Two Phase II randomized trials on the CRTh2 antagonist AZD1981 in adults with asthma

Drug Des Devel Ther. 2016 Aug 31:10:2759-70. doi: 10.2147/DDDT.S105142. eCollection 2016.

Abstract

Background: Chemoattractant receptor-homologous molecule expressed on T helper type 2 (Th2) cell (CRTh2) receptor antagonists is being investigated for asthma.

Objectives: The aim of this study was to assess the effects of the CRTh2 receptor antagonist, AZD1981 (with/without inhaled corticosteroids [ICSs]), on lung function and asthma control.

Patients and methods: Adults aged 18-60 years were enrolled in two randomized, placebo-controlled, parallel-group trials (protocol number: D9830C00003 [study 1, n=209] and protocol number: D9830C00004 [study 2, n=510]). In study 1, patients with stable asthma (forced expiratory volume in 1 second [FEV1]: 65%-110%) were withdrawn from ICS (<400 µg/d) and randomized to AZD1981 1,000 mg twice daily (bid) or placebo. In study 2, patients with uncontrolled asthma (FEV1: 40%-85%) despite ICS therapy (≥500 µg/d) were randomized to 50 mg, 400 mg, or 1,000 mg bid AZD1981 or placebo. The primary efficacy variable for both trials was the change in morning peak expiratory flow after 4 weeks of treatment. Secondary variables included Asthma Control Questionnaire (ACQ-5) scores, FEV1 assessments, safety, and tolerability. In study 2, efficacy was also assessed according to atopic status.

Results: Following 4 weeks of treatment, there was a nonsignificant increase in morning peak expiratory flow on AZD1981 1,000 mg bid (9.5 L/min vs placebo, P=0.086 [study 1] and 12 L/min vs placebo, P=0.16 [study 2]). In study 2, all doses of AZD1981 provided significant improvements in ACQ-5 scores (0.26-0.3 units vs placebo, P=0.010-0.022); however, there was no dose-response relationship. Improved ACQ-5 scores and FEV1 were observed in the majority of atopic patients treated with AZD1981. AZD1981 was well tolerated across treatment groups.

Conclusion: Further research may be warranted in atopic patients to fully evaluate the clinical efficacy of AZD1981.

Keywords: CRTh2 receptor; Phase II; Th2 cells; efficacy; prostaglandin D2; respiratory.

Publication types

  • Clinical Trial, Phase II
  • Multicenter Study
  • Randomized Controlled Trial

MeSH terms

  • Acetates / administration & dosage
  • Acetates / pharmacology*
  • Acetates / therapeutic use*
  • Administration, Oral
  • Adolescent
  • Adult
  • Asthma / drug therapy*
  • Double-Blind Method
  • Female
  • Humans
  • Indoles / administration & dosage
  • Indoles / pharmacology*
  • Indoles / therapeutic use*
  • Male
  • Middle Aged
  • Receptors, Immunologic / antagonists & inhibitors*
  • Receptors, Prostaglandin / antagonists & inhibitors*
  • Young Adult

Substances

  • Acetates
  • Indoles
  • Receptors, Immunologic
  • Receptors, Prostaglandin
  • AZD1981
  • prostaglandin D2 receptor