DRUG EVALUATION Roflumilast: a novel phosphodiesterase 4 inhibitor for the treatment of inflammatory airways disease
نویسندگان
چکیده
10.2217/14750708.4.2.153 © 2 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.
منابع مشابه
Roflumilast Increases Bacterial Load and Dissemination in a Model of Pseudomononas Aeruginosa Airway Infection.
Exacerbations present a major clinical problem in many patients suffering from chronic obstructive pulmonary disease (COPD). Roflumilast, an inhibitor of phosphodiesterase 4, has shown beneficial effects in several clinical trials and is currently widely used to prevent exacerbations in severe COPD. Roflumilast has anti-inflammatory properties that may interfere with potentially important host ...
متن کاملPDE4-inhibitors: a novel, targeted therapy for obstructive airways disease.
Roflumilast is a selective once daily, oral phosphodiesterase-4 inhibitor that has recently been registered in all European Union countries as novel targeted therapy for COPD, while FDA approval for the USA market is expected in 2011. In several phase III trials in patients with moderate to (very) severe COPD and in patients with symptoms of chronic bronchitis and recurrent exacerbations, roflu...
متن کاملIn vivo efficacy in airway disease models of roflumilast, a novel orally active PDE4 inhibitor.
We have investigated the bronchodilator and anti-inflammatory properties of roflumilast (3-cyclopropylmethoxy-4-difluoromethoxy-N-[3,5-dichloropyrid-4-yl]-benzamide), a novel, highly potent, and selective phosphodiesterase 4 (PDE4) inhibitor. Additionally, we compared the effects of roflumilast and its N-oxide, the primary metabolite in vivo, with those of the PDE4 inhibitors piclamilast, rolip...
متن کاملNew approaches to the modulation of inflammatory processes in airway disease models: ATS 2001, May 18-23, San Francisco
The 97th American Thoracic Society meeting proved to be an excellent meeting, providing a wealth of new information on inflammatory diseases of the airways. Once again there appeared to be an increased emphasis on chronic obstructive pulmonary disease (COPD) with most of the major drug companies concentrating a large part of their efforts in this field. An assessment of the new British Thoracic...
متن کاملPhosphodiesterase 4 inhibitors augment the ability of formoterol to enhance glucocorticoid-dependent gene transcription in human airway epithelial cells: a novel mechanism for the clinical efficacy of roflumilast in severe chronic obstructive pulmonary disease.
Post-hoc analysis of two phase III clinical studies found that the phosphodiesterase 4 (PDE4) inhibitor, roflumilast, reduced exacerbation frequency in patients with severe chronic obstructive pulmonary disease (COPD) who were taking inhaled corticosteroids (ICS) concomitantly, whereas patients not taking ICS derived no such benefit. In contrast, in two different trials also performed in patien...
متن کامل