Enzalutamide: A new prostate cancer targeted therapy against the androgen receptor

• The AR signalling pathway is a crucial element in the natural history of mCRPC.
• Enzalutamide has a much higher binding affinity to the AR than the other anti-androgenic drugs.
• Health-related quality of life is an important goal in the treatment of an incurable disease such as mCRPC.
• Enzalutamide appear to be better tolerated and it does not have the risk of corticosteroids-related complications.

Enzalutamide (MDV3100), an androgen receptor-signalling inhibitor, represents the most recent compound added to the therapeutic armamentarium for the treatment of metastatic castration-resistant prostate cancer (mCRPC) who progressed to docetaxel. The anti-tumour activity and safety of enzalutamide has been demonstrated in a phase III clinical trial, showing a benefit in overall survival, which was the primary endpoint. There are no head-to-head studies comparing the different treatment options in this subset of patients. In this article, most relevant data published in the literature have been reviewed, with special attention to the therapeutic alternatives currently available for postdocexatel mCRPC patients, emphasising the mechanisms of action of the different drugs, efficacy and quality of life-related aspects.