Selective estrogen receptor modulators and bone health

Abstract

Selective estrogen receptor modulators (SERMs) are synthetic molecules that bind to the estrogen receptor and can have agonistic activity in some tissues while being estrogen antagonistic in others. While not all SERMs are clinically available in all parts of the world, this article will review preclinical and clinical effects of various SERMs on bone. These include tamoxifen, used as adjuvant therapy in breast cancer patients as well as for breast cancer prevention; raloxifene, approved for osteoporosis prevention and treatment as well as breast cancer prevention; bazedoxifene, approved for prevention of osteoporosis and also in combination with conjugated equine estrogen for treatment of vasomotor symptoms and prevention of bone loss in postmenopausal patients; and ospemifene, approved for treatment of dyspareunia due to vulvovaginal atrophy/genitourinary syndrome of menopause. Thus, these SERMs are a diverse group of estrogen agonist/antagonists that seem to have class effects in the bone and breast, although the amount of clinical trial data is quite variable. However, there does not seem to be the same unidirectional class activity in tissues like the uterus or vagina. Health-care providers should be cognizant of all available information in helping patients make the best possible shared decision-making choices.

选择性雌激素受体调节剂与骨健康 摘要

选择性雌激素受体调节剂(SERMs)是与雌激素受体结合的合成分子, 在某些组织中具有激动活性, 而在其他组织中具有雌激素拮抗作用。虽然并非所有的选择性雌激素受体调节剂在世界各地都有临床应用, 但本文将回顾各种选择性雌激素受体调节剂对骨的临床前和临床影响。这些药物包括他莫西芬, 用于乳腺癌患者的辅助治疗以及乳腺癌预防;雷洛昔芬, 被批准用于骨质疏松症的预防和治疗以及乳腺癌的预防;巴多昔芬, 被批准用于预防骨质疏松症, 也可与雌激素结合用于治疗绝经后患者的血管舒缩症状和预防骨质流失;还有奥培米芬, 被批准用于治疗由于外阴阴道萎缩/泌尿生殖系统综合症引起的更年期性交困难。因此, 这些选择性雌激素受体调节剂是一组不同类型的雌激素激动剂/拮抗剂, 似乎在骨骼和乳房中有同类效应, 尽管临床试验数据的数量相当不同。然而, 在子宫或阴道等组织中似乎没有相同的单向类作用。医疗保健提供者应认识到所有可获得的信息, 以帮助患者作出尽可能最佳的共同决策选择。

Keywords:

• Selective estrogen receptor modulators
• effects on bone
• bone density
• fracture

Potential conflict of interest

No potential conflict of interest was reported by the author.

Source of funding

None.