地舒单抗治疗骨质疏松临床应用指南(2026)
Clinical application guidelines for denosumab in the treatment of osteoporosis(2026)
  
DOI:10.3969/j.issn.1006-7108.2026.07.001
中文关键词:  地舒单抗  骨质疏松  骨密度  脆性骨折  RANKL/RANK/OPG信号通路  研究证据  队列研究  回顾性研究  药代动力学  安全性
英文关键词:denosumab  osteoporosis  bone mineral density  brittle fracture  RANKL/RANK/OPG signaling pathway  research evidence  cohort study  retrospective study  pharmacokinetics  safety
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《地舒单抗治疗骨质疏松临床应用指南(2026)》编写组 《中国骨质疏松杂志》社,北京 100102 
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中文摘要:
      地舒单抗是核因子-κB受体活化因子配体(RANKL)抑制剂,与RANKL结合,阻止RANKL与其受体核因子-κB受体活化因子(receptor activator of nuclear factor-κB,RANK) 结合。当骨吸收与骨形成偶联破坏,骨吸收大于骨形成。RANKL与破骨细胞前体细胞表面的RANK结合,通过RANK的胞内信号通路诱导激活NF-κB,调控破骨细胞分化相关基因的表达,促进破骨细胞的分化成熟和活化。成骨细胞分泌的骨保护素(osteoprotegerin,OPG),与RANK竞争性结合RANKL。RANKL/OPG直接影响骨吸收,RANKL/RANK/OPG信号通路对调节骨重建有重要作用。本指南收录大量研究证据,对药代动力学及推荐证据,骨质疏松临床应用的适应证、禁忌证、用法用量、治疗方案、推荐等级、停药要求、序贯治疗、联合用药、安全性、罕见不良反应、肾功不全患者用药、骨质疏松性骨折用药、男性骨质疏松及糖尿病具骨折风险地舒单抗的应用等,进行精准论述。
英文摘要:
      Denosumab is a nuclear factor-κB receptor activator ligand (RANKL) inhibitor that binds to RANKL, preventing its interaction with the receptor nuclear factor-κB receptor activator (receptor activator of nuclear factor-κB, RANK). When the coupling of bone resorption and bone formation is disrupted, bone resorption exceeds bone formation. RANKL binds to RANK on the surface of osteoclast precursor cells, inducing NF-κB activation through the intracellular signaling pathway of RANK, thereby regulating the expression of genes related to osteoclast differentiation and promoting osteoclast differentiation, maturation, and activation. Osteoprotegerin (OPG), secreted by osteoblasts, competitively binds to RANKL. The RANKL/OPG ratio directly influences bone resorption, while the RANKL/RANK/OPG signaling pathway plays a crucial role in regulating bone remodeling. This guideline incorporates extensive research evidence, providing precise discussions on pharmacokinetics and supporting evidence, indications and contraindications for osteoporosis clinical applications, dosage and administration, treatment protocols, recommendation levels, discontinuation requirements, sequential therapy, combination therapy, safety, rare adverse reactions, medication use in patients with renal insufficiency, treatment of osteoporotic fractures, and the application of denosumab in conditions such as male osteoporosis and diabetes with fracture risk.
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