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    DRUG:

    BAY 1082439

    i
    Other names: BAY 1082439
    Company:
    Bayer
    Drug class:
    PI3K inhibitor
    Related drugs:
    2years
    Overcoming resistance to immune checkpoint therapy in PTEN-null prostate cancer by intermittent anti-PI3Kα/β/δ treatment. (PubMed, Nat Commun)
    Here we find that intermittent but not daily dosing of a PI3Kα/β/δ inhibitor, BAY1082439, on Pten-null prostate cancer models could overcome ICT resistance and unleash CD8 T cell-dependent anti-tumor immunity in vivo...Once primed, tumors remain T cell-inflamed, become responsive to anti-PD-1 therapy and have durable therapeutic effect. Our data suggest that intermittent PI3K inhibition can alleviate Pten-null cancer cell-intrinsic immunosuppressive activity and turn "cold" tumors into T cell-inflamed ones, paving the way for successful ICT.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog) • CD8 (cluster of differentiation 8) • IFNG (Interferon, gamma) • CXCL10 (Chemokine (C-X-C motif) ligand 10) • IFNA1 (Interferon Alpha 1)
    |
    BAY 1082439
    over3years
    The PI3K subunits, P110α and P110β are potential targets for overcoming P-gp and BCRP-mediated MDR in cancer. (PubMed, Mol Cancer)
    The reversal of the dual functions of ABC-transporter-mediated and AKT-activation-enhanced MDR through the inhibition or knockout of PI3K 110α or 110β promises to improve current strategies based on combined drug treatments to overcome MDR challenges.
    Journal
    |
    PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • ABCB1 (ATP Binding Cassette Subfamily B Member 1) • PIK3CB (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta)
    |
    BAY 1082439 • afuresertib (LAE002)