AZD9668, a neutrophil elastase inhibitor, plus ongoing budesonide/formoterol in patients with COPD

Respir Med. 2012 Apr;106(4):531-9. doi: 10.1016/j.rmed.2011.10.020. Epub 2011 Dec 23.

Abstract

Background: Neutrophil elastase (NE) is implicated in chronic obstructive pulmonary disease (COPD). AZD9668 is a reversible and selective inhibitor of NE, well tolerated at doses of 60 mg bid during Phase I/IIa development.

Methods: This 12-week, randomised, double-blind, placebo-controlled, Phase IIb, trial (NCT01023516), investigated the efficacy and safety of AZD9668 (60 mg bid) versus placebo in patients with symptomatic COPD and a history of exacerbation receiving maintenance budesonide/formoterol. Primary outcome variable: forced expiratory volume in one second (FEV1). Secondary endpoints included: post-bronchodilator FEV1, pre- and post-bronchodilator forced vital capacity, FEV6, forced expiratory flow between 25% and 75% of vital capacity and inspiratory capacity; peak expiratory flow and FEV1 measured at home; EXAcerbations of Chronic pulmonary disease Tool and Breathlessness, Cough and Sputum Scores; St George's respiratory questionnaire for COPD (SGRQ-C) scores; exacerbations; and safety assessments.

Results: Six hundred and fifteen patients were randomised: placebo (302), AZD9668 60 mg bid (313). AZD9668 showed no effect on lung function: change in mean pre-bronchodilator FEV1 versus placebo was 0.01L (95% confidence interval: -0.03, 0.05; p=0.533). AZD9668 did not significantly improve respiratory signs and symptoms, SGRQ-C score or time to first exacerbation. Adverse events were similar for AZD9668 and placebo.

Conclusions: Three months' treatment with AZD9668 did not improve lung function, respiratory signs and symptoms or SGRQ-C score when added to budesonide/formoterol maintenance therapy in patients with COPD. In the absence of definitive biomarkers of short-term disease progression, further research is needed to determine the optimal duration of studies to evaluate NE inhibitors as disease-modifying agents.

Publication types

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

MeSH terms

  • Adult
  • Aged
  • Aged, 80 and over
  • Biomarkers / metabolism
  • Bronchodilator Agents / adverse effects
  • Bronchodilator Agents / therapeutic use*
  • Budesonide / adverse effects
  • Budesonide / therapeutic use*
  • Double-Blind Method
  • Drug Combinations
  • Drug Therapy, Combination
  • Ethanolamines / adverse effects
  • Ethanolamines / therapeutic use*
  • Female
  • Forced Expiratory Volume / drug effects
  • Formoterol Fumarate
  • Glucocorticoids / adverse effects
  • Glucocorticoids / therapeutic use
  • Humans
  • Leukocyte Elastase / antagonists & inhibitors
  • Male
  • Middle Aged
  • Pulmonary Disease, Chronic Obstructive / drug therapy*
  • Pulmonary Disease, Chronic Obstructive / physiopathology
  • Pyridones / adverse effects
  • Pyridones / therapeutic use*
  • Quality of Life
  • Respiratory Mechanics / drug effects
  • Sulfones / adverse effects
  • Sulfones / therapeutic use*
  • Treatment Outcome

Substances

  • Biomarkers
  • Bronchodilator Agents
  • Drug Combinations
  • Ethanolamines
  • Glucocorticoids
  • Pyridones
  • Sulfones
  • Budesonide
  • N-((5-(methanesulfonyl)pyridin-2-yl)methyl)-6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-2-oxo-1-(3-(trifluoromethyl)phenyl)-1,2-dihydropyridine-3-carboxamide
  • Leukocyte Elastase
  • Formoterol Fumarate

Associated data

  • ClinicalTrials.gov/NCT01023516