The purpose of this review is to assimilate relevant experimental and clini
cal information available on selective estrogen receptor modulators with re
spect to their potential use as agents to improve women's health in the pos
tmenopausal years. In addition, the mechanisms of action of these drugs are
outlined. Selective estrogen receptor modulators represent an exciting gro
up of antiestrogens that possess agonist action on bone, lipids, and lipopr
oteins and antagonistic action in the endometrium and breast. Thus in theor
y these drugs may preserve bone density and reduce the risk of osteoporotic
fracture and coronary heart disease at the same time that they lower the i
ncidences of breast and endometrial neoplasms. Short-term data with the use
of raloxifene suggest that bone is preserved and lipid profiles are less a
therogenic. Long-term studies are needed to determine whether raloxifene or
other selective estrogen receptor modulators are associated with any decre
ase in the risk of breast or endometrial cancer.