ABSTRACT

Prostate cancer (PC) is the second-most frequently diagnosed cancer in men worldwide, with 1.1 million new cases estimated to have occurred in 2012. Chemoprevention, prostate-specific antigen screening for early detection, and innovative treatments for advanced PC are necessary to reduce the resultant mortality due to PC. Systematic treatment for advanced or metastatic PC includes androgen deprivation therapy (ADT) or chemotherapy. Conventional ADT involved surgical or medical castration and the administration of anti-androgen agents, such as bicalutamide, flutamide, and nilutamide. Selective estrogen modulators (SERMs) are involved in major therapeutic advancements in clinical practice for breast cancer, osteoporosis, and PC. Initially, the action of estrogens was believed to be mediated via the blockade of the pituitary–testicular axis, which effectively decreased circulating androgen levels and induced tumor regression. SERMs are synthetic ligands for estrogen receptors that can exhibit either estrogenic or anti-estrogenic effects, depending on the tissue type.