Formoterol fumarate + glycopyrrolate for the treatment of chronic obstructive pulmonary disease

ABSTRACT

Introduction: Chronic obstructive pulmonary disease (COPD) is characterized by a high disability and increasing mortality. Bronchodilators are the cornerstone of pharmacological treatment in COPD, while therapeutic optimization with an improvement in symptoms and compliance represent the actual goals. This has led to the development of devices that combine different classes of inhalatory drugs. Recently, a novel combination of the long acting antimuscarinic agent glycopyrronium bromide and the beta2-agonist formoterol fumarate has been developed in a metered dose inhaler delivery system.

Areas covered: The present article will discuss the current unmet needs in pharmacological therapy of COPD, will then briefly cover the pharmacokinetic and pharmacodynamic characteristics of the formoterol/glycopyrronium fixed dose combination and present the novel delivery system based on engineered microparticles and the co-suspension technology. Finally, efficacy and safety results of phase I, II and III trials will be reviewed.

Expert commentary: The novel combination therapy of formoterol/glycopyrronium is the first available as a metered dose inhaler and proved to have a good efficacy and safety profile compared to monocomponents and tiotropium. Although still limited, data from phase III trials provide good evidence to consider it a valid option in the pharmacological management of patients with COPD.

KEYWORDS:

• Formoterol fumarate
• glycopyrronium bromide
• metered dose inhaler
• chronic obstructive pulmonary disease
• porous particles
• bronchodilation
• fixed dose combination

Information Resources

Although so far the published literature on the topic is very narrow, for further study and research purposes the Authors suggest the following readings:

1. Vehring R, Lechuga-Ballesteros D, Joshi V, Noga B, Dwivedi SK. Cosuspensions of microcrystals and engineered microparticles for uniform and efficient delivery of respiratory therapeutics from pressurized metered dose inhalers. Langmuir. 28, 15015−15023 (2012).

2. Calzetta L, Matera MG, Cazzola M. Pharmacological interaction between LABAs and LAMAs in the airways: optimizing synergy. Eur J of Pharm. 761, 168–173 (2015).

3. Cazzola M, Molimard M. The scientific rationale for combining long-acting beta2-agonists and muscarinic antagonists in COPD. Pulm Pharmacol Ther. 23(4), 257-67 (2010).

4. http://www.accessdata.fda.gov/scripts/cder/drugsatfda/index.cfm?fuseaction=Search.DrugDetails

5. http://www.ukmi.nhs.uk/applications/ndo/record_view_open.asp?newDrugID=5371

Declaration of interest

P. Santus has received financial support for research from Pfizer, Almirall, Chiesi Farmaceutici, and AirLiquide. He has received honoraria for lectures at national meetings from Chiesi Farmaceutici, Novartis, Zambon Italia, AstraZeneca, Almirall, GlaxoSmithKline, Boehringer Ingelheim, Menarini, and Malesci Guidotti. He has served as consultant for Zambon Italia, AstraZeneca, Novartis, Chiesi Farmaceutici, Malesci Guidotti and Boehringer Ingelheim. The author states that no funding sources influenced the preparation of the current manuscript or in collection, interpretation, and presentation of data. G.F. Sferrazza Papa received speaking fees from GSK and Malesci-Guidotti. F. Di Marco has received honoraria for lectures at national and international meetings from Almirall, AstraZeneca, Boehringer Ingelheim, Chiesi Farmaceutici, Dompé, Guidotti/Malesci, GlaxoSmithKline, Menarini, Novartis, and Zambon. He has served as consultant for AstraZeneca, Chiesi Farmaceutici, Novartis, and Zambon. He has received financial support for research from Novartis. The author states that no funding sources influenced the preparation of the current manuscript or in collection, interpretation, and presentation of data. D. Radovanovic, S. Aliberti, V. Valenti and M. Mantero have no competing interests to declare. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Additional information

Funding

This paper was not funded.