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Raloxifene is used for the treatment and prevention of osteoporosis in postmenopausal women. [11] It is used at a dosage of 60 mg/day for both the prevention and treatment of osteoporosis. [12] In the case of either osteoporosis prevention or treatment, supplemental calcium and vitamin D should be added to the diet if daily intake is inadequate ...
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 .
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]
When the interactive distance between raloxifene and Asp-351 is increased from 2.7 Å to 3.5-5 Å it causes increased estrogen-like action of the raloxifene-ERα complex. When the piperidine ring of raloxifene is replaced by cyclohexane, the ligand loses antiestrogenic properties and becomes a full agonist. The interaction between SERM's ...
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]
The elimination half-life of toremifene is 3 to 7 days in healthy individuals. [1] In people with impaired liver function, the half-life is 11 days. [1] The elimination half-lives of the metabolites of toremifene are 5 to 21 days for N-desmethyltoremifene, 5 days for 4-hydroxytoremifene, and 4 days for ospemifene.
The antiestrogen withdrawal response is a paradoxical improvement in breast cancer caused by discontinuation of antiestrogen therapy for breast cancer. [1] [2] [3] [4 ...
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).