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    Association details:
    Biomarker:AR splice variant 7 expression
    Cancer:Prostate Cancer
    Drug:masofaniten (EPI-7386) (Androgen receptor antagonist)
    Direction:Sensitive
    Evidence:
    Evidence Level:
    Sensitive: D – Preclinical
    New
    Source:
    Ann Oncol
    Title:

    Preclinical profile of EPI-7386, a second-generation N-terminal domain androgen receptor inhibitor for the treatment of prostate cancer

    Published date:
    12/17/2020
    Excerpt:
    EPI-7386...inhibited both AR full-length and AR-V7 dependent gene expression and maintained antitumor activity in AR-V7-expressing tumor models, including in in vivo models resistant to enzalutamide (ENZ).
    Evidence Level:
    Sensitive: D – Preclinical
    Source:
    AACR-II 2020
    Title:

    Abstract 1953: Pre-clinical development of the second-generation N-terminal domain androgen receptor inhibitor, EPI-7386, for the treatment of prostate cancer

    Published date:
    05/15/2020
    Excerpt:
    EPI-7386 has an IC50 of 421 nM in LNCaP reporter assays, a similar range to the most active LBD inhibitors, but contrary to these drugs, antitumor activity was maintained in models of CRPC expressing AR-V7. As expected, no activity was observed in non-AR driven models.
    DOI:
    10.1158/1538-7445.AM2020-1953