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    DRUG:

    VRN101099

    i
    Other names: VRN101099
    Company:
    Voronoi
    Drug class:
    HER2 inhibitor
    Related drugs:
    2years
    VRN101099, Brain Permeable HER2 Kinase Inhibitor, Shows the Anti-tumor Activity in Preclinical Models of HER2-positive Cancers (SABCS 2022)
    While T-DXd showed positive results in HER2-positive breast cancer brain metastasis (BCBM), its activity and blood-brain barrier (BBB) permeability in active BCBM need to be further validated (TUXEDO-1 included 15 patients with active brain metastasis). Tucatinib plus Trastuzumab and Capecitabine triplet showed efficacy in patients with brain metastasis, but Tucatinib alone has poor BBB penetration...In summary, VRN101099 is a brain penetrant, orally bioavailable, irreversible, and highly selective inhibitor of HER2 with therapeutic potential in HER2-positive BCBM. These data support the clinical development of VRN101099 in HER2-driven cancers.
    Preclinical
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    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
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    HER-2 positive • EGFR mutation • HER-2 mutation • HER-2 expression • EGFR wild-type
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    Herceptin (trastuzumab) • Enhertu (fam-trastuzumab deruxtecan-nxki) • capecitabine • Tukysa (tucatinib) • VRN101099