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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.
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.
Naturally occurring phenethylamines are organic compounds which may be thought of as being derived from phenethylamine itself that are found in living organisms. Tyramine is a phenethylamine that occurs widely in plants [ 1 ] and animals , and is metabolized by various enzymes , including monoamine oxidases .
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 .
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Pages for logged out editors learn more. Contributions; Talk; Raloxifen
The study concluded that raloxifene caused fewer side-effects and less endometrial cancer than tamoxifen. [6] [7] Raloxifene was found to be more effective at preventing noninvasive breast cancer but less effective at preventing invasive breast cancer. [8]
Estradiol was used as a positive control and raloxifene was used because it is in the same drug class as ospemifene. [10] Multiple doses of oral ospemifene were tested. [10] 10 mg/kg/day of Ospemifene was found to cause a greater increase in vaginal weight and vaginal epithelial height than 10 mg/kg/day of raloxifene. [10]