IL-4 receptor polymorphisms predict reduction in asthma exacerbations during response to an anti-IL-4 receptor α antagonist

J Allergy Clin Immunol. 2012 Aug;130(2):516-22.e4. doi: 10.1016/j.jaci.2012.03.030. Epub 2012 Apr 26.

Abstract

Background: This is the first large pharmacogenetic investigation of the inflammatory IL-4/IL-13 pathway in patients with moderate-to-severe asthma. We analyzed genomic DNA from participants in a 12-week placebo-controlled efficacy trial of pitrakinra (1, 3, or 10 mg twice daily), a novel IL-4/IL-13 pathway antagonist (Clinicaltrials.govNCT00801853).

Objectives: The primary hypothesis for this analysis is that amino acid changes in the 3' end of the IL-4 receptor α gene (IL4RA) or closely proximal variants would predict reductions in asthma exacerbations for subjects randomized to pitrakinra therapy.

Methods: Nineteen IL4RA single nucleotide polymorphisms (SNPs) were tested in 407 non-Hispanic white subjects for association with the primary clinical end point of asthma exacerbations and changes in secondary end points for asthma symptom scores.

Results: The most consistent pharmacogenetic associations were observed for the correlated tagging SNPs rs8832 and rs1029489 in the IL4RA 3' untranslated and proximal regions, respectively. Subjects homozygous for the rs8832 common G allele randomized to pitrakinra (placebo group nonsignificant) had decreased asthma exacerbations and decreased nocturnal awakenings and activities limited by asthma. There was also a significant pitrakinra dose-response relationship (placebo/1 mg/3 mg/10 mg) for exacerbations in subjects homozygous for the common allele in rs1029489 (P = .005) and rs8832 (P= .009) and the intronic SNPs rs3024585, rs3024622, and rs4787956 (P = .03).

Conclusion: This study demonstrates a significant pharmacogenetic interaction between anti-IL-4 receptor α therapy and IL4RA gene variation, identifying an asthma subgroup that is more responsive to therapy with this antagonist.

Publication types

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

MeSH terms

  • 3' Untranslated Regions / genetics
  • 3' Untranslated Regions / immunology
  • Adult
  • Alleles
  • Anti-Asthmatic Agents / administration & dosage
  • Anti-Asthmatic Agents / therapeutic use*
  • Asthma / drug therapy*
  • Asthma / genetics
  • Asthma / immunology
  • Dose-Response Relationship, Drug
  • Double-Blind Method
  • Drug Administration Schedule
  • Female
  • Homozygote
  • Humans
  • Interleukin-13 / genetics
  • Interleukin-13 / immunology
  • Interleukin-4 / administration & dosage
  • Interleukin-4 / genetics
  • Interleukin-4 / immunology
  • Interleukin-4 / therapeutic use*
  • Interleukin-4 Receptor alpha Subunit / antagonists & inhibitors*
  • Interleukin-4 Receptor alpha Subunit / genetics
  • Interleukin-4 Receptor alpha Subunit / metabolism
  • Male
  • Middle Aged
  • Pharmacogenetics
  • Placebos
  • Polymorphism, Single Nucleotide / genetics*
  • Polymorphism, Single Nucleotide / immunology
  • Severity of Illness Index
  • Signal Transduction / genetics
  • Signal Transduction / immunology
  • Treatment Outcome

Substances

  • 3' Untranslated Regions
  • Anti-Asthmatic Agents
  • IL4R protein, human
  • Interleukin-13
  • Interleukin-4 Receptor alpha Subunit
  • Placebos
  • pitrakinra
  • Interleukin-4

Associated data

  • ClinicalTrials.gov/NCT00801853