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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.
Lasofoxifene, sold under the brand name Fablyn, is a nonsteroidal selective estrogen receptor modulator (SERM) which is marketed by Pfizer in Lithuania and Portugal for the prevention and treatment of osteoporosis and for the treatment of vaginal atrophy, [1] [2] and the result of an exclusive research collaboration with Ligand Pharmaceuticals (LGND).
One of the largest breast cancer prevention studies ever, [2] it included 22,000 women in 400 medical centers in the United States and Canada. [3] [4] [5]The study concluded that raloxifene caused fewer side-effects and less endometrial cancer than tamoxifen.
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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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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]
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