The identification of intracellular androgen synthesis by prostate cancer cells has led to the identification of new targets and the development of third generation drugs for the therapy of castration-resistant prostate cancer. Inhibitors of androgen synthesis and more potent androgen receptor antagonists, such as abiraterone acetate, MDV3100, TAK-700 and TOK-001, will improve treatment by prolongation of survival and palliation. A significant reduction of tumor-associated pain and a survival advantage of 4.6 months compared to placebo following docetaxel-based chemotherapy has already been shown for abiraterone in a phase III study. Further phase III studies with abiraterone, MDV3100 and TAK-700 before and after docetaxel-based chemotherapy are currently running. TOK-001 is the first of the new drugs which combines the therapeutic use of androgen synthesis inhibition and androgen receptor antagonism in a single drug. The first clinical studies with this therapy are currently being carried out and it remains to be seen whether this combination leads to increased effectiveness. With an increase in therapy options for prostate-resistant cancer, one of the projects in the coming years will be to integrate the present therapies into therapy concepts. In addition to an effective sequence of the individual medications, a combination with already established therapies, such as cytostatic agents, could also prove to be useful. Altogether, the development of new antihormonal therapies is a considerable expansion of the therapy options for patients which could contribute to an improvement of the quality of life and the prognosis of patients.