Selective estrogen receptor modulator
Selective Estrogen Receptor Modulator
A Selective Estrogen Receptor Modulator (SERM) is a type of drug that acts on the estrogen receptor. Pronounced as /sɪˈlɛktɪv ˈɛstrədʒən rɪˈsɛptər ˈmɒdʒəleɪtər/, the term is derived from the English words "selective" meaning to choose or make a selection, "estrogen" which is a primary female sex hormone, "receptor" referring to a protein molecule that receives chemical signals from outside a cell, and "modulator" meaning something that affects or controls the operation of a system or machine.
Mechanism of Action
SERMs are competitive partial agonists of the estrogen receptor. They bind to the estrogen receptor and change its conformation, which can either enhance or inhibit the effects of estrogen on a tissue-specific basis. This mechanism of action allows SERMs to have both estrogenic and antiestrogenic effects, depending on the tissue.
Uses
SERMs are used in the treatment of various conditions, including breast cancer, osteoporosis, and menopausal symptoms. They can also be used in fertility treatments as they can stimulate the release of gonadotropins.
Examples
Examples of SERMs include tamoxifen, raloxifene, and clomifene. Each of these drugs has a different profile of estrogenic and antiestrogenic effects, which makes them suitable for different clinical applications.
Side Effects
Common side effects of SERMs include hot flashes, vaginal dryness, and nausea. More serious side effects can include an increased risk of blood clots and endometrial cancer.
See Also
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