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    BIOMARKER:

    GPR20 expression

    i
    Other names: GPR20, G Protein-Coupled Receptor 20, G-Protein Coupled Receptor 20, CTD-3064M3.3
    Entrez ID:
    2843
    over3years
    Identification and Therapeutic Targeting of GPR20, Selectively Expressed in Gastrointestinal Stromal Tumors, with DS-6157a, a First-In-Class Antibody-Drug Conjugate. (PubMed, Cancer Discov)
    DS-6157a exhibited GPR20 expression-dependent antitumor activity in GIST xenograft models including a GIST model resistant to imatinib, sunitinib, and regorafenib. Pre-clinical pharmacokinetics and safety profile of DS-6157a support its clinical development as a potential novel GIST therapy in patients with resistance, refractory, or intolerance to approved TKIs.
    Journal
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • GPR20 (G Protein-Coupled Receptor 20)
    |
    KIT mutation • PDGFRA mutation • KIT expression • GPR20 expression
    |
    imatinib • sunitinib • Stivarga (regorafenib) • DS-6157
    over4years
    [VIRTUAL] Therapeutic targeting of GPR20, selectively expressed in gastrointestinal stromal tumor (GIST), with DS-6157a, an antibody-drug conjugate (ADC) (AACR-II 2020)
    In addition, DS-6157a showed antitumor activity in a GIST patient-derived xenograft model that was resistant to imatinib, sunitinib, and regorafenib. In preclinical toxicology studies using rats and cynomolgus monkeys, the pharmacokinetics and safety profile of DS-6157a were favorable at up to 200 mg/kg and 30 mg/kg, respectively. These data support the clinical development of DS-6157a as a potential novel GIST therapy with activity in patients that are resistant, refractory, or intolerant to approved TKIs.
    PARP Biomarker
    |
    KIT (KIT proto-oncogene, receptor tyrosine kinase) • PDGFRA (Platelet Derived Growth Factor Receptor Alpha) • CHEK1 (Checkpoint kinase 1) • GPR20 (G Protein-Coupled Receptor 20)
    |
    PDGFRA mutation • KIT expression • GPR20 expression
    |
    imatinib • sunitinib • Stivarga (regorafenib) • DS-6157