The discovery and development of aclidinium bromide for the treatment of chronic obstructive pulmonary disease

M Malerba, A Radaeli, G Santini, J Morjaria, Nadia Mores, C Mondino, Giuseppe Macis, Paolo Montuschi*

*Corresponding author

Research output: Contribution to journalArticlepeer-review

1 Citation (Scopus)


Bronchodilators, including long-acting muscarinic receptor antagonists (LAMAs), are a mainstay of the pharmacological treatment of chronic obstructive pulmonary disease (COPD). LAMAs act as bronchodilators principally by antagonizing airway smooth muscle cells M3 muscarinic receptors. Aclidinium bromide is a twice-daily LAMA which was developed to improve on the efficacy and/or safety of previous LAMAs. Area covered: Herein, the authors present the pharmacotherapeutic role of aclidinium in COPD and point out unmet need in this research area. The following aspects are covered: a) the discovery and medicinal chemistry of aclidinium bromide; b) an overview of the market; c) its mechanism of action; d) its pharmacokinetic/pharmacodynamic profile derived from pre-clinical studies; e) the clinical studies which led to its licensing; f) the evidence from meta-analyses; g) the aclidinium/formoterol fixed dose combination for COPD and h) priorities in this area of research. Expert opinion: Aclidinium bromide has the pharmacological properties, safety and efficacy profile and inhaler characteristics which makes it a valuable therapeutic option for pharmacological management of patients with COPD. Due to its rapid biotransformation into inactive metabolites, aclidinium is potentially one of the safest LAMAs. Further head-to-head randomized clinical trials are required to define efficacy and safety of aclidinium when compared to once-daily LAMAs. The clinical relevance of airway anti-remodeling effects of aclidinium has to be defined
Original languageEnglish
Pages (from-to)563-577
Number of pages15
JournalExpert Opinion on Drug Discovery
Publication statusPublished - 2018


  • aclidinium bromide
  • bronchodilators
  • chronic obstructive pulmonary disease
  • long-acting muscarinic receptor antagonists
  • pharmacotherapy


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