Chapter 17. Selective androgen receptor modulators (SARMs)

Publisher Summary This chapter examines the different aspects of selective androgen receptor modulators (SARMS). Testosterone (T) is an endogenous ligand for the androgen receptor (AR) and is essential for the development and maintenance of the male reproductive system and secondary male sex characteristics. SARMs with agonist activity in most target tissues but the prostate and other SARMs with antagonist activity only in prostate are likely to fulfill important unmet medical needs for a growing aging population. The discovery and development of SARMs can provide tissue-specific molecules for a specific indication. The therapeutic potential of SARMs should be expanded beyond the current androgen applications with better or total separation of the anabolic and androgenic activities of androgens. The AR is expressed in rat neurons and 5α- dihydrotestosterone upregulates neural AR in mice and rats. In the hamster, androgen was found to affect neural development in the hypothalamus and amygdala. A study reported that androgens at pharmacological doses increased serum erythropoietin (EPO) levels in anemic patients with non-severe aplastic anemia and myelodysplastic syndromes but not in non-anemic patients.