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Systematic (IUPAC) name
Clinical data
Routes of
CAS Number 162401-32-3
ATC code R03DX07 (WHO)
PubChem CID 449193
Chemical data
Formula C17H14Cl2F2N2O3
Molar mass 403.207 g/mol[[Script error: No such module "String".]]
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Roflumilast (trade name Daxas) is a drug which acts as a selective, long-acting inhibitor of the enzyme PDE-4. It has antiinflammatory effects and is under development as an orally administered drug for the treatment of inflammatory conditions of the lungs such as asthma, and chronic obstructive pulmonary disease (COPD).[1][2][3][4] While roflumilast was found to be effective in clinical trials, it produced several dose-limiting side effects including nausea, diarrhoea and headache, and development is continuing in an attempt to minimise the incidence of side effects while retaining clinical efficacy.[5]

In June 2010 it was approved in the EU for severe COPD associated with chronic bronchitis.[6]

Chemical synthesis

Chemical synthesis:[7]


See also


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  1. Boswell-Smith V, Spina D. PDE4 inhibitors as potential therapeutic agents in the treatment of COPD-focus on roflumilast. International Journal of Chronic Obstructive Pulmonary Disease. 2007;2(2):121-9. PMID 18044684
  2. Herbert C, Hettiaratchi A, Webb DC, Thomas PS, Foster PS, Kumar RK. Suppression of cytokine expression by roflumilast and dexamethasone in a model of chronic asthma. Clinical and Experimental Allergy. 2008 May;38(5):847-56. PMID 18307529
  3. Hohlfeld JM, Schoenfeld K, Lavae-Mokhtari M, Schaumann F, Mueller M, Bredenbroeker D, Krug N, Hermann R. Roflumilast attenuates pulmonary inflammation upon segmental endotoxin challenge in healthy subjects: a randomized placebo-controlled trial. Pulmonary Pharmacology and Therapeutics. 2008 Aug;21(4):616-23. PMID 18374614
  4. Field SK. Roflumilast: an oral, once-daily selective PDE-4 inhibitor for the management of COPD and asthma. Expert Opinion on Investigational Drugs. 2008 May;17(5):811-8. PMID 18447606
  5. Spina D. PDE4 inhibitors: current status. British Journal of Pharmacology. 2008 Jul 28. PMID 18660825
  7. Amschler, H.; 1998, U.S. Patent 5,712,298.