Pharmacology , pharmacokinetics , clinical study and safety of enzalutamide in the treatment of castration-resistant pros-tate cancer (CRPC) were reviewed in the paper.Enzalutamide, a pure second-generation androgen receptor antagonist , can inhibit multiple points in the androgen receptor signaling pathway , including the inhibition of androgen binding to the androgens receptor , nu-clear translocation of the androgens receptor complex and binding of the androgens receptor complex to deoxyribonucleix acid ( DNA) . The phase 3 clinical trials have revealed that enzalutamide is effective to delay the progression of metastatic CRPC , reduce the prostate-specific antigen (PSA) levels, decrease the progression time of PSA and prolong the overall survival time and the time of first skeletal -related events .Enzalutamide has become a novel treatment option for CRPC patients .Enzalutamide is well tolerated with low incidence of side effects .