| | Drug | Mechanism of action | Patient characteristics | Phase of development | Clinical trial registration number |
| | MDV-3100 | AR antagonist | Chemotherapy-treated | Phase III | NCT00974311 | | | Chemotherapy-naïve | Phase III | NCT01212991 | | ARN-509 | AR antagonist | ND | Phase I-II | NCT01171898 | | AZD3514 | AR antagonist | ND | Phase I-II | NCT01162395 | | Abiraterone acetate | CYP 17 inhibitor | Chemotherapy-treated | Phase III | NCT00638690 | | | Chemotherapy-naïve | Phase III | NCT00887198 | | Orteronel (TAK-700) | CYP 17 inhibitor | Chemotherapy-treated | Phase III | NCT01193257 | | VN/124-1 (TOK-001) | AR downregulating agent, CYP 17 inhibitor, and AR antagonist | ND | Phase I-II | NCT00959959 |
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