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Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonists/antagonists (ERAAs), [1] [2] are a class of drugs that act on estrogen receptors (ERs). [3] Compared to pure ER agonists – antagonists (e.g., full agonists and silent antagonists ), SERMs are more tissue-specific, allowing them to selectively inhibit or ...
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 ...
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 is a selective estrogen receptor modulator (SERM). [48] Even though it is an antagonist in breast tissue it acts as partial agonist on the endometrium and has been linked to endometrial cancer in some women. Therefore, endometrial changes, including cancer, are among tamoxifen's side effects. [49]
Tamoxifen is currently first-line treatment for nearly all pre-menopausal women with hormone receptor-positive breast cancer. [1] Raloxifene is another partial agonist SERM which does not seem to promote endometrial cancer , and is used primarily for chemoprevention of breast cancer in high-risk individuals, as well as to prevent osteoporosis ...
Endoxifen, also known as 4-hydroxy-N-desmethyltamoxifen, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group as well as a protein kinase C (PKC) inhibitor. It is under development for the treatment of estrogen receptor-positive breast cancer and for the treatment of mania in bipolar disorder.
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