Table 1: Agents targeting AR in clinical development for CRPC.

DrugMechanism of actionPatient characteristicsPhase of developmentClinical trial registration number

MDV-3100AR antagonistChemotherapy-treatedPhase IIINCT00974311
Chemotherapy-naïvePhase IIINCT01212991
ARN-509AR antagonistNDPhase I-IINCT01171898
AZD3514AR antagonistNDPhase I-IINCT01162395
Abiraterone acetateCYP 17 inhibitorChemotherapy-treatedPhase IIINCT00638690
Chemotherapy-naïvePhase IIINCT00887198
Orteronel (TAK-700)CYP 17 inhibitorChemotherapy-treatedPhase IIINCT01193257
VN/124-1 (TOK-001)AR downregulating agent, CYP 17 inhibitor, and AR antagonistNDPhase I-IINCT00959959

ND: not defined.