Estrogen receptor antagonists

What are Estrogen receptor antagonists?

Estrogen receptor antagonists bind to estrogen receptors and inhibit the action of estrogen. Estrogen controls the growth of certain types of breast cancers called estrogen receptor positive cancers. So estrogen receptor antagonists are useful in treating patients with estrogen sensitive breast cancers.

Some estrogen receptor antagonists are approved by FDA like fareston, faslodex, soltamox, tamoxifen, toremifene. These drugs currently observing with a problem like blood clots, stroke, endometrial cancer, osteoporosis, breast atrophy, and vaginal atrophy.

Estrogen agonists/antagonists, also referred to as selective estrogen-receptor (ER) modulators (SERMs), are one group of compounds that are being used or evaluated for both osteoporosis prevention and treatment and breast cancer prevention in women at risk for breast cancer.

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.

Tamoxifen is the most widely used drug in breast cancer treatment. Other antiestrogenic-active substances are anastrozole, raloxifene, cyclofenil, and clomiphene. In sports, they can be used for the treatment of adverse effects of anabolic steroid abuse such as gynecomastia and reduced testosterone production.

An estrogen antagonist is defined as a compound that produces only estrogen antagonistic effects in various tissues. It is used in the treatment of breast cancer, particularly in women who have progressed after tamoxifen therapy.