RD162 is a second-generation, orally available antiandrogen that binds to androgen receptor (AR) with IC50 of 30.9 nM.
RD162 suppresses growth and induces apoptosis in human prostate cancer cells in vitro.
RD162 demonstrates greater relative affinity than the clinically used antiandrogen bicalutamide, reduces the efficiency of its nuclear translocation, and impairs both DNA binding to androgen response elements and recruitment of coactivators.
RD162 induces tumor regression in mouse models of castration-resistant human prostate cancer.
