RD162 is a second-generation androgen receptor (AR) antagonist. It inhibits binding of 18F-FDHT to AR in human prostate cancer cells with an IC50 value of 30.9 nM. RD162 completely suppresses VCaP cell proliferation at 1 µM and induces apoptosis of VCaP cells at 10 µM. RD162 is bioavailable and reduces LNCaP/AR tumor growth in castrated male mice at a daily oral dose of 10 mg/kg.