PHARMACEUTICAL COMBINATIONS OF SOS1 INHIBITORS FOR TREATING AND/OR PREVENTING CANCER

    公开(公告)号:US20240366608A1

    公开(公告)日:2024-11-07

    申请号:US18262155

    申请日:2022-01-19

    Applicant: Lupin Limited

    Abstract: This disclosure relates to pharmaceutical combinations for treating and/or preventing cancer and methods and uses thereof. More particularly, provided is a pharmaceutical combination comprising a SOS1 Inhibitor and an additional active ingredient selected from a KRAS inhibitor such as a KRAS G12C inhibitor and a KRASG12D inhibitor, KRAS G13C inhibitor, and panKRAS inhibitor; an EGFR inhibitor; an ERK1/2 inhibitor; a BRAF inhibitor; a pan-RAF inhibitor; a MEK inhibitor; a AKT inhibitor; a SHP2 inhibitor; protein arginine methyltransferases (PRMTs) inhibitor such as a PRMT5 inhibitor and Type 1 PRMT inhibitor; a PI3K inhibitor; a cyclin-dependent kinase (CDK) inhibitor such as CDK4/6 inhibitor; a FGFR inhibitor; a c-Met inhibitor; a RTK inhibitor; a non-receptor tyrosine kinase inhibitor; a histone methyltransferases (HMTs) inhibitor; a DNA methyltransferases (DNMTs) inhibitor; a Focal Adhesion Kinase (FAK) inhibitor; a Bcr-Abl tyrosine kinase inhibitor; a mTOR inhibitor; a PD1 inhibitor; a PD-L1 inhibitor; CTLA4 inhibitor; and chemotherapeutic agents such as gemcitabine, doxorubicin, cisplatin, carboplatin, paclitaxel, docetaxel, topotecan, irinotecan and temozolomide.

    PHARMACEUTICAL COMBINATION AND APPLICATION THEREOF

    公开(公告)号:US20240342176A1

    公开(公告)日:2024-10-17

    申请号:US18292362

    申请日:2022-07-27

    CPC classification number: A61K31/519 A61K31/4439 A61P35/00 A61K2039/505

    Abstract: A pharmaceutical combination and an application thereof. The pharmaceutical combination comprises a PI3K inhibitor and an immune checkpoint inhibitor, wherein the PI3K inhibitor is selected from a compound represented by formula (I), linperlisib, samotolisib, copanlisib, SHC014748M, pilaralisib, buparlisib, taselisib, YZJ-0673, gedatolisib, omipalisib, bimiralisib, voxtalisib, AL58805, and HEC68498, and pharmaceutically acceptable salts thereof, and the immune checkpoint inhibitor is a PD-1/PD-L1 inhibitor. The compound represented by formula (Ia) has a high inhibitory effect on PI3Kδ and PI3Kγ kinases, and the pharmaceutical combination uses a PI3K inhibitor and a PD-1 inhibitor in combination, thereby effectively improving the inhibitory effect on tumors, and solving the problem of drug resistance of PD-1/PD-L1 inhibitors.

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