| Compound | Company | Structure | Stage of development | Mechanism of action |
| Targeting the androgen pathway | ||||
| Abiraterone | Janssen | Oral androgen biosynthesis inhibitor | Phase III | 17 a-hydroxylase/C17,20-lyase (CYP17) inhibitor |
| Enzalutamide | Astellas | Oral hormonal therapy | Phase III | Androgen receptor antagonist |
| Orteronel | Takeda Pharmaceutical Company | Oral androgen biosynthesis inhibitor | Phase III | CYP17A1 inhibitor |
| Galeterone | Tokai Pharmaceuticals | Oral hormonal therapy and androgen biosynthesis inhibitor | Phase III | Both androgen receptor antagonist and an CYP17A1 inhibitor |
| ARN-509 | Johnson & Johnson | Oral hormonal therapy | Phase III | Androgen receptor antagonist |
| ODM-201 | Orion and Bayer Health Care | Oral hormonal therapy | Phase III | Androgen receptor antagonist |
| Targeting bone microenvironment | ||||
| Zoledronic Acid | Novartis | Intravenous bone resorption inhibitor | Phase IV | Farnesyl pyrophosphate sy50*ntetase inhibitor |
| Denosumab | Amgen | Subcoutaneus bone resorption inhibitor | Phase IV | RANK-L antibody |
| Radium-223 | Bayer | Isotope of radium | Phase III | Radiopharmaceutical alpha-particles target |
| Targeting signal transduction pathways | ||||
| Cabozantinib | Exelixis | Oral small molecule TKi | Phase III | c-MET/HGF pathway inhibitor |
| Dasatinib | Bristol-Myers Squibb | Oral small molecule TKi | Phase III | c-Src/Abl kinase inhibitor |
| Zibotentan | AstraZeneca | Oral small molecule | Phase III | Endothelin receptor A antagonist |
| Immunotherapies | ||||
| Sipuleucel-T | Dendreon Corporation | Intravenous autologous cellular immunotherapy | Phase III | Immunomodulatory agent |
| Ipilimumab | Bristol-Myers Squibb | Intravenous monoclonal antibody | Phase III | CTLA-4 inhibitor and immunomodulatory agent |
| Other molecules | ||||
| Tasquinimod | Ipsen and Active Biotech | Oral small molecule tumor microenvironment inhibitor | Phase III | S100A9 inhibitor |
| Custirsen | Oncogenex Pharma | Intravenous antiapoptotic signalling inhibitor | Phase III | Clusterin production inhibitor |