Table 3.
Novel therapies against castrate-resistant prostate cancer (CRPC) currently in trials.
| Drug | Target | Mechanism of action | Trial Status | Reference |
|---|---|---|---|---|
| Novel androgen receptor (AR) therapeutics currently in clinical trial | ||||
| ARN-509 (apalutamide) | Androgen receptor (AR) | Competitively inhibits transcription | Phase II | (57, 63, 64) |
| EPI-506 | AR | Inhibits transcription | Phase II | (53) |
| AZD3514 | AR | Inhibition of AR nuclear translocation and AR-regulating gene transcription | Phase I | (65) |
| Ketoconazole | Cytochrome P450 c17 (CYP17) | Inhibits adrenal testosterone synthesis | Phase II | (66) |
| MDV3100 | AR | Inhibits AR binding and nuclear translocation of the AR | Phase I | (35) |
| Other novel drug targets | ||||
| Radium-223 (Xofigo) | Bone mineral hydroxyapatite | Induces double-strand DNA breaks | FDA approved for CRPC, bone metastasis | (67) |
| LGK974 | Porcupine [PORCN] (WNT-specific acyltransferase) | Inhibits Wnt signaling | Phase I | (68) |
| Cytarabine (Cytosine Arabinoside) | DNA polymerase | Inhibits DNA synthesis | Phase II | (69) |
| Ipatasertib | AKT (protein Kinase B) | Inhibits three isoforms of AKT | Phase II | (55, 70) |