Roflumilast
| 240px | |
| Systematic (IUPAC) name | |
|---|---|
|
3-(cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide | |
| Clinical data | |
| Routes of administration | Oral |
| Identifiers | |
| 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".]] |
| Script error: No such module "collapsible list". | |
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
References
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- ↑ 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
- ↑ 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
- ↑ 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
- ↑ 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
- ↑ Spina D. PDE4 inhibitors: current status. British Journal of Pharmacology. 2008 Jul 28. PMID 18660825
- ↑ http://www.genengnews.com/gen-news-highlights/nycomed-s-anti-inflammatory-gains-approval-in-eu-for-copd/81243622/
- ↑ Amschler, H.; 1998, U.S. Patent 5,712,298.
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