NCIt definition : An orally bioavailable dual-action androgen receptor (AR) inhibitor, with potential
antineoplastic activity. Upon oral administration, AR inhibitor ONCT-534 targets and
binds to both the ligand-binding domain (LBD) and the N-terminal domain (NTD) of the
AR, and inhibits AR-mediated signaling and induces the degradation of AR and AR splice
variant (AR-SV) proteins. This may inhibit cell growth in AR-overexpressing tumor
cells, including those with AR amplification, mutations in the AR LBD, and AR-SVs
with loss of the AR LBD. AR is overexpressed in prostate cancers and is involved in
the proliferation, survival and chemoresistance of tumor cells.;