Phosphodiesterase type 4 inhibitors for asthma: a real breakthrough or just expensive theophylline? American College of Allergy, Asthma, & Immunology

摘要

Theophylline is the archetypal nonselective phosphodiesterase inhibitor that has been extensively used for the treatment of asthma, despite having a relatively poor therapeutic ratio, potential drug interactions, and a need for therapeutic monitoring. It is a hybrid drug that exhibits bronchodilator and anti-inflammatory activity, depending on the dose. There has been recent interest in using lower doses of theophylline for its anti-inflammatory activity, especially as add-on therapy to inhaled corticosteroids.1 Roflumilast will be the first commercially available selective phosphodiesterase type 4 (PDE4) inhibitor for use in asthma, administered as a once-daily tablet, with claims of better efficacy, safety, and toler-ability than theophylline, although it is likely to be considerably more expensive. There remains an unmet need for a once-daily orally active nonsteroidal anti-inflammatory agent for use as monotherapy as an alternative to inhaled corticosteroids because there is still the perception that patients prefer pills. In this respect, it is likely that comparisons will be made to the leukotriene receptor antagonist montelukast, another once-daily oral anti-inflammatory tablet.