androgen receptor antagonist TAS3681

An orally bioavailable inhibitor of the androgen receptor (AR), with potential antineoplastic activity. Upon oral administration, AR inhibitor TAS3681 specifically binds to AR. This prevents AR activation, downregulates AR and prevents AR-mediated signaling. This inhibits cell growth in AR-overexpressing tumor cells. AR is overexpressed in prostate cancers and is involved in proliferation, survival and chemoresistance of tumor cells.