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[6] [8] [9] [5] It is a triphenylethylene derivative and is closely related to tamoxifen. [10] Toremifene was introduced for medical use in 1997. [11] [12] It was the first antiestrogen to be introduced since tamoxifen in 1978. [13] It is available as a generic medication in the United States. [14]
This list contains 1200 recommendations for 591 drugs and 103 therapeutic equivalents. [20] A separate list for children up to 12 years of age, known as the WHO Model List of Essential Medicines for Children (EMLc), was created in 2007 and is in its 9th edition.
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.
Footnotes: a = No longer used or recommended, due to health concerns. b = As a single patch applied once or twice per week (worn for 3–4 days or 7 days), depending on the formulation. Note: Dosages are not necessarily equivalent.
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 has been found to decrease insulin-like growth factor 1 (IGF-1) levels by 17 to 38% in women and men. [85] Suppression of IGF-1 production in the liver is a well-known action of estrogens and SERMs. [85] A 10 mg/day dosage of tamoxifen is nearly as effective as a 20 mg/day dosage in suppressing IGF-1 levels. [5]
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 ...
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