Roflumilast for the treatment of chronic obstructive pulmonary disease

Abstract

Roflumilast is a new phosphodiesterase 4 inhibitor that has recently completed Phase III trials for the treatment of chronic obstructive pulmonary disease (COPD). Preclinical studies have shown that roflumilast targets inflammatory processes in COPD, with beneficial effects on tobacco-induced lung inflammation, lung fibrosis and remodeling, mucociliary malfunction and oxidative stress. Two recent, 1-year Phase III trials in COPD have shown that roflumilast reduces exacerbations and improves lung function in patients with COPD who have symptoms of chronic bronchitis and a history of exacerbations. Two other 6-month Phase III trials have demonstrated the beneficial effects of roflumilast in patients already receiving treatment with the long-acting β-agonist salmeterol or the long-acting muscarinic antagonist tiotropium. This article reviews the pharmacology, pharmacokinetics and preclinical pharmacology of roflumilast, the clinical studies supporting its use in COPD and its side-effect profile.

Keywords::

• anti-inflammatory
• chronic obstructive pulmonary disease
• cough and sputum
• exacerbations
• lung function
• phosphodiesterase 4 inhibitor
• roflumilast

Financial & competing interests disclosure

Klaus F Rabe has served as a consultant for, participated in advisory board meetings for, and has received lecture fees from AstraZeneca, Boehringer Ingelheim, Chiesi Farmaceutici, Pfizer, Novartis, Nycomed, Merck Sharp and Dohme, and GlaxoSmithKline; and has received research funding from Altana Pharma, Novartis, AstraZeneca, Boehringer Ingelheim, Roche and GlaxoSmithKline. The author has 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.

Editorial assistance with the preparation of the paper was provided by Jane Davies and Paul Wilmott of Caudex Medical Ltd, supported by Nycomed, Konstanz, Germany.