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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]
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 pure antiestrogenic trans-isomer and has differential actions at estrogen target tissues throughout the body. Tamoxifen is selectively antiestrogenic in the breast but estrogen-like in bones and endometrial cancer. [24] Tamoxifen undergo phase I metabolism in the liver by microsomal cytochrome P450 (CYP) enzymes.
N-Desmethyltamoxifen (developmental code name ICI-55,548) is a major metabolite of tamoxifen, a selective estrogen receptor modulator (SERM). [1] [2] N-Desmethyltamoxifen is further metabolized into endoxifen (4-hydroxy-N-desmethyltamoxifen), which is thought to be the major active form of tamoxifen in the body.
Jordan, V.C. A current view of tamoxifen for the treatment and prevention of breast cancer (Gaddum Memorial Lecture)" British Journal of Pharmacology 110:507-517, 1993. (257 citations as of May 26, 2021). Jordan, V.C. and Morrow, M.M. Tamoxifen, raloxifene and the prevention of breast cancer. Endocrine Reviews 20:253-278, 1999.
Great question that points to a weakness in this article. Tamoxifen's mechanism of action in breast cancer is as a estrogen receptor (ER) antagonist (especially through the ER-alpha isoform). In addition, breast cancers may become resistant to tamoxifen through mutations of the ER which convert tamoxifen from an antagonist into an agonist.
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 ...
Endoxifen is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant). [3] [4] [5] The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce endoxifen and afimoxifene (4-hydroxytamoxifen). [6]
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related to: tamoxifen at night archive list- 109 S High St #100, Columbus, OH · Directions · (614) 224-4261
GoodRx helps people pay for Rx they otherwise couldn't afford. - Patch