The discovery of endocrine therapy of diseases of the prostate can be regarded as one of the most important events in the history of medicine and in urology in particular. This article delivers an overview about scientists and clinicians involved in this work during the last 200 years. A close historical relation between the endocrine therapy of benign prostatic hyperplasia and prostate cancer can be recognized. The historical framework between the work of John Hunter in the late eighteenth century, that of Charles Brenton Huggins in the late 1930s, and that of Andrew Schally in the 1970s has been assembled herein. With respect to all the other men who contributed greatly to this medical achievement, e.g., Edward L. Keyes and Russell S. Ferguson, with their first report on radioorchiectomy for the treatment of metastatic prostate cancer in 1936, this historical vignette is intended to make them part of the historical record.