Table 2.
Androgen receptor (AR) targeted therapies—FDA-approved drugs in clinic.
Drug | Target | Mechanism of action | Clinical use | Reference |
---|---|---|---|---|
Abiraterone acetate | Cytochrome P450 c17 (CYP17) | Inhibits androgen biosynthesis | Castration-resistant and high-risk castration sensitive prostate cancer (PCa) | (57) |
Enzalutamide (Xtandi) | AR | Inhibits nuclear translocation of the AR | Metastasized castrate-resistant prostate cancer | (14) |
Leuprolide acetate | Luteinizing hormone releasing hormone | Inhibits secretion of luteinizing hormone, androgen, and estradiol | Approved for palliative treatment of advanced PCa | (61) |
R-Bicalutamide (CASODEX) | Cytosolic AR | Inhibits androgen activity by binding cytosolic ARs and stimulating AR nuclear translocation | Approved for metastasized PCa | (62) |