Roflumilast
- US DailyMed: Roflumilast
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- AU: B3
administration
- R03DX07 (WHO) D05AX06 (WHO)
- 3-(Cyclopropylmethoxy)-N-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
- 162401-32-3 N
- 449193
- 6962
- DB01656 Y
- 395793 N
- 0P6C6ZOP5U
- D05744
- CHEBI:47657 N
- ChEMBL193240 N
- ROF (PDBe, RCSB PDB)
- DTXSID8044123
- Interactive image
- C1CC1COC2=C(C=CC(=C2)C(=O)NC3=C(C=NC=C3Cl)Cl)OC(F)F
- InChI=1S/C17H14Cl2F2N2O3/c18-11-6-22-7-12(19)15(11)23-16(24)10-3-4-13(26-17(20)21)14(5-10)25-8-9-1-2-9/h3-7,9,17H,1-2,8H2,(H,22,23,24) N
- Key:MNDBXUUTURYVHR-UHFFFAOYSA-N N
Roflumilast, sold under the brand name Daxas among others, is a medication that acts as a selective, long-acting inhibitor of the enzyme phosphodiesterase-4 (PDE-4). It has anti-inflammatory effects and is used as an orally administered drug for the treatment of inflammatory conditions of the lungs such as chronic obstructive pulmonary disease (COPD).[7][8][9][10]
In June 2010, it was approved in the European Union for severe COPD associated with chronic bronchitis.[4][11] In February 2011, it gained FDA approval in the United States for reducing COPD exacerbations.[12][13] It is available as a generic medication.[14]
Medical uses
Roflumilast is indicated for the treatment of severe chronic obstructive pulmonary disease (COPD)[2] and for the treatment of plaque psoriasis.[3][15]
It is used in the prevention of exacerbations (lung attacks) in severe chronic obstructive pulmonary disease (COPD).[1][2][4][5][6]
Adverse effects
Common (1–10% incidence) adverse effects include diarrhea, weight loss, nausea, headache, insomnia, decreased appetite, abdominal pain, rhinitis, sinusitis, urinary tract infection, and depression.[2][1][5][6][16]
References
- ^ a b c d e f g h "Daxas 250 micrograms tablets - Summary of Product Characteristics (SmPC)". (emc). 11 June 2020. Archived from the original on 19 September 2020. Retrieved 28 September 2020.
- ^ a b c d e f g h i "Daliresp- roflumilast tablet". DailyMed. 12 March 2020. Archived from the original on 25 March 2021. Retrieved 28 September 2020.
- ^ a b "Zoryve- roflumilast cream". DailyMed. 16 August 2022. Archived from the original on 21 January 2023. Retrieved 21 January 2023.
- ^ a b c "Daxas EPAR". European Medicines Agency. 17 September 2018. Archived from the original on 12 August 2020. Retrieved 28 September 2020.
- ^ a b c d e f g "Daliresp : EPAR - Product Information" (PDF). European Medicines Agency. Takeda GmbH. 26 September 2013. Archived (PDF) from the original on 26 June 2016. Retrieved 18 November 2013.
- ^ a b c d e f g "roflumilast (Rx) - Daliresp". Medscape Reference. WebMD. Archived from the original on 12 September 2017. Retrieved 18 November 2013.
- ^ Boswell-Smith V, Spina D (2007). "PDE4 inhibitors as potential therapeutic agents in the treatment of COPD-focus on roflumilast". International Journal of Chronic Obstructive Pulmonary Disease. 2 (2): 121–9. PMC 2695611. PMID 18044684.
- ^ Herbert C, Hettiaratchi A, Webb DC, Thomas PS, Foster PS, Kumar RK (May 2008). "Suppression of cytokine expression by roflumilast and dexamethasone in a model of chronic asthma". Clinical and Experimental Allergy. 38 (5): 847–56. doi:10.1111/j.1365-2222.2008.02950.x. PMID 18307529. S2CID 19050454.
- ^ Hohlfeld JM, Schoenfeld K, Lavae-Mokhtari M, Schaumann F, Mueller M, Bredenbroeker D, et al. (August 2008). "Roflumilast attenuates pulmonary inflammation upon segmental endotoxin challenge in healthy subjects: a randomized placebo-controlled trial" (PDF). Pulmonary Pharmacology & Therapeutics. 21 (4): 616–23. doi:10.1016/j.pupt.2008.02.002. PMID 18374614. Archived (PDF) from the original on 28 August 2019. Retrieved 24 June 2019.
- ^ Field SK (May 2008). "Roflumilast: an oral, once-daily selective PDE-4 inhibitor for the management of COPD and asthma". Expert Opinion on Investigational Drugs. 17 (5): 811–8. doi:10.1517/13543784.17.5.811. PMID 18447606. S2CID 73241684.
- ^ ""Nycomed's Anti-Inflammatory Gains Approval in EU for COPD"". Archived from the original on 24 August 2017. Retrieved 10 July 2010.
- ^ "Drug Approval Package: Daliresp Tablets (roflumilast) NDA #022522". U.S. Food and Drug Administration (FDA). 24 December 1999. Archived from the original on 27 October 2020. Retrieved 28 September 2020.
- ^ "FDA approves new drug to treat chronic obstructive pulmonary disease" (Press release). U.S. Food and Drug Administration (FDA). 1 March 2011. Archived from the original on 18 January 2017. Retrieved 16 December 2019.
- ^ "2022 First Generic Drug Approvals". U.S. Food and Drug Administration (FDA). 3 March 2023. Archived from the original on 30 June 2023. Retrieved 30 June 2023.
- ^ "FDA Approves Arcutis' Zoryve (Roflumilast) Cream 0.3% For the Treatment of Plaque Psoriasis in Individuals Age 12 and Older" (Press release). Arcutis Biotherapeutics. 29 July 2022. Archived from the original on 1 August 2022. Retrieved 1 August 2022 – via GlobeNewswire.
- ^ Spina D (October 2008). "PDE4 inhibitors: current status". British Journal of Pharmacology. 155 (3): 308–15. doi:10.1038/bjp.2008.307. PMC 2567892. PMID 18660825.
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