研究发现，雄激素受体与前列腺癌的发生存在密切关系。雄激素拮抗疗法成为临床治疗早期前列腺癌的有效手段，近20年来已有多个药物上市（如氟他胺、羟基氟他胺和比卡鲁胺等），但这些经典的药物在治疗中易产生抗雄激素撤除综合症等问题，因此其应用受到限制。目前，新近研发的非甾体类雄激素受体拮抗剂（如RD162、MDV3100和BMS-641988）活性更强，正进行临床试验，并有望解决过去雄激素受体拮抗剂存在的问题。查阅国内外相关文献，对已上市药物、当前临床研究的药物以及近年发现的小分子雄激素受体抑制剂的研究进展进行综述。

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.