Prostate cancer is a malignancy commonly occuring in male genitourinary system.Androgen receptor promotes gene transcription in prostate cell growth and carcinogenesis of prostate cancer,which makes it to become an important target in prostate cancer treatment possibly.Prostate cancer may be deteriorated into be castration-resistant prostate cancer easily after androgen deprivation therapy,so it is popular to seek the effective androgen receptor antagonists for treating of castration-resistant prostate cancer.This review focuses on the action mechanism and the development of androgen receptor antagonists for the treatment of prostate cancer.