| 词条 | Iguratimod |
| 释义 |
| drug_name = | IUPAC_name = N-(3-Formamido-4-oxo-6-phenoxy-4H-chromen-7-yl)methanesulfonamide | image = Iguratimod.svg | alt = | caption = | tradename = Careram; Kolbet | Drugs.com = | MedlinePlus = | pregnancy_AU = | pregnancy_US = | pregnancy_category= | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = 123663-49-0 | ATCvet = | ATC_prefix = None | ATC_suffix = | DrugBank = | PubChem = 124246 | ChemSpiderID = 110694 | ChEMBL = 2107455 | synonyms = T-614 | C=17 | H=14 | N=2 | O=6 | S=1 | molecular_weight = 374.368 g/mol | smiles = O=S(=O)(Nc3c(Oc1ccccc1)cc2c(O/C=C(\\C2=O)NC=O)c3)C | StdInChI = 1S/C17H14N2O6S/c1-26(22,23)19-13-8-15-12(17(21)14(9-24-15)18-10-20)7-16(13)25-11-5-3-2-4-6-11/h2-10,19H,1H3,(H,18,20) | StdInChIKey = ANMATWQYLIFGOK-UHFFFAOYSA-N }}Iguratimod is an anti-inflammatory small molecule drug used for the treatment of rheumatoid arthritis, together with methotrexate in Japan and China.[1] As of 2015 the biological target was not known, but it prevents NF-κB activation and subsequently selectively inhibits COX-2 and several inflammatory cytokines.[1] Adverse effects include Elevated transaminases, nausea, vomiting, stomach pain; rashes, and itchiness.[1] It is a derivative of 7-methanesulfonylamino-6-phenoxychromones and is a chromone with two amide groups; it was first published in 2000.[1][2] It was submitted for regulatory approval in Japan in 2003; the application was withdrawn in 2009, and it was resubmitted with additional data in 2011 and approved for marketing in Japan in 2012.[1] Eisai and Toyama Chemical market it in Japan.[3] Approval was obtained in China in 2011 by Simcere, independently of the Japanese originators.[1][4] During discovery and development it was called T-614 and it is marketed under the names Careram and Kolbet.[5] References1. ^1 2 3 4 5 {{cite journal|last1=Tanaka|first1=K|last2=Yamaguchi|first2=T|last3=Hara|first3=M|title=Iguratimod for the treatment of rheumatoid arthritis in Japan.|journal=Expert review of clinical immunology|date=May 2015|volume=11|issue=5|pages=565–73|doi=10.1586/1744666X.2015.1027151|pmid=25797025}} {{antineoplastic-drug-stub}}2. ^{{cite journal|last1=Inaba|first1=T|last2=Tanaka|first2=K|last3=Takeno|first3=R|last4=Nagaki|first4=H|last5=Yoshida|first5=C|last6=Takano|first6=S|title=Synthesis and antiinflammatory activity of 7-methanesulfonylamino-6-phenoxychromones. Antiarthritic effect of the 3-formylamino compound (T-614) in chronic inflammatory disease models.|journal=Chemical & Pharmaceutical Bulletin|date=January 2000|volume=48|issue=1|pages=131–9|pmid=10705489|url=https://www.jstage.jst.go.jp/article/cpb1958/48/1/48_1_131/_pdf/-char/en}} 3. ^{{cite journal|last1=Bronson|first1=J|last2=Dhar|first2=M|last3=Ewing|first3=W|last4=Lonberg|first4=N|title=Chapter Thirty-One – To Market, To Market—2011|journal=Annual Reports in Medicinal Chemistry|date=2012|volume=47|pages=499–569|doi=10.1016/B978-0-12-396492-2.00031-X}} 4. ^{{cite web|title=Iguratimod - Simcere|url=https://adisinsight.springer.com/drugs/800032226|publisher=AdisInsight|accessdate=27 May 2018|language=en}} 5. ^{{cite web|title=Iguratimod - Toyama Chemical|url=https://adisinsight.springer.com/drugs/800001541|publisher=AdisInsight|accessdate=27 May 2018|language=en}} 4 : Sulfonamides|Anti-inflammatory and antirheumatic products|Chromones|Formamides |
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