Roflumilast : the new orally active, selective phophodiesterase-4 inhibitor, for the treatment of COPD.

INTRODUCTION: Chronic obstructive pulmonary disease (COPD) is a progressive disease, the clinical course of which is punctuated by acute exacerbations. While long-acting bronchodilators and inhaled corticosteroids can reduce exacerbations, some patients do not respond adequately to these agents. Roflumilast , a novel orally active, once-daily phophodiesterase-4-selective inhibitor with anti-inflammatory properties, has been shown to reduce exacerbations and has been approved for the treatment of the subset of COPD patients with symptoms of chronic cough and sputum who have a history of exacerbations. AREAS COVERED: This article describes the pre-clinical and clinical pharmacology of roflumilast and analytically reviews the published data from the most relevant Phase-II and -III clinical trials evaluating its efficacy and safety. EXPERT OPINION: Roflumilast is the first drug specifically targeted to a particular subset of the heterogeneous population of COPD patients, namely those with chronic bronchitis in addition to severe airflow obstruction and an exacerbation history. Its efficacy in reducing exacerbations in patients already receiving a LABA or anticholinergic bronchodilator underscores its potential utility as an add-on agent in patients who continue to experience exacerbations despite treatment with other agents. Adverse events include gastrointestinal side effects, most commonly, as well as unexplained weight loss.