Since 2010, six drugs have been approved for the treatment of 
castration-resistant prostate cancer, i.e., CYP17 inhibitor Abiraterone, 
androgen receptor antagonist Enzalutamide, cytotoxic agent Cabazitaxel, vaccine 
Sipuleucel-T, antibody Denosumab against receptor activator of nuclear factor 
kappa B ligand and radiopharmaceutical Alpharadin. All these drugs demonstrate 
improvement on overall survival, expect for Denosumab, which increases the bone 
mineral density of patients under androgen deprivation therapy and prolongs 
bone-metastasis-free survival. Besides further CYP17 inhibitors (Orteronel, 
Galeterone, VT-464 and CFG920), androgen receptor antagonists (ARN-509, ODM-201, 
AZD-3514 and EZN-4176) and vaccine Prostvac, more drug candidates with various 
mechanisms or new indications of launched drugs are currently under evaluation 
in different stages of clinical trials, including various kinase inhibitors and 
platinum complexes. Some novel strategies have also been proposed aimed at 
further potentiation of antitumor effects or reduction of side effects and 
complications related to treatments. Under these flourishing circumstances, more 
investigations should be performed on the optimal combination or the sequence of 
treatments needed to delay or reverse possible resistance and thus maximize the 
clinical benefits for the patients.