Anti-IL-5 (mepolizumab) therapy reduces eosinophil activation ex vivo and increases IL-5 and IL-5 receptor levels

J Allergy Clin Immunol. 2008 Jun;121(6):1473-83, 1483.e1-4. doi: 10.1016/j.jaci.2008.02.033. Epub 2008 Apr 14.

Abstract

Background: Anti-IL-5 might be a useful therapeutic agent for eosinophilic disorders, yet its immunologic consequences have not been well characterized.

Objective: We sought to characterize the hematologic and immunologic effects of anti-IL-5 in human subjects.

Methods: The effects of 3-month infusions of mepolizumab were assessed in 25 patients with a variety of eosinophilic syndromes. Samples with increased IL-5 levels after therapy were analyzed by using size exclusion filtration. Immunoreactive IL-5 fraction and plasma samples were subsequently precipitated with saturating concentrations of protein A/G.

Results: Twenty-three patients responded to anti-IL-5 therapy with a decrease in blood eosinophil counts and a reduced percentage of CCR3(+) cells by 20- and 13-fold, respectively (P < .0001). Responsiveness was not related to the levels of baseline plasma IL-5 or the presence of FIP1L1-PDGFRA fusion gene. Persistently decreased blood eosinophilia remained for 3 months after final infusion in 76% of subjects. Therapy was associated with a large increase in blood IL-5 levels, likely because of a circulating IL-5/mepolizumab complex precipitated with protein A/G, a significant increase in eosinophil IL-5 receptor alpha expression, and increased percentage of CD4(+) and CD8(+) cells producing intracellular IL-5 (P < .05). Additionally, anti-IL-5 therapy decreased eotaxin-stimulated eosinophil shape change ex vivo.

Conclusions: Anti-IL-5 therapy induces a dramatic and sustained decrease in blood eosinophilia (including CCR3(+) cells), decreased eosinophil activation, and increased circulating levels of IL-5 in a variety of eosinophilic disorders. Increased levels of IL-5 receptor alpha and lymphocyte IL-5 production after anti-IL-5 therapy suggest an endogenous IL-5 autoregulatory pathway.

Publication types

  • Clinical Trial, Phase I
  • Clinical Trial, Phase II
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Adolescent
  • Adult
  • Antibodies, Monoclonal / therapeutic use*
  • Antibodies, Monoclonal, Humanized
  • Cytokines / biosynthesis
  • Enzyme-Linked Immunosorbent Assay
  • Eosinophilia / blood
  • Eosinophilia / drug therapy*
  • Eosinophils / drug effects*
  • Female
  • Flow Cytometry
  • Fluorescent Antibody Technique
  • Humans
  • Interleukin-5 / antagonists & inhibitors
  • Interleukin-5 / blood*
  • Male
  • Middle Aged
  • Receptors, Interleukin-5 / blood
  • Receptors, Interleukin-5 / drug effects*
  • T-Lymphocyte Subsets / drug effects
  • T-Lymphocytes / drug effects

Substances

  • Antibodies, Monoclonal
  • Antibodies, Monoclonal, Humanized
  • Cytokines
  • Interleukin-5
  • Receptors, Interleukin-5
  • mepolizumab