{{위키데이터 속성 추적}}
{{Infobox drug
| Verifiedfields = changed
| Watchedfields = changed
| verifiedrevid = 464383196
| image = Roflumilast structure.svg
| width = 240
| alt = 
| image2 = Roflumilast ball-and-stick model.png
| width2 = 240
| alt2 = 
| caption = 

<!-- Clinical data -->
| pronounce = 
| tradename = Daxas, Daliresp, Zoryve 등
| Drugs.com = {{drugs.com|monograph|roflumilast}}
| MedlinePlus = a611034
| DailyMedID = Roflumilast
| pregnancy_AU = B3
| pregnancy_AU_comment = 
| pregnancy_category = 
| routes_of_administration = [[경구 투여]], [[국소 투여]]
| class = 
| ATCvet = 
| ATC_prefix = R03
| ATC_suffix = DX07
| ATC_supplemental = {{ATC|D05|AX06}}

<!-- Legal status -->
| legal_AU = S4
| legal_AU_comment = 
| legal_BR = <!-- OTC, A1, A2, A3, B1, B2, C1, C2, C3, C4, C5, D1, D2, E, F -->
| legal_BR_comment = 
| legal_CA = Rx-only
| legal_CA_comment = 
| legal_DE = <!-- Anlage I, II, III or Unscheduled -->
| legal_DE_comment = 
| legal_NZ = <!-- Class A, B, C -->
| legal_NZ_comment = 
| legal_UK = POM
| legal_UK_comment =<ref name="Daxas SmPC" />
| legal_US = Rx-only
| legal_US_comment =<ref name="Daliresp FDA label" /><ref name="Zoryve FDA label" />
| legal_EU = Rx-only
| legal_EU_comment =<ref name="Daxas EPAR" />
| legal_UN = <!-- N I, II, III, IV / P I, II, III, IV -->
| legal_UN_comment = 
| legal_status = <!-- For countries not listed above -->

<!-- Pharmacokinetic data -->
| bioavailability = 79%<ref name = "Daliresp FDA label"/><ref name = "Daxas SmPC"/><ref name = EMA/><ref name = MSR/>
| protein_bound = 99%<ref name = "Daliresp FDA label"/><ref name = "Daxas SmPC"/><ref name = EMA/><ref name = MSR/>
| metabolism = [[간]] ([[CYP1A2]] & [[CYP3A4]])<ref name = "Daliresp FDA label"/><ref name = "Daxas SmPC"/><ref name = EMA/><ref name = MSR/>
| metabolites = 
| onset = 
| elimination_half-life = 17시간 (활성 대사산물은 30시간)<ref name = "Daliresp FDA label"/><ref name = "Daxas SmPC"/><ref name = EMA/><ref name = MSR/>
| duration_of_action = 
| excretion = [[소변]] (70%)<ref name = "Daliresp FDA label"/><ref name = "Daxas SmPC"/><ref name = EMA/><ref name = MSR/>

<!-- Identifiers -->
| CAS_number_Ref = {{cascite|changed|??}}
| CAS_number = 162401-32-3
| CAS_supplemental = 
| PubChem = 449193
| IUPHAR_ligand = 6962
| DrugBank_Ref = {{drugbankcite|correct|drugbank}}
| DrugBank = DB01656
| ChemSpiderID_Ref = {{chemspidercite|changed|chemspider}}
| ChemSpiderID = 395793
| UNII_Ref = {{fdacite|correct|FDA}}
| UNII = 0P6C6ZOP5U
| KEGG_Ref = 
| KEGG = D05744
| ChEBI_Ref = {{ebicite|changed|EBI}}
| ChEBI = 47657
| ChEMBL_Ref = {{ebicite|changed|EBI}}
| ChEMBL = 193240
| NIAID_ChemDB = 
| PDB_ligand = ROF
| synonyms = 

<!-- Chemical and physical data -->
| IUPAC_name = 3-(Cyclopropylmethoxy)-''N''-(3,5-dichloropyridin-4-yl)-4-(difluoromethoxy)benzamide
| C=17 | H=14 | Cl=2 | F=2 | N=2 | O=3
| SMILES = C1CC1COC2=C(C=CC(=C2)C(=O)NC3=C(C=NC=C3Cl)Cl)OC(F)F
| StdInChI_Ref = {{stdinchicite|changed|chemspider}}
| StdInChI = 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)
| StdInChI_comment = 
| StdInChIKey_Ref = {{stdinchicite|changed|chemspider}}
| StdInChIKey = MNDBXUUTURYVHR-UHFFFAOYSA-N
| density = 
| density_notes = 
| melting_point = 
| melting_high = 
| melting_notes = 
| boiling_point = 
| boiling_notes = 
| solubility = 
| sol_units = 
| specific_rotation = 
}}

'''로플루밀라스트'''(roflumilast)는 '''닥사스'''(Daxas), '''달리레스프'''(Daliresp) 등의 상품명으로 판매되는 약제로, 선택적 지속성 [[포스포다이에스터레이스-4 억제제]](PDE4 억제제)로 작용한다. 항염증 효과가 있어 [[만성 폐쇄성 폐질환]](COPD) 같은 폐의 염증성 질환 치료를 위해 [[경구 투여]]한다.<ref name="pmid18044684">{{저널 인용| vauthors = Boswell-Smith V, Spina D | title = PDE4 inhibitors as potential therapeutic agents in the treatment of COPD-focus on roflumilast | journal = International Journal of Chronic Obstructive Pulmonary Disease | volume = 2 | issue = 2 | pages = 121–9 | year = 2007 | pmid = 18044684 | pmc = 2695611 | url = }}</ref><ref name="pmid18307529">{{저널 인용| vauthors = Herbert C, Hettiaratchi A, Webb DC, Thomas PS, Foster PS, Kumar RK | title = Suppression of cytokine expression by roflumilast and dexamethasone in a model of chronic asthma | journal = Clinical and Experimental Allergy | volume = 38 | issue = 5 | pages = 847–56 | date = May 2008 | pmid = 18307529 | doi = 10.1111/j.1365-2222.2008.02950.x | s2cid = 19050454 }}</ref><ref name="pmid18374614">{{저널 인용| vauthors = Hohlfeld JM, Schoenfeld K, Lavae-Mokhtari M, Schaumann F, Mueller M, Bredenbroeker D, Krug N, Hermann R | display-authors = 6 | title = Roflumilast attenuates pulmonary inflammation upon segmental endotoxin challenge in healthy subjects: a randomized placebo-controlled trial | journal = Pulmonary Pharmacology & Therapeutics | volume = 21 | issue = 4 | pages = 616–23 | date = August 2008 | pmid = 18374614 | doi = 10.1016/j.pupt.2008.02.002 | url = https://hal.archives-ouvertes.fr/hal-00499153/file/PEER_stage2_10.1016%252Fj.pupt.2008.02.002.pdf | access-date = 24 June 2019 | archive-date = 28 August 2019 | archive-url = https://web.archive.org/web/20190828080728/https://hal.archives-ouvertes.fr/hal-00499153/file/PEER_stage2_10.1016%25252Fj.pupt.2008.02.002.pdf | url-status = live }}</ref><ref name="pmid18447606">{{저널 인용| vauthors = Field SK | title = Roflumilast: an oral, once-daily selective PDE-4 inhibitor for the management of COPD and asthma | journal = Expert Opinion on Investigational Drugs | volume = 17 | issue = 5 | pages = 811–8 | date = May 2008 | pmid = 18447606 | doi = 10.1517/13543784.17.5.811 | s2cid = 73241684 }}</ref>

2010년 6월, 만성 기관지염을 동반한 중증 COPD를 [[적응증]]으로 [[유럽연합]]에서 사용을 승인했다.<ref name="Daxas EPAR">{{웹 인용| title=Daxas EPAR | website=[[European Medicines Agency]] | date=17 September 2018 | url=https://www.ema.europa.eu/en/medicines/human/EPAR/daxas | access-date=28 September 2020 | archive-date=12 August 2020 | archive-url=https://web.archive.org/web/20200812193907/https://www.ema.europa.eu/en/medicines/human/EPAR/daxas | url-status=live }}</ref><ref>{{웹 인용|url=http://www.genengnews.com/gen-news-highlights/nycomed-s-anti-inflammatory-gains-approval-in-eu-for-copd/81243622/ |title="Nycomed's Anti-Inflammatory Gains Approval in EU for COPD" |access-date=10 July 2010 |archive-date=24 August 2017 |archive-url=https://web.archive.org/web/20170824222207/http://www.genengnews.com/gen-news-highlights/nycomed-s-anti-inflammatory-gains-approval-in-eu-for-copd/81243622 |url-status=live }}</ref> 2011년 6월에는 COPD 급성 악화의 완화를 적응증으로 미국 [[미국 식품의약국|FDA]]에서 사용 허가를 내렸다.<ref>{{웹 인용| title=Drug Approval Package: Daliresp Tablets (roflumilast) NDA #022522 | website=U.S. [[Food and Drug Administration]] (FDA) | date=24 December 1999 | url=https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022522Orig1s000TOC.cfm | access-date=28 September 2020 | archive-date=27 October 2020 | archive-url=https://web.archive.org/web/20201027013611/https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022522Orig1s000TOC.cfm | url-status=live }}</ref><ref>{{보도자료 인용| url = https://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm244989.htm | title = FDA approves new drug to treat chronic obstructive pulmonary disease | date = 1 March 2011 | publisher = U.S. [[Food and Drug Administration]] (FDA) | access-date = 16 December 2019 | archive-date = 18 January 2017 | archive-url = https://web.archive.org/web/20170118091136/http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm244989.htm | url-status = dead }}</ref> [[복제약]]으로 이용 가능하다.<ref>{{웹 인용| title=2022 First Generic Drug Approvals | website=U.S. [[Food and Drug Administration]] (FDA) | date=3 March 2023 | url=https://www.fda.gov/drugs/drug-and-biologic-approval-and-ind-activity-reports/2022-first-generic-drug-approvals | archive-url=https://web.archive.org/web/20230630003602/https://www.fda.gov/drugs/drug-and-biologic-approval-and-ind-activity-reports/2022-first-generic-drug-approvals | archive-date=30 June 2023 | url-status=live | access-date=30 June 2023}}</ref>

== 의학적 사용 ==
로플루밀라스트의 적응증은 중증 COPD 치료,<ref name = "Daliresp FDA label" /> 그리고 판상 [[건선]] 치료이다.<ref name="Zoryve FDA label">{{웹 인용| title=Zoryve- roflumilast cream | website=DailyMed | date=16 August 2022 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ec1bb0d1-f38a-4080-831a-68791d1d1fdb | access-date=21 January 2023 | archive-date=21 January 2023 | archive-url=https://web.archive.org/web/20230121062229/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=ec1bb0d1-f38a-4080-831a-68791d1d1fdb | url-status=live }}</ref><ref>{{보도자료 인용| title=FDA Approves Arcutis' Zoryve (Roflumilast) Cream 0.3% For the Treatment of Plaque Psoriasis in Individuals Age 12 and Older | publisher=Arcutis Biotherapeutics | via=GlobeNewswire | date=29 July 2022 | url=https://www.globenewswire.com/news-release/2022/07/29/2488966/0/en/FDA-Approves-Arcutis-ZORYVE-Roflumilast-Cream-0-3-For-the-Treatment-of-Plaque-Psoriasis-in-Individuals-Age-12-and-Older.html | access-date=1 August 2022 | archive-date=1 August 2022 | archive-url=https://web.archive.org/web/20220801114445/https://www.globenewswire.com/news-release/2022/07/29/2488966/0/en/FDA-Approves-Arcutis-ZORYVE-Roflumilast-Cream-0-3-For-the-Treatment-of-Plaque-Psoriasis-in-Individuals-Age-12-and-Older.html | url-status=live }}</ref> 또한 중증 COPD의 악화를 예방하는 데에도 사용한다.<ref name = "Daxas SmPC">{{웹 인용| title=Daxas 250 micrograms tablets - Summary of Product Characteristics (SmPC) | website=(emc) | date=11 June 2020 | url=https://www.medicines.org.uk/emc/product/9162/smpc | access-date=28 September 2020 | archive-date=19 September 2020 | archive-url=https://web.archive.org/web/20200919164902/https://www.medicines.org.uk/emc/product/9162/smpc | url-status=live }}</ref><ref name = "Daliresp FDA label">{{웹 인용| title=Daliresp- roflumilast tablet | website=DailyMed | date=12 March 2020 | url=https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c9a1d0a8-581f-4f91-a2b8-f419192d0ebf | access-date=28 September 2020 | archive-date=25 March 2021 | archive-url=https://web.archive.org/web/20210325081719/https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=c9a1d0a8-581f-4f91-a2b8-f419192d0ebf | url-status=live }}</ref><ref name="Daxas EPAR" /><ref name = EMA>{{웹 인용|title=Daliresp : EPAR - Product Information|work=European Medicines Agency|publisher=Takeda GmbH|date=26 September 2013|access-date=18 November 2013|url=http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002398/WC500103078.pdf|archive-date=26 June 2016|archive-url=https://web.archive.org/web/20160626155812/http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Information/human/002398/WC500103078.pdf|url-status=live}}</ref><ref name = MSR>{{웹 인용|title=roflumilast (Rx) - Daliresp|work=Medscape Reference|publisher=WebMD|access-date=18 November 2013|url=http://reference.medscape.com/drug/daliresp-roflumilast-999626|archive-date=12 September 2017|archive-url=https://web.archive.org/web/20170912145935/http://reference.medscape.com/drug/daliresp-roflumilast-999626|url-status=live}}</ref>

== 부작용 ==
발생률 1~10%로 비교적 흔한 부작용에는 [[설사]], [[체중 감소]], [[구역질]], [[두통]], [[불면증]], [[식욕부진]], [[복통]], [[비염]], [[부비동염]], [[요로감염증]], 우울감 등이 있다.<ref name = "Daliresp FDA label"/><ref name = "Daxas SmPC"/><ref name = EMA/><ref name = MSR/><ref name="pmid18660825">{{저널 인용| vauthors = Spina D | title = PDE4 inhibitors: current status | journal = British Journal of Pharmacology | volume = 155 | issue = 3 | pages = 308–15 | date = October 2008 | pmid = 18660825 | pmc = 2567892 | doi = 10.1038/bjp.2008.307 }}</ref>

== 작용 기전 ==
로플루밀라스트는 [[포스포다이에스터레이스-4 억제제]]로, [[효소]]의 일종인 [[포스포다이에스터레이스-4]](PDE-4)에 직접 결합해 효과를 차단한다. PDE-4는 COPD의 발병 기전에 관여하는 다양한 염증성 세포에서 발현하는 것으로 알려져 있다. 로플루밀라스트 자체가 직접적인 [[기관지확장제]]로서 효과를 보이지는 않으나, 만성 염증을 경감시키는 효과가 있으므로 이미 사용 중인 기관지확장제에 추가해서 보조 약제로서 주로 사용한다.<ref>{{서적 인용|url=https://www.sciencedirect.com/science/article/pii/B9781455707928000167|제목=Chapter 16 - Antiinflammatory Drugs|성=Rabe|이름=Klaus F.|날짜=2012-01-01|편집자-성=Spiro|편집자-이름=Stephen G.|편집자2-성=Silvestri|편집자2-이름=Gerard A.|출판사=W.B. Saunders|위치=Philadelphia|쪽=213–220|isbn=978-1-4557-0792-8|편집자3-성=Agustí|편집자3-이름=Alvar}}</ref>

== 각주 ==
{{각주}}

[[분류:벤즈아마이드]]
[[분류:클로로피리딘]]
[[분류:사이클로프로필 화합물]]
[[분류:유기 플루오린 화합물]]
[[분류:PDE4 억제제]]
[[분류:페놀 에터]]