^
    11d
    Identification of Oral Bioavailable Coumarin Derivatives as Potential AR Antagonists Targeting Prostate Cancer. (PubMed, J Med Chem)
    Especially, 4a showed superior efficacy against ARF876L/T877A and ARW741C mutants compared to darolutamide and enzalutamide. Moreover, 4a exhibited favorable pharmacokinetic profiles (F = 66.24%) in vivo and significant tumor growth inhibition in an LNCaP xenograft mouse model upon oral administration. These results highlight the potential of 4a as a promising oral AR antagonist for overcoming drug resistance in PCa.
    Journal
    |
    AR (Androgen receptor)
    |
    AR F876L • AR T877A • AR W741C
    |
    Xtandi (enzalutamide capsule) • Nubeqa (darolutamide)