Selective estrogen receptor modulators

What are Selective estrogen receptor modulators?

Selective estrogen receptor modulators are agents that bind to estrogen receptors but act either as agonists or antagonists in different tissues. For example, some selective estrogen receptor modulators act as agonists on the bone and uterus estrogen receptors, and antagonists on the breast estrogen receptors.

Growth of some forms of breast cancers is dependent on estrogen. Selective estrogen receptor modulators that act as antagonists on breast tissue are used in the treatment of breast cancer.

Estrogen is important in maintaining bone structure in women, so selective estrogen receptor modulators can also be useful in preventing post-menopausal osteoporosis.

Selective estrogen receptor modulators (SERMs) are hormone therapies that manage how estrogen works in your body. SERMs such as tamoxifen (Nolvadex®, Soltamox®) and raloxifene (Evista®) are effective treatments for some types of breast cancer and osteoporosis.

Two of the most common SERMs are tamoxifen (Nolvadex, Soltamox) and raloxifene (Evista). There are several others as well, including lasofoxifene, bazedoxifene, and clomiphene citrate. Keep reading to learn more about the types of SERMs and how they work to treat different conditions.

Selective estrogen receptor modulators (SERMs) are synthetic molecules which bind to estrogen receptors (ER) and can modulate its transcriptional capabilities in different ways in diverse estrogen target tissues. Tamoxifen, the prototypical SERM, is extensively used for targeted therapy of ER positive breast cancers.

The mechanism of action of SERDs involves binding to the estrogen receptor, leading to a conformational change that facilitates recruitment of cellular machinery to degrade the receptor protein.