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.