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Prodrug
Carotegrast methyl
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    Carotegrast methyl

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    Carotegrast methyl
    Carotegrast methyl.svg
    Clinical data
    Trade names Carogra
    Other names AJM 300
    Legal status
    Legal status
    • Rx in Japan
    Identifiers
    • methyl (2S)-2-[(2,6-dichlorobenzoyl)amino]-3-[4-[6-(dimethylamino)-1-methyl-2,4-dioxoquinazolin-3-yl]phenyl]propanoate
    CAS Number
    PubChem CID
    IUPHAR/BPS
    DrugBank
    ChemSpider
    UNII
    KEGG
    CompTox Dashboard (EPA)
    Chemical and physical data
    Formula C28H26Cl2N4O5
    Molar mass 569.44 g·mol−1

    Carotegrast methyl (trade name Carogra) is a drug used for the treatment of ulcerative colitis.

    Carotegrast methyl is a prodrug that has little pharmacological activity itself. The methyl ester, which is designed to enhance oral bioavailability, is hydrolyzed to a carboxylic acid, carotegrast, by the enzyme carboxylesterase 1 in the liver. Carotegrast is an α4-integrin antagonist which prevents the chronic inflammation affecting the gastrointestinal tract in individuals with ulcerative colitis.

    Chemical structure of the active metabolite carotegrast

    Carotegrast methyl received approval in Japan in March 2022 for the treatment of moderate ulcerative colitis in patients who had inadequate response to mesalazine.


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