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 estrogen receptor 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 of the estrogen receptor. They bind with the receptor and place it in a conformation that is intermediate between that found with estrogen and that found with the antiestrogens. As a result, parts of the receptor complex are blocked and other parts are put into play. The result is that in some tissues, SERMs activate the estrogen receptor, while in others they block it.

Clinical uses

SERMs are used for various estrogen-related diseases. Tamoxifen is used in the treatment of breast cancer, Raloxifene is used in the prevention of osteoporosis, and Clomifene (clomiphene) is used to treat infertility in women. Furthermore, they are also used in hormone replacement therapy for trans women.

Side effects

Like all drugs, SERMs can have side effects. Some of these include hot flashes, leg cramps, and an increased risk of developing certain types of uterine cancer. In rare cases, they can also cause blood clots or stroke.

Research

Research into the functions and potential uses for SERMs is ongoing. For example, they are being studied for their potential to help prevent breast cancer in women at high risk of the disease.

See also

• Estrogen receptor
• Estrogen
• Tamoxifen
• Raloxifene
• Clomifene