Abstract: Castration-resistant prostate cancer (CRPC) is the lethal form of prostate cancer with developed resistance to androgen deprivation therapy. However, anti- androgen therapy remains an important treatment option because androgen receptor activation is a major driver of the advanced phase of CRPC. Drug resistance is frequently manifested despite the development of various novel anti-an-drogens with significant clinical efficacy. This review introduces several drugs prevalently used to treat CRPC. The mechanisms of ac-tion and pathways to resistance of these drugs are also discussed.