Selective Androgen Receptor Modulators (SARMs): A Novel Approach to Androgen Therapy for the New Millennium

Extract

Androgen therapy, using injectable, oral and more recently, transdermal preparations, has been available to physicians for many years to treat a variety of male disorders; to a lesser degree, their use has been extended to some female indications. Unlike female sex hormone therapies, which have found extensive use and applications in the fields of hormone replacement, reproductive disorders, gynecological cancers, and contraception, androgen therapy has not been widespread.

A more widely accepted use of androgen therapy has been hampered by the lack of orally active preparations with good efficacy and, particularly, a safe profile. Progress has been limited over the last three decades in developing synthetic molecules that could separate androgenic activities considered desirable (i.e., anabolic) from others that were undesirable or had dose-limiting side effects (1). The abuse of synthetic anabolic steroids by athletes and body builders has contributed to the general perception of certain negative side effects (i.e., aggressive behavior), effects that we do not expect to see with replacement regimens of testosterone or other androgen receptor agonists that target judicious restoration of physiological functions normally regulated by endogenous androgens.