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Raloxifene is widely distributed throughout the body. [3] There is extensive distribution of raloxifene into the liver, serum, lungs, and kidneys. [3] The volume of distribution of raloxifene with a single 30 to 150 mg oral dose is approximately 2348 L/kg, which corresponds to ~170,000 L for a 72 kg person.
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 .
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 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]
The antiestrogen withdrawal response is a paradoxical improvement in breast cancer caused by discontinuation of antiestrogen therapy for breast cancer. [1] [2] [3] [4 ...
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.
Levels of 4-hydroxytoremifene at steady state with toremifene were 438 ng/mL at 200 mg/day and 889 ng/mL at 400 mg/day. [1] Concentrations of toremifene increase linearly across a dose range of 10 to 680 mg. [ 37 ] [ 38 ]
Raloxifene alone: 1.49 (1.24–1.79)* ... The developmental code name SH-81041 referred to a combination of high-dose 100 mg CPA and 40–50 μg EE administered in ...