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    DRUG:

    crenigacestat (LY3039478)

    i
    Other names: LY3039478, LY-3039478, LY 3039478, JSMD194, BMS-986405, BMS986405, BMS 986405, JSMD-194, JSMD 194
    Associations

    News

    Trials
    Company:
    BMS, Eli Lilly
    Drug class:
    γ-secretase inhibitor, Notch inhibitor
    Related drugs:
    Associations

    News

    Trials
    3ms
    KarMMa-7: Safety and Efficacy of bb2121 (Ide-cel) Combinations in Multiple Myeloma (clinicaltrials.gov)
    P1/2, N=21, Terminated, Celgene | Completed --> Terminated; Business objectives have changed
    Trial termination
    |
    Abecma (idecabtagene vicleucel) • iberdomide (CC-220) • crenigacestat (LY3039478)
    4ms
    A Study of LY3039478 in Participants With Advanced or Metastatic Solid Tumors (clinicaltrials.gov)
    P1, N=94, Terminated, Eli Lilly and Company | Phase classification: P1b --> P1 | Completed --> Terminated; The study was terminated due to business considerations
    Phase classification • Trial termination
    |
    cisplatin • carboplatin • gemcitabine • Verzenio (abemaciclib) • samotolisib (LY3023414) • crenigacestat (LY3039478) • taladegib (ENV 101)
    7ms
    KarMMa-7: Safety and Efficacy of bb2121 (Ide-cel) Combinations in Multiple Myeloma (clinicaltrials.gov)
    P1/2, N=21, Completed, Celgene | Active, not recruiting --> Completed | N=312 --> 21
    Trial completion • Enrollment change
    |
    Abecma (idecabtagene vicleucel) • iberdomide (CC-220) • crenigacestat (LY3039478)
    9ms
    Immunosuppressive JAG2+ tumor-associated neutrophils hamper PD-1 blockade response in ovarian cancer by mediating the differentiation of effector regulatory T cells. (PubMed, Cancer Commun (Lond))
    The emergence of JAG2+ TANs is crucial for the differentiation of eTregs, which triggers immune evasion and resistance to anti-PD-1 therapy. Inhibiting Notch signaling with LY3039478 or JAG2 neutralization antibodies may overcome this anti-PD-1 resistance in HGSOC.
    Journal • PD(L)-1 Biomarker • IO biomarker
    |
    PD-L1 (Programmed death ligand 1) • CD14 (CD14 Molecule)
    |
    crenigacestat (LY3039478)
    12ms
    KarMMa-7: Safety and Efficacy of bb2121 (Ide-cel) Combinations in Multiple Myeloma (clinicaltrials.gov)
    P1/2, N=312, Active, not recruiting, Celgene | Trial completion date: Dec 2026 --> Jan 2025
    Trial completion date
    |
    Abecma (idecabtagene vicleucel) • iberdomide (CC-220) • crenigacestat (LY3039478)
    12ms
    Structural basis of human γ-secretase inhibition by anticancer clinical compounds. (PubMed, Nat Struct Mol Biol)
    Here we report the cryo-electron microscopy structures of human γ-secretase bound individually to five clinically tested GSIs (RO4929097, crenigacestat, BMS906024, nirogacestat and MK-0752) at overall resolutions of 2.4-3.0 Å. The size and shape of the binding pocket are induced by the bound GSI. Analysis of these structural features suggest strategies for modification of the GSI with improved inhibition potency.
    Journal
    |
    NICD (NOTCH1 intracellular domain)
    |
    Ogsiveo (nirogacestat) • AL101 • RG4733 • MK-0752 • crenigacestat (LY3039478)
    12ms
    GINS1 Enhances Glycolysis, Proliferation and Metastasis in Lung Adenocarcinoma Cells by Activating the Notch/PI3K/AKT/mTORC1 Signaling Pathway (PubMed, Zhongguo Fei Ai Za Zhi)
    The expression of GINS1 enhances the expression of Notch1 and Notch3 receptors, and then phosphorylates and activates the downstream PI3K/AKT/mTORC1 signaling pathway to enhance the glycolysis, proliferation and metastasis of LUAD cells.
    Journal
    |
    NOTCH1 (Notch 1) • NOTCH3 (Notch Receptor 3)
    |
    NOTCH1 expression • NOTCH3 expression
    |
    crenigacestat (LY3039478)
    1year
    Targeting cancer-associated fibroblasts/tumor cells cross-talk inhibits intrahepatic cholangiocarcinoma progression via cell-cycle arrest. (PubMed, J Exp Clin Cancer Res)
    The hCAFs/iCCA cross-talk is a new target for reducing cancer progression with drugs such as Crenigacestat.
    Journal • Tumor cell
    |
    NOTCH1 (Notch 1) • CCNE2 (Cyclin E2)
    |
    crenigacestat (LY3039478)
    over1year
    A Study of CC-99712, a BCMA Antibody-Drug Conjugate, in Participants With Relapsed and Refractory Multiple Myeloma (clinicaltrials.gov)
    P1, N=47, Terminated, Celgene | N=160 --> 47 | Active, not recruiting --> Terminated; Slow accrual
    Enrollment change • Trial termination
    |
    crenigacestat (LY3039478) • ispectamab debotansine (BMS-986352)
    almost2years
    A Study of CC-99712, a BCMA Antibody-Drug Conjugate, in Participants With Relapsed and Refractory Multiple Myeloma (clinicaltrials.gov)
    P1, N=160, Active, not recruiting, Celgene | Trial completion date: May 2025 --> Aug 2024 | Trial primary completion date: May 2025 --> Aug 2024
    Trial completion date • Trial primary completion date
    |
    crenigacestat (LY3039478) • ispectamab debotansine (BMS-986352)
    almost2years
    A Study of CC-99712, a BCMA Antibody-Drug Conjugate, in Participants With Relapsed and Refractory Multiple Myeloma (clinicaltrials.gov)
    P1, N=160, Active, not recruiting, Celgene | Trial completion date: Apr 2024 --> May 2025 | Trial primary completion date: Apr 2024 --> May 2025
    Trial completion date • Trial primary completion date
    |
    crenigacestat (LY3039478) • ispectamab debotansine (BMS-986352)
    almost2years
    A Study of LY3039478 in Japanese Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=11, Completed, Eli Lilly and Company | Active, not recruiting --> Completed | Trial completion date: Oct 2023 --> May 2023
    Trial completion • Trial completion date • Metastases
    |
    crenigacestat (LY3039478)