2010年7月，欧盟获准用于用于严重的慢性阻塞性肺病(COPD)和慢性支气管炎，商品名为Daxas；2011年2月28日，美国FDA批准其用于严重的COPD治疗，商品名为Daliresp。由此成为十数年来在全球范围内获准用于慢性阻塞性肺病治疗的第一个新型口服药物。
该药品已经证明能够以一种崭新的作用方式抑制与 (COPD) 有关的炎症。作为一天口服一次的药片，罗氟司特不仅是严重 COPD 新疗法中的第一种药品，而且是第一种面向 COPD 患者的口服抗炎药。其独特的性质，有助于更好地治疗慢性阻塞性肺病患者：当与支气管扩张剂联合用药治疗最重度慢性阻塞性肺病患者时，罗氟司特能够提供进一步减少症状和疾病恶化率的额外益处，由此成为靶向特定表型慢性阻塞性肺病即存在与长期咳嗽和多痰相关的严重气流受限且具反复疾病恶化史患者的第一个药物。
剂型及规格
片剂，0.5 mg/片。
适应症
治疗有严重慢性阻塞性肺病（COPD）伴有慢性支气管炎和加重史的患者的咳嗽及黏液过多症。

Daliresp (Roflumilast), Treatment to Reduce COPD, United States of America
Daliresp (Roflumilast) is an oral tablet that is proved to reduce the risk of exacerbations in patients suffering from severe chronic obstructive pulmonary disease (COPD). The drug has been developed by Nycomed.
Marketed as Daxas in the European markets, Daliresp was approved by the US FDA in March 2011. The European marketing approval for Daxas was received in 2010.
Daliresp will be available in US markets in the second quarter of 2011. It will be marketed by Nycomed's partner Forest Laboratories.
Chronic obstructive pulmonary disease
COPD is a progressive and irreversible lung disease which narrows the airways, thus causing respiratory problems. Breathlessness, chronic cough and congestion of phlegm in the lungs are the major symptoms associated with COPD.
These symptoms worsen further to cause exacerbation that lasts for weeks, requiring immediate hospitalisation and intensive medication. If left unattended, exacerbation can result in failure of lungs and could even be fatal.
Daliresp
Daliresp is an oral tablet to be taken once daily. It is the first and the only selective phosphodiesterase-4 (PDE4) inhibitor approved by the FDA.
Although the mechanism of action of the drug is not known, it is believed that the therapeutic action is exerted in patients by effects related to increase in intracellular cyclic adenosine metaphosphate (cAMP) in lung cells.
Clinical trials
Daliresp was eva luated in eight clinical trials conducted in a randomised double-blind, controlled parallel group. Around 9,394 patients of 40 years and above were enrolled in these trials.
Trials 1 and 2 were placebo-controlled dose selection trials of six months duration. These trials were conducted on 1,929 patients to eva luate the efficacy of Daliresp 250mcg and 500mcg tablet once daily. The median age of the enrolled patients was 63 years, associated with severe COPD in the range of 30%-80%.
Of the total randomised population, 751 patients were administered with 250mcg Daliresp and 724 with 500mcg. The 500mcg was selected over 250mcg based on the nominal improvement in lung function.
Trials 3, 4, 5 and 6 were once-year placebo-controlled trials. These were conducted to eva luate the efficacy of the treatment in patients who reported to have less than 50% of COPD severity and faced exacerbations. The enrolled patients were in the median age of 64 years.
Trials 3 and 4 included patients with less than 50% severity with chronic bronchitis and smoking history of 10 years. Trial 3 enrolled 1,176 patients of whom 567 were tested with Daliresp. Trial 4 was conducted on 1,514 patients of whom 760 were treated with Daliresp.
Both these trials failed to show significant reduction in the exacerbations in majority of the population. However, exploratory studies revealed that the treatment showed better response in reduction of COPD exacerbation in a small section of the population. Therefore further trials 5 and 6 were conducted on patients associated with chronic bronchitis, at least one COPD exacerbation in the previous year and a 20 pack year of smoking history.
Trial 5 had enrolled a total of 1,525 patients of whom 765 were administered Daliresp. Trial 6 had a total of 1,571 patients enrolled of whom 772 were tested with Daliresp. In both the trials, 500mcg Daliresp once daily confirmed that the treatment of Daliresp had resulted in a significant reduction of moderate or severe exacerbations compared to placebo. These two trials proved the safety and supported the use of Daliresp in the reduction of exacerbations of COPD.
Trials 7 and 8 were six months trails conducted to eva luate the efficacy of Daliresp as an add-on therapy to a bronchodilator. Patients enrolled for these trials were with moderate to severe COPD and of 65 years of median age.
The trials were conducted on patients with moderate to severe (40%-70% predicted) COPD without any chronic bronchitis or history of exacerbations. The results indicated that the drug showed significant response in reducing the exacerbations.