Abstract

Roflumilast: a novel phosphodiesterase 4 inhibitor for the treatment of inflammatory airways disease

Author(s): Victoria Boswell-Smith and Clive P Page

Isoenzyme phosphodiesterase 4 inhibitors are novel therapeutic agents in late clinical development for the treatment of chronic obstructive pulmonary disease and asthma, both diseases with significant unmet treatment needs. Roflumilast is one such isoenzyme phosphodiesterase 4 inhibitor that is undergoing Phase III clinical development. It is an orally active compound that owes part of its efficacy and long duration of action to its primary metabolite roflumilast N-oxide. Preclinical and clinical studies have indicated that its probable mechanism of action is anti-inflammatory, although it may also have the ability to relax airway smooth muscle. Its relatively low incidence of class-associated gastrointestinal events and long duration of action may account for its improved therapeutic profile over other agents in its class.