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SERMs and SERMs with estrogen for postmenopausal osteoporosis
1Bethesda Health Research, Bethesda, MD, USA. mbolognese@erols.com
Reviews in Endocrine & Metabolic Disorders
|May 7, 2010
Summary
Selective Estrogen Receptor Modulators (SERMs) offer new avenues for treating postmenopausal osteoporosis, aiming to mimic estrogen
Area of Science:
- Endocrinology and Bone Metabolism
- Pharmacology of Estrogen Receptor Modulators
Background:
- Postmenopausal osteoporosis affects millions globally, increasing fracture risk and mortality.
- Current treatments like Hormone Replacement Therapy (HRT) have safety concerns, necessitating novel approaches.
- Selective Estrogen Receptor Modulators (SERMs) present a diverse class of drugs with unique clinical profiles.
Purpose of the Study:
- To review approved and investigational Selective Estrogen Receptor Modulators (SERMs) for postmenopausal osteoporosis.
- To discuss the potential of Tissue Selective Estrogen Complexes (TSEC) as a novel therapeutic strategy.
Main Methods:
- Review of approved SERMs (tamoxifen, raloxifene) and investigational agents.
- Discussion of the mechanism of action and clinical responses of SERMs.
- Exploration of the TSEC concept and its evaluation with bazodoxifene.
Main Results:
- SERMs exhibit varied interactions with the estrogen receptor, leading to distinct tissue-specific effects.
- The ideal SERM would provide estrogenic benefits in bone, heart, and CNS while antagonizing effects in breast and endometrium.
- Tissue Selective Estrogen Complexes (TSEC) combine SERMs with conjugated estrogens to optimize therapeutic outcomes.
Conclusions:
- SERMs represent a promising therapeutic class for managing postmenopausal bone loss.
- TSEC, exemplified by bazodoxifene, offers a novel approach to achieve beneficial estrogenic effects with potentially improved safety and tolerability.
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