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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]
Tamoxifen is a SERM and is one of the most common and oldest forms of hormone therapy. [8] When breast cancer is found at an early stage or found to be Metastatic breast cancer, tamoxifen can be prescribed to selectively block estrogen's effect on certain cells. SERMs like tamoxifen attach to receptors on the cancer cells which blocks estrogen ...
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.
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.
The most commonly prescribed SERMs are raloxifene and tamoxifen. Raloxifene exhibits oestrogen agonist activity on bone and lipids, and antagonist activity on breast and the endometrium. [90] Tamoxifen is in widespread use for treatment of hormone sensitive breast cancer.
Hormone replacement therapy (HRT), also known as menopausal hormone therapy (MHT), is for women with menopausal symptoms. It is based on the idea that the treatment may prevent discomfort caused by diminished circulating estrogen and progesterone hormones, or in the case of the surgically or prematurely menopausal, that it may prolong life and may reduce incidence of dementia. [1]
Tamoxifen acts indirectly to inhibit ER signaling in breast cancer cells. ... Tamoxifen is routinely and very commonly prescribed for treating all stages of MBC ...
In 2022, it was the 50th most commonly prescribed medication in the United States, with more than 12 ... (SERM) tamoxifen. ...