| 词条 | Crisaborole |
| 释义 |
| IUPAC_name = 4-[(1-Hydroxy-1,3-dihydro-2,1-benzoxaborol-5-yl)oxy]benzonitrile | image = Crisaborole.svg |pronounce= | tradename = Eucrisa, {{IPAc-en|j|uː|ˈ|k|r|ɪ|s|ə}} {{respell|yoo|KRIS|ə}} | legal_US = Rx-only | routes_of_administration = Topical (ointment) | CAS_number = 906673-24-3 | CAS_supplemental = | ATCvet = | ATC_prefix = D11 | ATC_suffix = AH06 | ATC_supplemental = | PubChem = 44591583 | PubChemSubstance = | IUPHAR_ligand = | DrugBank = DB05219 | ChemSpiderID = 24701949 | UNII = Q2R47HGR7P | KEGG = D10873 | ChEBI_Ref = {{ebicite|correct|EBI}} | ChEBI = 134677 | ChEMBL = | NIAID_ChemDB = | synonyms = | chemical_formula = | C=14 | H=10 | B=1 | N=1 | O=3 | molecular_weight = 251.045100 g/mol | SMILES = B1(c2ccc(cc2CO1)Oc3ccc(cc3)C#N)O | StdInChI = 1S/C14H10BNO3/c16-8-10-1-3-12(4-2-10)19-13-5-6-14-11(7-13)9-18-15(14)17/h1-7,17H,9H2 | StdInChI_comment = | StdInChIKey = USZAGAREISWJDP-UHFFFAOYSA-N }}Crisaborole (trade name Eucrisa) is a nonsteroidal topical medication used for the treatment of mild-to-moderate atopic dermatitis (eczema) in people two years or older.[1][2] It was approved by U.S. Food and Drug Administration on Dec 14, 2016.[3] Mechanism of actionIt is a phosphodiesterase-4 inhibitor, mainly acting on phosphodiesterase 4B (PDE4B), which causes inflammation.[4] Chemically, crisaborole is a phenoxybenzoxaborole.[4] Inhibition of PDE4B appears to suppress the release of tumor necrosis factor alpha (TNFα), interleukin-12 (IL-12), IL-23 and other cytokines, proteins believed to be involved in the immune response and inflammation.[4] ChemistryThe chemical name for crisaborole is 4-[(1-hydroxy-1,3-dihydro-2,1-benzoxaborol-5-yl)oxy]benzonitrile.[4] HistoryCrisaborole was developed by Anacor Pharmaceuticals for the topical treatment of psoriasis.[5][6][7] During preclinical and clinical development, crisaborole was called AN2728 and PF-06930164.[8] See also
References1. ^{{cite web | title = FDA Approves Eucrisa for Eczema | url = http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm533371.htm | publisher = U.S. Food and Drug Administration | date = 14 December 2016}} {{Phosphodiesterase inhibitors}}2. ^{{cite web | title=Eucrisa (crisaborole) Ointment, 2%, for Topical Use. Full Prescribing Information | url = http://labeling.pfizer.com/ShowLabeling.aspx?id=5331 | publisher = Anacor Pharmaceuticals, Inc. Palo Alto, CA 94303 USA | accessdate = 17 December 2016}} 3. ^{{cite press release | url = https://www.fda.gov/newsevents/newsroom/pressannouncements/ucm533371.htm | title = FDA approves Eucrisa for eczema | date = December 14, 2016 | publisher = U.S. Food and Drug Administration}} 4. ^{{cite web|title=WHO Drug Information, Vol. 29, No. 3, 2015. International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 74|url=http://www.who.int/medicines/publications/druginformation/innlists/RL74.pdf|publisher=World Health Information|accessdate=26 April 2016|page=391}} 5. ^{{cite journal | last1 = Nazarian | first1 = R | last2 = Weinberg | first2 = JM | title = AN-2728, a PDE4 Inhibitor for the Potential Topical Treatment of Psoriasis and Atopic Dermatitis | journal = Current Opinion in Investigational Drugs | date = November 2009 | volume = 10 | issue = 11 | pages = 1236–42 | pmid = 19876791}} 6. ^1 2 3 {{cite journal | last1 = Moustafa | first1 = F | last2 = Feldman | first2 = SR | title = A Review of Phosphodiesterase-Inhibition and the Potential Role for Phosphodiesterase 4-Inhibitors in Clinical Dermatology | journal = Dermatology Online Journal | date = 16 May 2014 | volume = 20 | issue = 5 | pages = 22608 | pmid = 24852768 | url = http://escholarship.org/uc/item/2hx1m6kv.pdf}} 7. ^{{cite journal | last1 = Spreitzer | first1 = H | title = Neue Wirkstoffe: Crisaborol | journal = Österreichische Apotheker-Zeitung | date = 16 August 2016 | issue = 17/2016 | language = German}} 8. ^{{cite web|title=Crisaborole|url=http://adisinsight.springer.com/drugs/800024239|publisher=AdisInsight|accessdate=24 July 2017|language=en}} 5 : Ethers|Nitriles|Organoboron compounds|PDE4 inhibitors|Phosphodiesterase inhibitors |
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