The medical treatment of endometriosis is a critical aspect of the therapeutic approach to this disease. Past methods have been based upon systemic hormonal alterations, resulting in suppression of this estrogen-responsive disorder. Treatments such as danazol, progestogens, oral contraceptives, GnRH-agonists, and gestrinone achieve their effects upon endometriosis via this method. However, with a growing understanding of the pathogenesis of this disease, more precise molecular targets for treatment have been identified. Thus, a series of newer agents are under development and hold the potential of greater efficacy and flexibility than traditional treatments. This review analyzes the available and experimental medical treatments of endometriosis, their utility in the treatment of pain and infertility, and their role in the future.