Apalutamide (ErleadaTM) is a next-generation oral androgen receptor (AR) 
inhibitor that is being developed by Janssen for the treatment of prostate 
cancer (PC). It binds directly to the ligand-binding domain of the AR and blocks 
the effects of androgens. In February 2018, apalutamide received its first 
global approval in the USA for the treatment of non-metastatic 
castration-resistant PC (nmCRPC). Apalutamide is undergoing phase III 
investigation in chemotherapy-naive patients with metastatic CRPC (in 
combination with abiraterone acetate plus prednisone), patients with high-risk 
localized or locally advanced PC receiving primary radiation therapy, and in 
patients with metastatic hormone-sensitive PC and biochemically-relapsed PC. 
This article summarizes the milestones in the development of apalutamide leading 
to this first approval in nmCRPC.