Roflumilast
IUPAC: N-( 3,5-dichloropyrid -4-yl ) - 3 - cyclopropylmethoxy -4- difluoromethoxybenzamide
R03DX07
PDE 4 inhibitors
Template: Infobox chemical / molecular formula search available
Roflumilast is a drug selected from the group of phosphodiesterase -4 inhibitors ( PDE -4 ) inhibitor, which is used for the treatment of chronic obstructive pulmonary disease ( COPD).
- 2.1 Chemical and pharmaceutical information
- 2.2 History
- 2.3 Trade name
Clinical information
Areas of application
Approved Areas of application
Roflumilast can be used for maintenance therapy in adult patients with severe COPD and chronic bronchitis and frequent deterioration of the disease ( called exacerbations ) in the past in addition to a treatment with a drug bronchodilatativen. Severe COPD in accordance with the authorization of roflumilast has a reduced volume in one second (FEV1) following use of a bronchodilatativen drug of less than 50 % of the setpoint.
Previous clinical studies have shown that the therapeutic window of PDE4 inhibitors for use in respiratory diseases due to dose-limiting side effects such as nausea, diarrhea and headache is limited. At low efficacy of the drug against COPD and asthma, these studies showed side effects in the gastrointestinal area. Especially in underweight patients with COPD, a possible further weight loss is critical. The cost - effectiveness analysis concluded that roflumilast would increase the cost of treatment for COPD, but follow-up costs in the further treatment of the patients could be saved.
Other possible areas of application
The drug has also been studied for the treatment of bronchial asthma. The results of these studies were, however, not yet published. According to the manufacturer to roflumilast 2008 was in the development of Phase I of the application areas atopic dermatitis and psoriasis.
Other Information
Chemical and pharmaceutical information
The following synthetic route was described in a patent granted in 1998:
History
The 2006 pharmaceutical division of Nycomed acquired the company Altana (formerly Byk Gulden ) was roflumilast in 2004 filed for approval in the EU for COPD, but in 2005 the application withdrawn after consultation with the European Medicines Agency. Shortly before Altana's former development partner Pfizer had finished working with Altana.
2009, the application for admission on the basis of positive results in four new clinical trials of Nycomed was re-submitted in the EU. 2010, the European Commission granted Nycomed, an EU approval for roflumilast. 2011 was the manufacturer has been licensed in the USA. A decision for Switzerland is still pending. Patent protection for roflumilast is already in the year 2014.
Trade names
Daxas ® ( EU), Daliresp ® ( USA)