[CAS NO. 162401-32-3]  Roflumilast

Animal studies with Roflumilast demonstrated that it reduced the accumulation of neutrophils in bronchoalveolar lavage fluid following short-term exposure of guinea pigs, mice or rats to tobacco smoke, and following exposure of rats to a combination of tobacco smoke and bacterial lipopolysaccharide, and abolished the lung parenchymal influx of inflammatory cells seen in rats exposed to tobacco smoke for 7 months ^[2] . Roflumilast blocks COPD progression in pIgR ^−/− mice. For these studies, 9-month-old WT or pIgR ^−/− mice are treated daily by oral gavage with 100 μg of Roflumilast (5 μg/g) or vehicle (4% methylcellulose, 1.3% PEG400) for 3 months and lungs are harvested at 12 months of age. Unlike pIgR ^−/− mice treated with vehicle, mice treated with Roflumilast had no progression of small airway wall remodelling after starting treatment. Strikingly, 12-month-old pIgR ^−/− mice treated with Roflumilast had reduced indices of emphysema compared with 9-month-old pIgR ^−/− mice, indicating that Roflumilast not only blocks progression of emphysema in this model but apparently facilitates some resolution of the emphysematous destruction of lung parenchyma ^[4] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.