An orally bioavailable, second-generation inhibitor of the N-terminal domain (NTD) of androgen receptor (AR), with potential antineoplastic activity. Upon oral administration, AR inhibitor EPI-7386 specifically binds to the NTD of AR, thereby inhibiting both AR activation and the AR-mediated signaling pathway. This may inhibit cell growth in AR-overexpressing tumor cells. AR is overexpressed in prostate cancers and is involved in the proliferation, survival and chemoresistance of tumor cells. EPI-7386 may be more active and metabolically stable than first-generation AR NTD inhibitors.