The study has found that androgen receptor is closely associated with development of prostate cancer, and now, androgen antagonist therapy has become an effective way of clinical treatment for early prostate cancer. A number of drugs were launched in the past two decades such as flutamide, hydroxyl-flutamide, and bicalutamide. However, these classic drugs were easy in the anti-androgen withdrawal syndrome which limited their application in clinical. At present, the newly-developed non-steroidal androgen receptor antagonists (such as RD162, MDV3100, and BMS-641988) show more potent activity and are tested in clinical trials, which could solve the above problems to some extents. This paper summarizes the progress on the launched drugs, the current clinical studied drugs and small-molecule androgen receptor antagonists based on relevant literatures.