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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.
Dora Nellie Richardson (1919-1998) was an organic chemist who first synthesised Tamoxifen in England in 1962. [1] She was born on 1 June 1919 and died in September 1998 in England. [2] Richardson decided to become a chemist after seeing people working in hospital laboratories while visiting her grandmother in hospital in London.
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.
The Study of Tamoxifen and Raloxifene (STAR) is a clinical trial from the early 2000s designed determine how the drug raloxifene compares with the drug tamoxifen in reducing the incidence of breast cancer in women who are at increased risk of the disease.
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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.