^
    Back
    Association details:
    Biomarker:GPR20 expression
    Cancer:Gastrointestinal Stromal Tumor
    Drug:DS-6157 (Topoisomerase I inhibitor, GPR20 -targeted antibody-drug conjugate)
    Direction:Sensitive
    Evidence:
    Evidence Level:
    Sensitive: D – Preclinical
    Source:
    AACR-II 2020
    Title:

    Abstract 5181: Therapeutic targeting of GPR20, selectively expressed in gastrointestinal stromal tumor (GIST), with DS-6157a, an antibody-drug conjugate (ADC)

    Published date:
    05/15/2020
    Excerpt:
    In addition, DS-6157a showed antitumor activity in a GIST patient-derived xenograft model that was resistant to imatinib, sunitinib, and regorafenib. In vitro, DS-6157a induced TOP1 inhibitor-associated markers of DNA damage (phosphorylation of Chk1) and apoptosis (cleaved PARP) in GPR20 expressing cells.
    DOI:
    10.1158/1538-7445.AM2020-5181
    Evidence Level:
    Sensitive: D – Preclinical
    New
    Source:
    Cancer Discov
    Title:

    Identification and Therapeutic Targeting of GPR20, Selectively Expressed in Gastrointestinal Stromal Tumors, with DS-6157a, a First-in-Class Antibody-Drug Conjugate

    Excerpt:
    DS-6157a exhibited GPR20 expression-dependent antitumor activity in GIST xenograft models including a GIST model resistant to imatinib, sunitinib, and regorafenib.
    DOI:
    https://doi.org/10.1158/2159-8290.CD-20-1434