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Selective Estrogen Receptor Modulators (SERMs)

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Osteoporotic Fracture and Systemic Skeletal Disorders

Abstract

Selective Estrogen Receptor Modulators (SERMs) are tissue-specific mild anti-remodeling agents that were developed to avoid some of the adverse problems created by estrogen-based hormone replacement therapies. Several have been approved to prevent breast cancer and for their positive effects on the cardiovascular system. Although they have a limited effect on increasing bone mineral density, they are effective in significantly reducing vertebral fractures. In general, they have not been shown to be effective in preventing non-vertebral fractures. This chapter focuses primarily on two SERMs approved to treat osteoporosis, raloxifene and bazedoxifene, as well as Duavee, a combination of conjugated estrogen and bazedoxifene. A dual mechanism of action has been identified for raloxifene: it both suppresses bone resorption and has a cell-independent physical effect on bone matrix by increasing the bound fraction of bone water, which improves bone toughness. Whether this dual action also applies to other SERMs is unknown.

The present invited review was completed and submitted to the publisher on 05-Aug-19. 

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Burr, D.B., Phipps, R. (2022). Selective Estrogen Receptor Modulators (SERMs). In: Takahashi, H.E., Burr, D.B., Yamamoto, N. (eds) Osteoporotic Fracture and Systemic Skeletal Disorders. Springer, Singapore. https://doi.org/10.1007/978-981-16-5613-2_26

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  • DOI: https://doi.org/10.1007/978-981-16-5613-2_26

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