Selective estrogen receptor
modulators (SERMs) exhibit a pharmacologic
profile characterized by estrogen agonist activity in some tissues with estrogen antagonist activity in other tissues. The first widely
used SERM, tamoxifen, has
estrogen antagonist activity in breast tissue but shows estrogen-like activity in other tissues. Raloxifene is another SERM in clinical use, and it was developed to avoid some of the undesirable estrogen agonist
actions of other SERMs to improve the drug safety
profile. Raloxifene has been
introduced for clinical use in treatment and prevention of postmenopausal osteoporosis.
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