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[6] [8] [9] [5] It is a triphenylethylene derivative and is closely related to tamoxifen. [10] Toremifene was introduced for medical use in 1997. [11] [12] It was the first antiestrogen to be introduced since tamoxifen in 1978. [13] It is available as a generic medication in the United States. [14]
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.
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 ...
Tamoxifen was initially made in 1962, by chemist Dora Richardson. [17] [18] It is on the World Health Organization's List of Essential Medicines. [19] Tamoxifen is available as a generic medication. [14] In 2020, it was the 317th most commonly prescribed medication in the United States, with more than 900 thousand prescriptions. [20] [21]
Antiestrogens include selective estrogen receptor modulators (SERMs) like tamoxifen, clomifene, and raloxifene, the ER silent antagonist and selective estrogen receptor degrader (SERD) fulvestrant, [6] [7] aromatase inhibitors (AIs) like anastrozole, and antigonadotropins including androgens/anabolic steroids, progestogens, and GnRH analogues.
This is a complete list of estrogens and formulations that are approved by the FDA Tooltip Food and Drug Administration and available in the United States. Estrogens are used as hormonal contraceptives, in hormone replacement therapy, and in the treatment of gynecological disorders.
The drug also counteracts gynecomastia as well as fat and water retention following excessive aromatase production due to testosterone doping. [17] It is also used by steroid users to lower female sexual horomone levels following a cycle of steroids, often called a "post-cycle therapy", it is also used alongside Selective estrogen receptor ...
Bazedoxifene, used as bazedoxifene acetate, is a medication for bone problems and possibly (pending more study) for cancer. [2] It is a third-generation selective estrogen receptor modulator (SERM). [3]
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