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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 ...
Estrogen deprivation therapy, also known as endocrine therapy, is a form of hormone therapy that is used in the treatment of breast cancer.Modalities include antiestrogens or estrogen blockers such as selective estrogen receptor modulators (SERMs) such as tamoxifen, selective estrogen receptor degraders such as fulvestrant, and aromatase inhibitors such as anastrozole and ovariectomy.
Tamoxifen, sold under the brand name Nolvadex among others, is a selective estrogen receptor modulator used to prevent breast cancer in women and men. [15] It is also being studied for other types of cancer. [15] It has been used for Albright syndrome. [16] Tamoxifen is typically taken daily by mouth for five years for breast cancer. [16]
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]
Afimoxifene, also known as 4-hydroxytamoxifen (4-OHT) and by its tentative brand name TamoGel, is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and an active metabolite of tamoxifen. [1] [2] [3] The drug is under development under the tentative brand name TamoGel as a topical gel for the treatment of hyperplasia ...
In the field of pharmacology, a selective receptor modulator or SRM is a type of drug that has different effects in different tissues. [1] A SRM may behave as an agonist in some tissues while as an antagonist in others. Hence selective receptor modulators are sometimes referred to as tissue selective drugs or mixed agonists / antagonists. This ...
Perhaps the most familiar example of hormonal therapy in oncology is the use of the selective estrogen-response modulator tamoxifen for the treatment of breast cancer, although another class of hormonal agents, aromatase inhibitors, now have an expanding role in that disease.
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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