Bazedoxifene acetate (1-[4-(2-Azepan-1-yl-ethoxy)benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetate) is a third generation nonsteroidal selective estrogen receptor modulator (SERM), used clinically to treat postmenopausal osteoporosis and also being studied for possible treatment of breast cancer and pancreatic cancer. Bazedoxifene binds to estrogen receptor-α with IC50 = 26 nM, similar to that of raloxifene, but lower affinity than 17-β estradiol. Bazedoxifene did not stimulate proliferation of MCF-7 cells, instead inhibited 17β -estradiol-induced proliferation with IC50 = 0.19 nM, exhibiting a desirable profile of agonist/antagonist activity.
Design, synthesis, and preclinical characterization of novel, highly selective indole estrogens.
In vitro metabolism, permeability, and efflux of bazedoxifene in humans.
Relaxant Effects of the Selective Estrogen Receptor Modulator, Bazedoxifene, and Estrogen Receptor Agonists in Isolated Rabbit Basilar Artery.
The Tissue-Selective Estrogen Complex (Bazedoxifene/Conjugated Estrogens) for the Treatment of Menopause.
Effects of Bazedoxifene on Bone Mineral Density and Fracture in Post-Menopausal Osteoporotic Women: a Systematic Review and Meta-Analysis.
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