Selective estrogen receptor modulator

Selective estrogen receptor modulators (SERMs) are a class of drugs that act on the estrogen receptor. A characteristic that distinguishes these substances from pure agonists and antagonists is that their action is different in various tissues, thereby granting the possibility to selectively inhibit or stimulate estrogen-like action in various tissues.

Mechanism of action

SERMs are competitive partial agonists for the estrogen receptor. They bind to the estrogen receptor and hold it in a conformation that is intermediate between that induced by full agonists and that induced by antagonists. As a result, parts of the receptor binding site that are exposed in the presence of an antagonist, but not in the presence of an agonist, are covered up, and vice versa.

Uses

SERMs are used for various estrogen-related diseases. Tamoxifen is used in the treatment of hormone receptor-positive breast cancer, while raloxifene is used for preventing osteoporosis in postmenopausal women. Other examples of SERMs include clomifene, toremifene, and ospemifene.

Side effects

Possible side effects of SERMs include hot flashes, leg cramps, and an increased risk of blood clots and other cardiovascular events. The risk of endometrial cancer may be slightly increased in women taking tamoxifen.

See also

• Estrogen receptor
• Estrogen
• Receptor antagonist
• Receptor agonist

References

Selective estrogen receptor modulator Resources
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