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Eganelisib
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    Eganelisib

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    Eganelisib
    IPI-549.svg Eganelisib ball-and-stick 6XRL.png
    Clinical data
    Routes of
    administration
    Oral
    ATC code
    • None
    Identifiers
    • 2-amino-N-[(1S)-1-{8-[(1-methyl-1H-pyrazol-4-yl)ethynyl]-1-oxo-2-phenyl-1,2-dihydroisoquinolin-3-yl}ethyl]pyrazolo[1,5-a]pyrimidine-3-carboxamide
    CAS Number
    PubChem CID
    ChemSpider
    UNII
    KEGG
    ChEMBL
    PDB ligand
    Chemical and physical data
    Formula C30H24N8O2
    Molar mass 528.576 g·mol−1
    3D model (JSmol)
    • Cn1cc(cn1)C#Cc6cccc2c6C(=O)N(C(=C2)C(C)NC(=O)c4c3ncccn3nc4N)c5ccccc5
    • InChI=1S/C30H24N8O2/c1-19(34-29(39)26-27(31)35-37-15-7-14-32-28(26)37)24-16-22-9-6-8-21(13-12-20-17-33-36(2)18-20)25(22)30(40)38(24)23-10-4-3-5-11-23/h3-11,14-19H,1-2H3,(H2,31,35)(H,34,39)/t19-/m0/s1
    • Key:XUMALORDVCFWKV-IBGZPJMESA-N

    Eganelisib (USAN), codenamed IPI-549, is an experimental drug being investigated as a possible treatment for cancer. It is a highly selective phosphoinositide 3-kinase inhibitor, and thus works by inhibiting the enzyme PIK3CG, disrupting the PI3K/AKT/mTOR signaling pathway which plays important roles in the development of cancer.

    Eganelisib is being developed by Infinity Pharmaceuticals. Early clinical trial results were published in September 2016. On September 29, 2020, it was granted Fast Track designation by the United States Food and Drug Administration (FDA) as a treatment for inoperable, locally advanced, or metastatic triple-negative breast cancer, combined with a checkpoint inhibitor and chemotherapy.

    As of October 2020, five phase I/II clinical trials were ongoing in the United States, and one in Europe.

    Further reading


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