Androgen deprivation therapy has been the standard treatment for patients with advanced prostate cancer. Androgen deprivation therapy initially suppresses the growth of prostate cancer. However, most patients eventually progress to castration-resistant prostate cancer. Antiandrogens including enzalutamide and abiraterone acetate are recently able to be used for the patients with castration-resistant prostate cancer. Even so, the therapeutic options for castration-resistant prostate cancer are not enough. Androgen receptor splice variants have been attracted attention as one of the mechanisms for castration-resistant prostate cancer. Several androgen receptor splice variants lack the ligand-binding domain, and antiandrogens targeting the ligand-binding domain have little suppression on the growth of prostate cancer. Importantly, the androgen receptor splice variant lacking the ligand-binding domain functions as a constitutively active androgen receptor in the absence of androgen. In this chapter, androgen receptor splice variants are summarized.
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