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Toremifene appears to be safer than tamoxifen. [15] It has a lower risk of venous thromboembolism (VTE) (e.g., pulmonary embolism), stroke, and cataracts. [15] The lower risk of VTE may be related to the fact tamoxifen decreases levels of the antithrombin III to a significantly greater extent than either 60 or 200 mg/day toremifene. [15]
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.
Afimoxifene, also known as 4-hydroxytamoxifen (4-OHT) and by its tentative brand name TamoGel, is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and an active metabolite of tamoxifen. [1] [2] [3] The drug is under development under the tentative brand name TamoGel as a topical gel for the treatment of hyperplasia ...
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 ...
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]
[20] [14] Raloxifene has a lower risk of thromboembolism than tamoxifen. [15] In the MORE trial, raloxifene caused a 40% decrease in risk of cardiovascular events in women who were at increased risk for coronary artery disease, although there was no decrease in cardiovascular events for the group as a whole. [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.
Clomifene is a prodrug being activated via similar metabolic pathways as the related triphenylethylene SERMs tamoxifen and toremifene. [36] [37] The affinity of clomifene for the ER relative to estradiol ranges from 0.1 to 12% in different studies, which is similar to the range for tamoxifen (0.06–16%).
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