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The antiestrogen withdrawal response is a paradoxical improvement in breast cancer caused by discontinuation of antiestrogen ... tamoxifen and raloxifene. [1] [2 ...
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]
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.
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]
Where risks or harms is the reason for withdrawal, this will usually have been prompted by unexpected adverse effects that were not detected during Phase III clinical trials, i.e. they were only made apparent from postmarketing surveillance data collected from the wider community over longer periods of time.
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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.