Bazedoxifene (TSE-424; Figure 10) is a novel SERM developed by Wyeth Pharmaceuticals that is currently in phase III clinical trials for the prevention and treatment of postmenopausal osteoporosis. It is an indole-based estrogen receptor ligand that has been stringently selected to ensure an improved profile over its predecessor raloxifene. It was developed using preclinical selection parameters, which included favorable effects on the skeleton and lipid metabolism, demonstrable mammary and uterine safety, and neutral effects on hot flashes.192 Bazedoxifene treatment maintains bone mineral density, preserves normal bone histology, increases bone compressive strength, and reduces total cholesterol levels in animal models.192-194 It lacks uterotropic activity194 and it blocks raloxifene-induced increases in uterine weight192 and inhibits E2-induced proliferation in MCF-7 breast cancer cells.192 Based on the favorable preclinical evaluation, it is suggested that bazedoxifene has the potential to improve the SERM profile beyond that achieved by raloxifene.
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