In the contemporary scene, less than 5% of men with newly diagnosed prostate cancer (PC) have metastases at first presentation, compared to 20-25%, more than 20 years ago. Nonetheless, the use of androgen deprivation therapy (ADT) has increased over the years, suggesting that patients in Europe and United States may receive ADT in cases of lower disease burden, and not always according to evidence based indications. Nonetheless, PC remains the second most common cause of cancer death after lung cancer in American men. Thus, there is a need for more effective, specific and well tolerated agents which can provide a longer and good quality of life while avoiding the side effects related to disease and treatment morbidity.After mentioning the current knowledge on the endocrinology of androgens and androgen receptor, relevant to PC development, as well as the possible events occurring during PC initiation, we will compare different hormonal compounds available for the treatment of PC, both from a pharmacological standpoint, and in terms of contemporary clinical indications.