The first modern description of prostate cancer was made in 1853 and until the 1900’s was considered a rare disease. The discovery of the effect of castration and oestrogen on prostate cancer, made by Huggins and Hodges in the 1940’s, paved the way for more modern prostate cancer management, including the development of luteinising hormone releasing hormone analogues, antagonists and antiandrogens that are commonly used today. This chapter discusses the key historical discoveries in pharmacological management of prostate cancer which provides a foundation for modern therapeutic strategies.