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[地诺单抗。首个用于治疗骨质疏松症的核因子κB受体活化因子配体抑制剂]

[Denosumab. The first inhibitor of RANK-ligand for treatment of osteoporosis].

作者信息

Bruhn Claudia

出版信息

Med Monatsschr Pharm. 2010 Oct;33(10):370-5.

PMID:21072910
Abstract

Denosumab is a fully human monoclonal antibody, that specifically binds with high affinity to RANK-ligand (RANKL) and prevents interaction of RANKL with its receptor, called RANK (Receptor activator of nuclear factor kappa B). Blocking this signalling pathway (RANKL/RANK pathway) inhibits osteoclast differentiation and activation, and reduces bone resorption. Application of denosumab (60 mg s. c., every six months) results in increased bone mineral density, as showed in several clinical trials. Incidence of new vertebral fractures in postmenopausal women with osteoporosis was reduced significantly by semi-annual application of denosumab versus placebo. Patients suffering from malignant diseases could also benefit from treatment with denosumab in future.

摘要

地诺单抗是一种全人源单克隆抗体,它以高亲和力特异性结合核因子κB受体活化因子配体(RANKL),并阻止RANKL与其受体核因子κB受体活化因子(RANK)相互作用。阻断这一信号通路(RANKL/RANK通路)可抑制破骨细胞的分化和活化,并减少骨吸收。如多项临床试验所示,应用地诺单抗(皮下注射60mg,每6个月一次)可提高骨密度。与安慰剂相比,每半年应用一次地诺单抗可显著降低绝经后骨质疏松症女性新发椎体骨折的发生率。患有恶性疾病的患者未来也可能从地诺单抗治疗中获益。

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