Introduction: Prostate cancer is the second leading cause of cancer death in men in the United States. The disease is driven by androgen receptor (AR) signaling, and the majority of patients initially respond to androgen deprivation therapies. The lethal form of this disease occurs when metastatic lesions progress in the setting of low testosterone levels, in what is conventionally referred to as castration-resistant prostate cancer (CRPC). Recent insights suggest that CRPC continues to rely on an active AR pathway for cell survival and growth. Areas covered: This review summarizes the rationale, mechanism of action and relevant clinical data of abiraterone acetate, an oral androgen biosynthesis inhibitor, in the management of CRPC. Expert opinion: Abiraterone acetate is an oral, well-tolerated drug that targets a newly elucidated paradigm of continued AR activation in CRPC. Abiraterone acetate is approved in CRPC patients who have received docetaxel, and recent data suggest that the drug will also be effective and utilized in the pre-chemotherapy setting. Significant areas of scientific investigation remain in the optimization and further understanding of the therapy.