Iguratimod

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INN
Drug class
Routes of administration
Pregnancy category
Bioavailability
Metabolism
Elimination half-life
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Legal status
CAS Number 123663-49-0
PubChem 124246
DrugBank
ChemSpider 110694
KEGG


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it was first published in 2000.[1][2] It was submitted for regulatory approval in Japan in 2003; the application was withdrawn in 2009, and it was resubmitted with additional data in 2011 and approved for marketing in Japan in 2012.[1] Eisai and Toyama Chemical market it in Japan.[3]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]

References[edit | edit source]

  1. 1.0 1.1 1.2 1.3 1.4 1.5 , Iguratimod for the treatment of rheumatoid arthritis in Japan., Expert review of clinical immunology, Vol. 11(Issue: 5), pp. 565–73, DOI: 10.1586/1744666X.2015.1027151, PMID: 25797025,
  2. , Synthesis and antiinflammatory activity of 7-methanesulfonylamino-6-phenoxychromones. Antiarthritic effect of the 3-formylamino compound (T-614) in chronic inflammatory disease models., Chemical & Pharmaceutical Bulletin, Vol. 48(Issue: 1), pp. 131–9, PMID: 10705489, Full text,
  3. , Chapter Thirty-One – To Market, To Market—2011, Annual Reports in Medicinal Chemistry, Vol. 47 pp. 499–569, DOI: 10.1016/B978-0-12-396492-2.00031-X,
  4. Iguratimod - Simcere Full text, , AdisInsight,
  5. Iguratimod - Toyama Chemical Full text, , AdisInsight,


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