Estrogen receptor modulators, alternative

Bryant HU, Dere WH (1998) Selective estrogen receptor modulators an alternative to hormone replacement therapy. Proc Soc Exp Biol Med 217 45-52... 

Calcitonin therapy results in decreased bone resorption. Osteoclasts have calcitonin receptors and calcitonin inhibits their activity. Sodium fluoride stimulates bone formation by unknown mechanisms. In women with osteoporosis, fluoride therapy produced an increased bone mineral density but no reduction in the rate of vertebral fractures. Other drugs known as selective estrogen receptor modulators (raloxifene, droloxifene, idoxifene, and levormeloxifene) may provide an alternative to estrogen replacement therapy (Chapter 34). Administration of low doses of PTH [or recombinant PTH( 1 -34)] does not affect serum calcium concentration, promotes bone formation, and increases mineral density. This anabolic action of PTH is probably mediated by decreasing osteoblast apoptosis. 

The clinical significance of the selective estrogen receptor modulators (SERMs) is well documented. The intensive research is currently directed at discovery of the ideal SERM , an agent that is antiestrogenic in breast and endometrial tissue, but pro-estrogenic in the vasculature and brain, which would be of use as a preventative in breast and uterine cancer and an alternate attractive HRT. Compound 1-(R) is a backup development candidate of the bisbenzopyran lead compound in our SERM program. This compound has shown promising preclinical profile with excellent pharmacokinetic properties. The identification and profiles of this novel SERM will be discussed. 

Cassanova J, Helmer E, Selmi-Ruby S, Qi JS, Au-Fliegner M, Desai-Yajnik V, Koudinova N, Yarm F, Raaka BM, Samuels HH (1994) Functional evidence for ligand-dependent dissociation of thyroid hormone and retinoic acid receptors from an inhibitory cellular factor. Mol Cell Biol 14 5756-5765 Bryant HU, Dere WH (1998) Selective estrogen receptor modulators an alternative to hormone replacement therapy. Proc Soc Exp Biol Med 217 45-52... 

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