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Raloxifene is a selective estrogen receptor modulator (SERM) and therefore a mixed agonist–antagonist of the estrogen receptor (ER). [6] It has estrogenic effects in bone and antiestrogenic effects in the breasts and uterus. [6] Raloxifene was approved for medical use in the United States in 1997. [6] It is available as a generic medication.
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.
Raloxifene belongs to the second-generation benzothiophene SERM drugs. It has a high affinity for the ER with potent antiestrogenic activity and tissue-specific effects distinct from estradiol. [19] Raloxifene is an ER agonist in bone and the cardiovascular system, but in breast tissue and the endometrium it acts as an ER antagonist.
Estradiol/raloxifene (E2/RLX) is a tissue-selective estrogen complex (TSEC) which was studied for potential use in menopausal hormone therapy but was never marketed. [ 2 ] [ 1 ] [ 3 ] [ 4 ] [ 5 ] Today, E2/RLX is not generally used due to concerns of endometrial hyperplasia .
Therapeutic use exemption (TUE) is a term used by WADA and the United States Anti-Doping Agency to denote banned substances that athletes may be "required to take to treat an illness or condition". [12] [13] These exemptions are regulated by the International Standard for Therapeutic Use Exemptions (ISTUE). The detection of such substances in ...
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.
As finasteride use by younger men soars, some doctors caution about rare side effects. Akshay Syal, M.D. June 9, 2024 at 7:00 AM. NBC News / Getty Images (NBC News)
The antiestrogen withdrawal response is a paradoxical improvement in breast cancer caused by discontinuation of antiestrogen therapy for breast cancer. [1] [2] [3] [4 ...
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