Panorama MediClinic and University of Stellenbosch, Cape Town, South Africa.
Climacteric. 2010 Jun;13(3):210-8. doi: 10.3109/13697130903568542.
Several new selective estrogen receptor modulators (SERMs) are currently under clinical development for the prevention and/or treatment of postmenopausal osteoporosis, with the goal of optimizing the estrogen receptor agonist/antagonist activity in target tissues. Bazedoxifene is a novel SERM under clinical investigation for the prevention and treatment of postmenopausal osteoporosis. Emerging clinical data have shown that bazedoxifene is effective in preventing bone loss and osteoporotic fractures in postmenopausal women, with no evidence of breast or endometrial stimulation. Two large, prospective, international phase 3 studies have been completed. In postmenopausal women at risk for osteoporosis, bazedoxifene has been shown to preserve bone mineral density and to reduce bone turnover. In postmenopausal women with osteoporosis, bazedoxifene has demonstrated significant protection against new vertebral fractures and against non-vertebral fractures in women at higher fracture risk. The treatment effects of bazedoxifene were supported by findings from independent re-analyses using the Fracture Risk Assessment Tool (FRAX), which showed that bazedoxifene significantly reduced the risk of all clinical and morphometric vertebral fracture and of non-vertebral fracture in women at or above a FRAX-based threshold. Bazedoxifene was generally safe and well tolerated in the phase 3 studies and showed neutral effects on the breast and an excellent endometrial safety profile; such attributes allow for the partnering of bazedoxifene with conjugated estrogens for menopausal symptom relief. Collectively, these results suggest that bazedoxifene may be a promising new therapy for the prevention and treatment of postmenopausal osteoporosis as a monotherapy or in combination with conjugated estrogens in menopausal hormone therapy.
几种新的选择性雌激素受体调节剂（SERMs）目前正在临床开发中，用于预防和/或治疗绝经后骨质疏松症，目标是优化靶组织中的雌激素受体激动剂/拮抗剂活性。巴多昔芬是一种正在临床研究中用于预防和治疗绝经后骨质疏松症的新型 SERM。新出现的临床数据表明，巴多昔芬可有效预防绝经后妇女的骨质流失和骨质疏松性骨折，且无乳房或子宫内膜刺激的证据。两项大型、前瞻性、国际 3 期研究已经完成。在有骨质疏松症风险的绝经后妇女中，巴多昔芬已被证明可保持骨密度并减少骨转换。在患有骨质疏松症的绝经后妇女中，巴多昔芬对新的椎体骨折和骨折风险较高的妇女的非椎体骨折具有显著的保护作用。使用骨折风险评估工具（FRAX）进行的独立重新分析结果支持了巴多昔芬的治疗效果，该工具表明巴多昔芬可显著降低所有临床和形态计量椎体骨折以及骨折风险较高的妇女的非椎体骨折风险。在 3 期研究中，巴多昔芬总体上是安全且耐受良好的，对乳房的影响呈中性，且具有极好的子宫内膜安全性；这些属性允许将巴多昔芬与结合雌激素联合用于缓解绝经症状。总的来说，这些结果表明，巴多昔芬可能是一种有前途的新疗法，可单独或与绝经激素治疗中的结合雌激素联合用于预防和治疗绝经后骨质疏松症。
