Abstract: Prostate cancer (PCa) is a major cancer affecting men worldwide, with an increasing incidence in recent years. The androgen receptor (AR) signaling pathway has always been a key pathway in the treatment of prostate cancer, and the hormone treatments such as androgen deprivation therapy (ADT) and AR antagonists are only effective for early-stage non-metastatic disease, while the vast majority of patients progress to castration-resistant prostate cancer (CRPC) at an advanced stage prostate cancer. In recent years, significant progress has been made in research on the mechanisms of resistance to AR antagonists in CRPC patients. This article reviews the roles of abnormalities in the AR signaling pathway, AR gene mutations, and alterations in AR co-regulators in the development of resistance to AR antagonists among CRPC patients, and the current research on the resistance mechanism of AR antagonists in the treatment of PCa, aiming to provide some insight for the development of related new antagonists and the design of clinical treatment.