^
    almost3years
    AR-V7 in Metastatic Prostate Cancer: A Strategy beyond Redemption. (PubMed, Int J Mol Sci)
    AR-V7 is an important oncogenic driver and plays a role as an early diagnostic and prognostic marker, as well as a therapeutic target for antagonists such as niclosamide and TAS3681. Anti-AR-V7 drugs have shown promise in recent clinical investigations on this subset of patients. This mini-review focuses on the relevance of AR-V7 in the clinical manifestations of castration-resistant prostate cancer (CRPC) and summarizes redemptive therapeutic strategies.
    Review • Journal
    |
    AR (Androgen receptor)
    |
    AR splice variant 7
    |
    niclosamide • TAS3681
    3years
    [VIRTUAL] First-in-human study of TAS3681, an oral androgen receptor (AR) antagonist with AR and AR splice variant (AR-SV) downregulation activity, in patients (pts) with metastatic castration-resistant prostate cancer (mCRPC) refractory to abiraterone (ABI) and/or enzalutamide (ENZ) and chemotherapy (CT). (ASCO 2021)
    The recommended phase 2 dose is 300 mg BID . TAS3681 has a manageable safety profile and has antitumor activity against heavily pretreated, multi-drug resistant mCRPC . The study expansion phase is enrolling pts who have progressed on ABI or ENZ +/- taxane CT.
    Clinical • P1 data
    |
    AR (Androgen receptor)
    |
    AR mutation • AR overexpression
    |
    Xtandi (enzalutamide capsule) • abiraterone acetate • TAS3681