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    BIOMARKER:

    RET C634W

    i
    Other names: RET, Ret Proto-Oncogene, Proto-Oncogene Tyrosine-Protein Kinase Receptor Ret, Cadherin-Related Family Member 16, Rearranged During Transfection, RET Receptor Tyrosine Kinase, Cadherin Family Member 12, Proto-Oncogene C-Ret, CDHF12, CDHR16, PTC, Ret Proto-Oncogene (Multiple Endocrine Neoplasia And Medullary Thyroid Carcinoma 1, Hirschsprung Disease), Multiple Endocrine Neoplasia And Medullary Thyroid Carcinoma 1, Hirschsprung Disease 1, RET-ELE1, HSCR1, MEN2A, MEN2B, RET51, MTC1
    Entrez ID:
    5979
    Related biomarkers:
    Expression
    Mutation
    CNA
    Fusion
    Others
    almost3years
    The preclinical selectivity and activity of APS03118, a highly selective and potent next-generation RET inhibitor (AACR 2022)
    Selective RET inhibitors selpercatinib and pralsetinib were recently approved by the FDA and EMA for patients with RET-dependent NSCLC and thyroid cancers. APS03118 is a novel highly selective next-generation RET inhibitor that possesses potent in vitro and in vivo activity against a diverse range of RET alterations, including SFMs-mediated resistance. A first-in-human phase 1 trial for patients with RET-driven solid tumors with activating RET alterations is planned for 2022.
    Preclinical
    |
    RET (Ret Proto-Oncogene) • KIF5B (Kinesin Family Member 5B) • KDR (Kinase insert domain receptor) • CCDC6 (Coiled-Coil Domain Containing 6)
    |
    RET fusion • RET mutation • RET M918T • RET C634W • RET V804L • RET V804M • RET C634* • RET V804*
    |
    Retevmo (selpercatinib) • Gavreto (pralsetinib) • APS03118
    3years
    Clinical features and signaling effects of RET D631Y variant multiple endocrine neoplasia type 2 (MEN2). (PubMed, Korean J Intern Med)
    We suggest that the tumorigenic potential conferred by the D631Y mutation is lower than that conferred by the C634R/W mutation, but higher than that conferred by C630Y. Thus, the risk level of the RET D631Y variant appears to be higher than that of C630Y and lower than that of C634R/W.
    Clinical • Observational data • Retrospective data • Review • Clinical Trial,Phase II • Journal
    |
    RET (Ret Proto-Oncogene)
    |
    RET mutation • RET C634W • RET C634R • RET C634*
    over4years
    [VIRTUAL] The next-generation RET inhibitor TPX-0046 is active in drug-resistant and naïve RET-driven cancer models. (ASCO 2020)
    Selective RET inhibitors (selpercatinib/pralsetinib) are active in patients with these cancers; unfortunately, resistance often occurs. TPX-0046 is a unique next-generation RET inhibitor that possesses potent in vitro and in vivo activity against a diverse range of RET alterations, including SFM-mediated resistance. A phase 1/2 trial for RET inhibitor-resistant and naïve RET-driven cancers is on-going (NCT04161391). Research Funding: Turning Point Therapeutics
    Preclinical
    |
    RET (Ret Proto-Oncogene) • KIF5B (Kinesin Family Member 5B) • CCDC6 (Coiled-Coil Domain Containing 6)
    |
    RET fusion • RET mutation • RET C634W
    |
    Retevmo (selpercatinib) • Gavreto (pralsetinib) • enbezotinib (TPX-0046)