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    DRUG CLASS:

    MDM2 protein degrader

    Related drugs:
    11d
    KT253-AL-101: Safety and Clinical Activity of KT-253 in Adult Patients with High Grade Myeloid Malignancies, Acute Lymphocytic Leukemia, Lymphoma, Solid Tumors (clinicaltrials.gov)
    P1, N=70, Active, not recruiting, Kymera Therapeutics, Inc. | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    7ms
    Discovery of ganoderic acid A (GAA) PROTACs as MDM2 protein degraders for the treatment of breast cancer. (PubMed, Eur J Med Chem)
    Finally, in vivo experiments showed that, V10 also exhibited good tumor inhibitory activity in xenografted TNBC zebrafish models, with an inhibition rate of 27.2% at 50 μg/mL. In conclusion, our results suggested that V10 has anti-tumor effects on p53-mutant breast cancer in vitro and in vivo, and may be used as a novel lead compound for the future development of TNBC.
    Journal • IO biomarker
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    TP53 (Tumor protein P53) • BCL2 (B-cell CLL/lymphoma 2) • BAX (BCL2-associated X protein) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • CCNB1 (Cyclin B1)
    |
    TP53 mutation • BCL2/BAX ratio elevation
    11ms
    Safety and Clinical Activity of KT-253 in Adult Patients With High Grade Myeloid Malignancies, Acute Lymphocytic Leukemia, Lymphoma, Solid Tumors (clinicaltrials.gov)
    P1, N=70, Recruiting, Kymera Therapeutics, Inc.
    Trial completion date • Trial primary completion date • Metastases
    over1year
    A MDM2 degrader inhibits cell proliferation and growth of MDM2-overexpressing acute lymphoblastic leukemia in SCID mice (AACR 2023)
    Importantly, MX69-114b had minimal or no inhibitory effect on normal human hematopoiesis in vitro and was very well tolerated in vivo in animal models. Based on the strong inhibitory and apoptotic activity against MDM2-overexpressing ALL, along with minimal or no toxicity to normal cells/tissues, MX69-114b is a candidate for further development as a novel MDM2-targeted therapeutic drug for refractory ALL.
    Preclinical
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    MDM2 (E3 ubiquitin protein ligase)
    |
    MDM2 overexpression
    |
    MX69-114b