Enfuvirtide

Drugs. 2003;63(24):2755-66; discussion 2767-8. doi: 10.2165/00003495-200363240-00005.

Abstract

Enfuvirtide is the first of a new class of drugs, the fusion inhibitors. It is a synthetic peptide which binds to the HIV glycoprotein 41 (gp41), blocking fusion of the viral and cellular membranes. HIV isolates with reduced susceptibility to enfuvirtide have been recovered from patients receiving enfuvirtide in combination with other antiretroviral agents. Enfuvirtide 90mg (subcutaneously, twice daily) in combination with optimised background (OB) antiretroviral therapy significantly reduced plasma HIV RNA levels compared with OB alone after treatment for 24 weeks in two randomised trials involving adults with advanced HIV infection. The antiviral efficacy of enfuvirtide was maintained through to 48 weeks. At 24 and 48 weeks, the increase from baseline in the CD4+ cell count was significantly greater for patients receiving enfuvirtide plus OB than for those receiving OB alone. Enfuvirtide 30 mg/m(2) or 60 mg/m(2) in combination with other antiretroviral agents reduced plasma HIV RNA levels and increased CD4+ cell counts in a small trial involving paediatric patients with HIV infection. Local injection-site reactions were common. Lymphadenopathy and pneumonia occurred more often in patients receiving enfuvirtide plus OB than in the control group. The incidence of most other events was similar in each group.

Publication types

  • Review

MeSH terms

  • Adolescent
  • Adult
  • Area Under Curve
  • Biological Availability
  • Cells, Cultured
  • Child
  • Cost-Benefit Analysis
  • Enfuvirtide
  • HIV Envelope Protein gp41* / adverse effects
  • HIV Envelope Protein gp41* / therapeutic use
  • HIV Fusion Inhibitors* / adverse effects
  • HIV Fusion Inhibitors* / pharmacokinetics
  • HIV Fusion Inhibitors* / therapeutic use
  • HIV Infections / drug therapy*
  • Half-Life
  • Humans
  • Peptide Fragments* / adverse effects
  • Peptide Fragments* / pharmacokinetics
  • Peptide Fragments* / therapeutic use
  • Quality-Adjusted Life Years
  • Randomized Controlled Trials as Topic

Substances

  • HIV Envelope Protein gp41
  • HIV Fusion Inhibitors
  • Peptide Fragments
  • Enfuvirtide