Description:
IC50 Value: N/A
AZD3514 is a small-molecule androgen receptor downregulator for treatment of advanced prostate cancer [1]. AZD3514 binds to the AR ligand binding domain and has selectivity for binding to AR over other nuclear hormone receptors.
in vitro: AZD3514 inhibits cell growth in prostate cancer cells expressing wild-type (VCaP) and mutated (T877A) AR (LNCaP), but is inactive in AR-negative prostate cancer cells, indicating a dependency on AR for efficacy [2].
in vivo: We assessed activity initially in the Hershberger castrated rat assay in which oral dosing of AZD3514 (100mg/kg once-daily for 7 days) significantly inhibited testosterone-induced growth of sexual accessory organs [2].
Clinical trial: Open-label Prostate Cancer Study. Phase 1