Roflumilast: systemic therapy for chronic obstructive pulmonary disease

Chronic obstructive pulmonary disease (COPD) is a leading cause of morbidity and mortality worldwide and is characterized by chronic inflammation in both the pulmonary compartment and the rest of the body. Phosphodiesterase type 4 is expressed in inflammatory cells involved in COPD; and the phosphodiesterase 4 inhibitor roflumilast has been extensively evaluated in patients with this disease. Results from two large-scale, well-controlled clinical trials that included patients with moderate-to-very severe COPD have shown that once-daily administration of roflumilast significantly improves forced expiratory volume in 1 s and decreases exacerbations, particularly in patients with severe disease. Roflumilast is well tolerated with a low incidence of gastrointestinal adverse events that declines with continued treatment. In contrast to inhaled medications, which are the mainstay of COPD therapy, a systemic therapy is more likely to reach targets outside the lungs (e.g., the cardiovascular system) and may have the potential to decrease the severity of common comorbidities in COPD patients.