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Toremifene, sold under the brand name Fareston among others, is a medication which is used in the treatment of advanced breast cancer in postmenopausal women. [4] [6] [3] It is taken by mouth. [4] Side effects of toremifene include hot flashes, sweating, nausea, vomiting, dizziness, vaginal discharge, and vaginal bleeding.
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.
Estrogen deprivation therapy, also known as endocrine therapy, is a form of hormone therapy that is used in the treatment of breast cancer.Modalities include antiestrogens or estrogen blockers such as selective estrogen receptor modulators (SERMs) like tamoxifen, selective estrogen receptor degraders like fulvestrant, and aromatase inhibitors like anastrozole and ovariectomy.
Tamoxifen is also thought to lower the risk of breast cancer in those who have a predisposition or at risk. [9] Tamoxifen may be used in pre and postmenopausal women. [10] Toremifene is a similar SERM drug to tamoxifen, but is less common and only approved for treatment of metastatic cancer. Toremifene is generally prescribed once tamoxifen is ...
[11] [7] Peak levels of tamoxifen after a single 40 mg oral dose were 65 ng/mL and steady state levels at 20 mg/day were 310 ng/mL. [5] Levels of tamoxifen show clear dose dependency across a dosage range of 1 to 20 mg/day. [5] [93] Endoxifen levels are approximately 5 to 10 times higher than afimoxifene levels, with large interindividual ...
A nonsteroidal estrogen is an estrogen with a nonsteroidal chemical structure. [1] The most well-known example is the stilbestrol estrogen diethylstilbestrol (DES). [1] [2] Although nonsteroidal estrogens formerly had an important place in medicine, they have gradually fallen out of favor following the discovery of toxicities associated with high-dose DES starting in the early 1970s, and are ...
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.
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.
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