Table 1 AR axis targeting drugs in clinical development
From: Targeting molecular resistance in castration-resistant prostate cancer
Agent | Pharmaceutical company | Mechanisms of action/target | Current development status |
|---|---|---|---|
ARN-509 | Johnson & Johnson | AR antagonist – inhibits nuclear transportation, inhibits DNA binding | In multiple phase III clinical trials (SPARTAN, etc.) |
AZD3514 | Astra Zeneca | Small molecule modulating AR through two distinct mechanisms | Completed Phase I recruitment |
EPI-001 | ESSA Pharma Inc. | Inhibiting the N-terminus of the AR protein | Awaiting clinical development |
ODM-201 | Bayer HealthCare | AR antagonist – distinct from enzalutamide and ARN509 | In phase III clinical trial (ARAMIS) |
OGX-011 (Custirsen) | OncoGenex Pharmaceuticals and Teva Pharmaceuticals | Second-generation antisense drug that targets clusterin, a secreted protein that acts as a cell-survival protein and is over-expressed in response to anti-cancer agents | In phase III clinical trials (AFFINITY) |
OGX427 (Apatorsen) | OncoGenex Pharmaceuticals | Second-generation antisense drug targeting HSP27 | In phase II clinical trials |
TAK-700 (Orteronel) | Takeda Pharmaceutical Company | Non-steroidal imidazole inhibitor of CYP17A1 | In phase III clinical trial |
TOK-001 (Galeterone) | Tokai Pharmaceuticals | CYP17 lyase inhibitor Competitive AR antagonist (binding to the steroid-binding pocket of AR) | Phase III randomized control trial (ARMOR3 trial) |
VT-464 | Viamet Pharmaceuticals | Non-steroidal CYP17 lyase inhibitor AR antagonist activity independent of CYP17 lyase inhibition | Phase II clinical trial |