A phase 2a study of toreforant, a histamine H4 receptor antagonist, in eosinophilic asthma

Ann Allergy Asthma Immunol. 2018 Nov;121(5):568-574. doi: 10.1016/j.anai.2018.08.001. Epub 2018 Aug 11.

Abstract

Background: Data from preclinical and clinical studies support the evaluation of histamine 4 receptor antagonists in the treatment of asthma. Toreforant is a selective histamine 4 receptor antagonist that could be effective in patients with eosinophilic asthma.

Objective: To evaluate the efficacy and safety of toreforant in patients with eosinophilic, persistent asthma that was inadequately controlled despite current treatment.

Methods: In this phase 2a, multicenter, randomized, double-blinded, parallel-group, placebo-controlled, proof-of-concept study, 162 eligible patients were randomized (1:1) to placebo or 30 mg of toreforant once daily through week 24 and followed for 4 weeks. The primary end point was change from baseline in pre-bronchodilator percent-predicted forced expiratory volume in 1 second at week 16. Secondary end points included change from baseline at week 16 in postbronchodilator percent-predicted forced expiratory volume in 1 second, Asthma Control Questionnaire scores, weekly averages of Daytime and Nighttime Asthma Diary Symptom Scores, and weekly average of number of puffs in a day that rescue medication was used.

Results: There was no significant difference between groups in pre-bronchodilator percent-predicted forced expiratory volume in 1 second at week 16 (difference in least-square means -0.19%; 95% confidence interval -3.01 to 2.64; P = .90). Similarly, there were no significant differences between groups at week 16 in changes from baseline in the secondary end points (P ≥ .30). Toreforant was generally well tolerated. No deaths or serious adverse events were reported at any time point.

Conclusion: Toreforant, at the dose tested, failed to provide therapeutic benefit in this population of patients with uncontrolled, eosinophilic, persistent asthma.

Trial registration: ClinicalTrials.gov, NCT01823016.

Publication types

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

MeSH terms

  • Asthma / drug therapy*
  • Bronchodilator Agents / therapeutic use
  • Double-Blind Method
  • Female
  • Forced Expiratory Volume
  • Histamine Antagonists / adverse effects
  • Histamine Antagonists / therapeutic use*
  • Humans
  • Male
  • Middle Aged
  • Proof of Concept Study
  • Pulmonary Eosinophilia / drug therapy*
  • Receptors, Histamine H4 / antagonists & inhibitors*
  • Treatment Outcome
  • United States

Substances

  • Bronchodilator Agents
  • Histamine Antagonists
  • Receptors, Histamine H4

Associated data

  • ClinicalTrials.gov/NCT01823016