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Experimental cancer drugs
Galunisertib
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    Galunisertib

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    Galunisertib
    Galunisertib.svg
    Clinical data
    Routes of
    administration    		 PO
    Identifiers
    • 4-(5,6-Dihydro-2-(6-methyl-2-pyridinyl)-4H-pyrrolo(1,2-b)pyrazol-3-yl)-6-quinolinecarboxamide
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    KEGG
    ChEBI
    CompTox Dashboard (EPA)
    Chemical and physical data
    Formula C22H19N5O
    Molar mass 369.428 g·mol−1
    3D model (JSmol)
    • N1=CC=C(C2=CC(=CC=C12)C(=O)N)C1=C2N(N=C1C1C=CC=C(N=1)C)CCC2
    • InChI=1S/C22H19N5O/c1-13-4-2-5-18(25-13)21-20(19-6-3-11-27(19)26-21)15-9-10-24-17-8-7-14(22(23)28)12-16(15)17/h2,4-5,7-10,12H,3,6,11H2,1H3,(H2,23,28)
    • Key:IVRXNBXKWIJUQB-UHFFFAOYSA-N

    Galunisertib (LY2157299) is a small molecular experimental cancer drug previously in development by Eli Lilly. It is a TGF-b inhibitor. Development of galunisertib by Eli Lilly was discontinued in January 2020.

    Galunisertib was investigated in a phase II trial for treatment of hepatocellular carcinoma. Pre-clinically, combination of galunisertib with PD-L1 blockade resulted in improved tumor growth inhibition.


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