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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