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Antiresorptive Drugs Beyond Bisphosphonates and Selective Oestrogen Receptor Modulators for the Management of Postmenopausal Osteoporosis

机译:除双膦酸盐和选择性雌激素受体调节剂以外的抗吸收药用于治疗绝经后骨质疏松症

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摘要

Osteoporotic fractures are a major cause of morbidity in the elderly population. Since postmenopausal osteoporosis is related to an increase in osteoclastic activity at the time of menopause, inhibitors of bone resorption have genuinely been considered an adequate strategy for prevention and treatment of osteoporosis. Bisphosphonates and selective oestrogen receptor modulators are widely prescribed to treat osteoporosis. However, other antiresorptive drugs have been developed for the management of osteoporosis, with the objective of providing a substantial reduction in osteoporotic fractures at all skeletal sites, combined with an acceptable long-term skeletal and systemic safety profile. Denosumab, a human monoclonal antibody to receptor activator for nuclear factor kappa B ligand, has shown efficacy against vertebral, nonvertebral and hip fractures. Its administration every 6 months as a subcutaneous formulation might significantly influence compliance and persistence to therapy. Additional results regarding long-term skeletal safety (i.e. osteonecrosis of the jaw and atypical diaphyseal femoral fracture) are needed. Odanacatib, a selective cathepsin K inhibitor, is a promising new approach to the inhibition of osteoclastic resorption, with the potential to uncouple bone formation from bone resorption. Results regarding its anti-fracture efficacy are expected in the coming months.
机译:骨质疏松性骨折是老年人口发病的主要原因。由于绝经后骨质疏松症与绝经时破骨细胞活性的增加有关,因此,骨吸收抑制剂确实被认为是预防和治疗骨质疏松症的适当策略。双膦酸盐和选择性雌激素受体调节剂被广泛处方用于治疗骨质疏松症。但是,还开发了其他抗吸收药物来治疗骨质疏松症,目的是在所有骨骼部位显着减少骨质疏松性骨折,并具有可接受的长期骨骼和全身安全性。 Denosumab是一种针对核因子κB配体的受体激活剂的人类单克隆抗体,已显示出对椎骨,非椎骨和髋部骨折的功效。每6个月以皮下制剂形式给药可能会显着影响治疗的依从性和持久性。还需要有关长期骨骼安全性(即下颌骨坏死和非典型干fe端股骨骨折)的其他结果。 Odanacatib是一种选择性的组织蛋白酶K抑制剂,是一种抑制破骨细胞吸收的有前途的新方法,具有将骨形成与骨吸收解耦的潜力。有关其抗骨折功效的结果有望在未来几个月内得出。

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