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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.
[6] [15] Toremifene has been found to be effective in the treatment of breast pain and may be a more effective medication than tamoxifen for this indication. [16] It also has superior effects on bone mineral density and lipid profile , including levels of cholesterol and triglycerides , compared to tamoxifen. [ 15 ]
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.
Medication discontinuation is the ceasing of a medication treatment for a patient by either the clinician or the patient themself. [1] [2] When initiated by the clinician, it is known as deprescribing. [3] Medication discontinuation is an important medical practice that may be motivated by a number of reasons: [4] [3] Reducing polypharmacy
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]
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.