynes
  • Anti-HIV Agents / administration & dosage*
  • Anti-HIV Agents / pharmacology
  • Anti-HIV Agents / therapeutic use
  • Benzoxazines / administration & dosage
  • Benzoxazines / adverse effects*
  • Benzoxazines / therapeutic use
  • Cyclopropanes
  • HIV Infections / drug therapy*
  • HIV Infections / psychology
  • HIV Infections / virology
  • HIV-1* / drug effects
  • HIV-1* / physiology
  • Humans
  • Mental Disorders / chemically induced*
  • Middle Aged
  • Nervous System Diseases / chemically induced*
  • Nitriles / administration & dosage
  • Nitriles / adverse effects*
  • Nitriles / therapeutic use
  • Pyrimidines / administration & dosage
  • Pyrimidines / adverse effects*
  • Pyrimidines / therapeutic use
  • Rilpivirine
  • Viral Load / physiology
  • Young Adult

Substances

  • Alkynes
  • Anti-HIV Agents
  • Benzoxazines
  • Cyclopropanes
  • Nitriles
  • Pyrimidines
  • Rilpivirine
  • efavirenz