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It was approved for prevention and treatment of osteoporosis and was the first clinically available SERM to prevent both osteoporosis and breast cancer. [7] Ospemifene was approved on February 26, 2013, for the treatment of moderate to severe dyspareunia , which is a symptom, due to menopause , of vulvar and vaginal atrophy .
Sivifene (A-007) was initially thought to be a SERM due to its structural similarity to tamoxifen but it was subsequently found not to bind to the estrogen receptor (ER). [8] Tesmilifene (DPPE; YMB-1002, BMS-217380-01) is also structurally related to tamoxifen but similarly does not bind to the ER and is not a SERM. [9] [10]
Tamoxifen, sold under the brand name Nolvadex among others, is a selective estrogen receptor modulator used to prevent breast cancer in women and men. [13] It is also being studied for other types of cancer. [13] It has been used for Albright syndrome. [14] Tamoxifen is typically taken daily by mouth for five years for breast cancer. [14]
It is a third-generation selective estrogen receptor modulator (SERM). [3] Since late 2013 it has had U.S. FDA approval for bazedoxifene as part of the combination drug Duavee in the prevention (not treatment) of postmenopausal osteoporosis. It is also being studied for possible treatment of breast cancer and pancreatic cancer. [4]
The medication is a selective estrogen receptor modulator (SERM) and hence is a mixed agonist–antagonist of the estrogen receptor (ER), the biological target of estrogens like estradiol. [ 5 ] [ 7 ] It has estrogenic effects in bone , the liver , and the uterus and antiestrogenic effects in the breasts .
Tamoxifen is also thought to lower the risk of breast cancer in those who have a predisposition or at risk. [9] Tamoxifen may be used in pre and postmenopausal women. [10] Toremifene is a similar SERM drug to tamoxifen, but is less common and only approved for treatment of metastatic cancer. Toremifene is generally prescribed once tamoxifen is ...
A tissue-selective estrogen complex (TSEC) is a combination of an estrogen, such as estradiol or conjugated estrogens, and a selective estrogen receptor modulator (SERM), such as tamoxifen, raloxifene, or bazedoxifene. [1]
[4] [5] [6] It contains the selective estrogen receptor modulator bazedoxifene and conjugated estrogens. It is taken by mouth . The combination was approved for medical use in the United States in October 2013, [ 7 ] and in the European Union in December 2014.