A proof-of-concept study of the effect of a novel H3-receptor antagonist in allergen-induced nasal congestion

J Allergy Clin Immunol. 2013 Oct;132(4):838-46.e1-6. doi: 10.1016/j.jaci.2013.05.001. Epub 2013 Jun 20.

Abstract

Background: H1-receptor inverse agonists are used effectively for treating several symptoms of allergic rhinitis, including nasal itching, rhinorrhea, and sneezing, although most agents are not very effective in treating nasal congestion.

Objective: This study evaluated the relative efficacy of a novel selective H3-receptor antagonist, JNJ-39220675, in preventing nasal congestion induced by exposing participants with ragweed allergy to ragweed allergen in an environmental exposure chamber model.

Methods: In this single-dose, patient-blind, double-dummy, placebo- and active-controlled, phase IIa cross-over study, 53 participants were randomized to JNJ-39220675 plus placebo, placebo plus pseudoephedrine, or only placebo. The primary efficacy assessment was change in nasal patency assessed by measuring the minimal cross-sectional area of the nasal cavity by using acoustic rhinometry. Secondary assessment included total nasal symptom scores (TNSSs) over the 8-hour environmental exposure chamber exposure period.

Results: Smaller decreases in minimal cross-sectional area were observed after JNJ-39220675 (least square mean difference, -0.126; P = .06) and pseudoephedrine (least square mean difference, -0.195; P = .004) treatment compared with placebo. The means for the baseline-adjusted area under the curve of TNSSs were significantly smaller for JNJ-39220675 (P = .0003) and pseudoephedrine (P = .04) versus placebo. JNJ-39220675 was significantly effective in treating all 4 individual symptoms (P ≤ .05 for all scores) compared with placebo, whereas pseudoephedrine only showed a trend for improvement in individual symptom scores of the TNSS. Insomnia was the most frequent adverse event (17.3%) associated with JNJ-39220675 treatment.

Conclusion: Prophylactic treatment with the H3-antagonist JNJ-39220675 relieved allergen-induced nasal congestion by using standard nasal symptom scoring; however, in contrast to pseudoephedrine, it only showed a trend for increasing nasal patency by using objective measures.

Keywords: AUC; AcR; Acoustic rhinometry; Allergic rhinitis; Area under the curve; CNS; Central nervous system; ECP; EEC; Environmental exposure chamber; Eosinophil cationic protein; H(3)-receptor antagonist; JNJ-39220675; LSM; Least square mean; MCA; Minimal cross-sectional area; SAR; Seasonal allergic rhinitis; TEAE; TNSS; Total nasal symptom score; Treatment-emergent adverse event; acoustic rhinometry; environmental exposure chamber; pseudoephedrine; total nasal symptom scores.

Publication types

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

MeSH terms

  • Adolescent
  • Adult
  • Aged
  • Allergens
  • Ambrosia / adverse effects
  • Ambrosia / immunology*
  • Azepines / administration & dosage
  • Azepines / therapeutic use*
  • Cross-Over Studies
  • Female
  • Histamine H3 Antagonists / administration & dosage
  • Histamine H3 Antagonists / therapeutic use*
  • Humans
  • Male
  • Middle Aged
  • Nasal Obstruction / drug therapy*
  • Pyridines / administration & dosage
  • Pyridines / therapeutic use*
  • Rhinitis, Allergic, Seasonal / drug therapy*
  • Rhinitis, Allergic, Seasonal / immunology
  • Rhinometry, Acoustic
  • Sneezing / immunology
  • Treatment Outcome
  • Young Adult

Substances

  • (4-cyclobutyl-(1,4)diazepan-1-yl)-(6-(4-fluorophenoxy)pyridin-3-yl)methanone
  • Allergens
  • Azepines
  • Histamine H3 Antagonists
  • Pyridines