| Clinical data | |
|---|---|
| Trade names | Daxas, Daliresp, Zoryve, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a611034 |
| License data | |
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| Routes of administration | By mouth,topical |
| Drug class | PDE4 inhibitor |
| ATC code | |
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| Pharmacokinetic data | |
| Bioavailability | 79%[4][3][8][9] |
| Protein binding | 99%[4][3][8][9] |
| Metabolism | Hepatic viaCYP1A2 &CYP3A4[4][3][8][9] |
| Eliminationhalf-life | 17 hours (30 hours [active metabolite])[4][3][8][9] |
| Excretion | Urine (70%)[4][3][8][9] |
| Identifiers | |
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| CAS Number | |
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| ChemSpider |
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| UNII | |
| KEGG | |
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| PDB ligand | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.210.960 |
| Chemical and physical data | |
| Formula | C17H14Cl2F2N2O3 |
| Molar mass | 403.21 g·mol−1 |
| 3D model (JSmol) | |
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Roflumilast, sold under the brand nameDaxas among others, is a medication used for the treatment ofchronic obstructive pulmonary disease,[4]plaque psoriasis,[5]seborrheic dermatitis,[6] andatopic dermatitis.[5] It acts as a selective, long-actinginhibitor of the enzyme phosphodiesterase-4 (PDE-4).[10] It hasanti-inflammatory effects.[10][11][12]
It was approved for medical use in the European Union in 2010,[7] in the United States in 2011,[4] and in Canada in 2017.[1] It is available as ageneric medication.[13]
Roflumilast isindicated for the treatment of severe chronic obstructive pulmonary disease (COPD),[4] plaquepsoriasis,[5][14] seborrheic dermatitis,[6] and atopic dermatitis,[5][15]
It is used in the prevention of exacerbations (lung attacks) in severe chronic obstructive pulmonary disease (COPD).[3][4][7][8][9]
Common (1–10% incidence) adverse effects include diarrhea, weight loss, nausea, headache, insomnia, decreased appetite, abdominal pain, rhinitis, sinusitis, urinary tract infection, and depression.[4][3][8][9][16]
In June 2010, it was approved in the European Union for severe COPD associated with chronic bronchitis.[7][17] In February 2011, it gained FDA approval in the United States for reducing COPD exacerbations.[18][19]