Given the global incidence of prostate cancer and its sociological impact, it remains a challenging disease to clinicians and researchers alike. In the last few years several new drugs have been added to the armamentarium of prostate cancer therapy and offers survival benefit to patients with prostate cancer. However, effective drugs are still needed that offer extended survival benefit and alter the natural history of the disease. Recent efforts have focused on better understanding the underlying biology and genetic heterogeneity of the disease and identified novel targets that can be utilized for drug development and therapeutics in the future. In this review we present an overview of the genetic landscape of prostate cancer, novel targets in the prostate cancer therapy and the results of key clinical trials of these novel drugs.