List of selective estrogen receptor modulators

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Selective estrogen receptor modulators (SERMs) are a class of compounds that act on the estrogen receptor. A unique feature of SERMs is that their action is different in various tissues, which means they can act as estrogen receptor agonists in some tissues and antagonists in others. This property makes them useful in a variety of clinical applications, including the treatment of breast cancer, osteoporosis, and menopausal symptoms.

Common SERMs

• Tamoxifen - One of the most well-known SERMs, tamoxifen is primarily used in the treatment and prevention of breast cancer. It acts as an estrogen antagonist in breast tissue but can act as an agonist in other tissues such as the endometrium.
• Raloxifene - This SERM is used mainly for the prevention and treatment of osteoporosis in postmenopausal women. It also reduces the risk of invasive breast cancer.
• Toremifene - Similar to tamoxifen, toremifene is used in the treatment of metastatic breast cancer.
• Bazedoxifene - Used in combination with conjugated estrogens for the treatment of menopausal symptoms and the prevention of postmenopausal osteoporosis.
• Ospemifene - This SERM is used to treat moderate to severe dyspareunia, a symptom of vulvar and vaginal atrophy due to menopause.

Mechanism of Action

SERMs bind to estrogen receptors and exert their effects by modulating the receptor's activity. The differential action of SERMs in various tissues is due to the presence of different co-regulators (co-activators and co-repressors) that interact with the estrogen receptor in a tissue-specific manner. This allows SERMs to mimic or block the effects of estrogen in a tissue-dependent manner.

Clinical Applications

• Breast Cancer - SERMs like tamoxifen and toremifene are used to treat and prevent breast cancer by blocking estrogen's proliferative action on breast tissue.
• Osteoporosis - Raloxifene and bazedoxifene are used to prevent and treat osteoporosis by mimicking estrogen's bone-preserving effects.
• Menopausal Symptoms - Bazedoxifene, in combination with conjugated estrogens, is used to treat menopausal symptoms such as hot flashes and to prevent osteoporosis.
• Dyspareunia - Ospemifene is used to treat dyspareunia, a symptom of vulvar and vaginal atrophy due to menopause.

Side Effects

The side effects of SERMs can vary depending on the specific agent and the tissue in which it acts. Common side effects include hot flashes, leg cramps, and an increased risk of venous thromboembolism. Some SERMs, like tamoxifen, can also increase the risk of endometrial cancer due to their agonistic effects on the endometrium.

Related Pages

• Estrogen receptor
• Breast cancer
• Osteoporosis
• Menopause
• Hormone replacement therapy

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