Roflumilast: a novel treatment for chronic obstructive pulmonary disease.

OBJECTIVE: To evaluate the efficacy and safety of roflumilast, approved by the Food and Drug Administration in February 2011 as a treatment to reduce the risk of chronic obstructive pulmonary disease (COPD) exacerbations in patients with severe COPD associated with chronic bronchitis and a history of exacerbations. DATA SOURCES: Literature was retrieved through MEDLINE (1977-December 2011), using the terms roflumilast and COPD. In addition, US government Web sites, including clinicaltrials.gov and fda.gov, were reviewed for pertinent information. Lastly, reference citations from publications identified were reviewed. STUDY SELECTION AND DATA EXTRACTION: All articles published in English identified from the data sources were evaluated. For the evaluation of clinical efficacy and safety, only Phase 3 studies were included. DATA SYNTHESIS: Limited treatment options are available for patients with moderate-to-severe COPD and repeated exacerbations. In 6 published Phase 3 trials to date, roflumilast 500 μg daily exhibited modest improvements in lung function, measured by pre- and postbronchodilator forced expiratory volume in 1 second, and reduced rates of moderate and severe exacerbations. Roflumilast was generally well tolerated, with diarrhea, nausea, and headache the most common adverse events seen in clinical trials, although it has also been associated with an increased risk of neuropsychiatric abnormalities and dose-limiting weight loss. The greatest benefit seen with roflumilast was among patients with moderate-to-severe COPD associated with chronic bronchitis along with a recent history of exacerbations. The benefits were demonstrated with monotherapy and in combination with long-acting β(2)-agonists or anticholinergic agents.
CONCLUSIONS: Despite its only modest benefits in improving lung function and reducing exacerbation rates, roflumilast serves as a safe and effective option in the treatment of COPD.