Selective Estrogen Receptor Modulators (SERMs)

Compared to estrogens or estradiol, SERMS comprise a structurally heterogeneous group of compounds that interact with intracellular estrogen receptors in a unique tissue specific manner. SERMs have been designed to elicit the beneficial aspects of estrogen treatment or block non-beneficial actions in specific target tissues. Compared with conjugated estrogens and some other SERMS, ospemifene has unique action to estrogen alpha receptors in the vaginal tissue. This allows for ospemifene to have more targeted action on vaginal tissue. In contrast, prasterone (DHEA) is a steroid precursor to testosterone and estrogen. Prasterone is applied through a vaginal insert and metabolized locally, which is thought to limit the site of action.