tcsc1443 AZD3514

AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 μM and has ability of reducing AR protein expression.

IC50 Value: 2.2 uM (Ki)

Target: androgen receptor

AZD3514 binds to the AR ligand binding domain and has selectivity for binding to AR over other nuclear hormone receptors [1].

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