Department of Endocrinology, 424 General Military Hospital, Thessaloniki.
Ther Clin Risk Manag. 2012;8:295-306. doi: 10.2147/TCRM.S24239. Epub 2012 Jun 19.
Denosumab is a fully human monoclonal antibody to the receptor activator of nuclear factor-κB ligand (RANKL), a member of the tumor necrosis factor receptor superfamily essential for osteoclastogenesis. Denosumab treatment is associated with a rapid, sustained, and reversible reduction in bone turnover markers, a continuous marked increase in bone mineral density at all sites, and a marked decrease in the risk of vertebral, hip, and nonvertebral fractures in women with postmenopausal osteoporosis. Therefore, it could be considered as an effective alternative to previous bisphosphonate treatment as well as first-line treatment of severe osteoporosis. Cost-effectiveness studies support this suggestion. In addition, denosumab seems to be the safest treatment option in patients with impaired renal function. Denosumab is characterized by reversibility of its effect after treatment discontinuation, in contrast with bisphosphonates. Large-scale clinical trials, including the extension of FREEDOM trial for up to 5 years, are reassuring for its safety. However, given its brief post-market period, vigilance regarding adverse events related to putative RANKL inhibition in tissues other than bone, as well as those related to bone turnover oversuppression, is advised.
地舒单抗是一种针对核因子-κB 配体(RANKL)受体激活剂的全人源单克隆抗体,RANKL 属于肿瘤坏死因子受体超家族成员,是破骨细胞生成所必需的。地舒单抗治疗可迅速、持续和可逆地降低骨转换标志物,持续显著增加所有部位的骨密度,并显著降低绝经后骨质疏松症女性的椎体、髋部和非椎体骨折风险。因此,它可以被认为是对以前的双膦酸盐治疗的有效替代,也是严重骨质疏松症的一线治疗。成本效益研究支持这一建议。此外,地舒单抗似乎是肾功能受损患者的最安全治疗选择。与双膦酸盐不同,地舒单抗的作用在停药后可逆转。包括 FREEDOM 试验延长至 5 年的大规模临床试验对地舒单抗的安全性提供了保证。然而,鉴于其上市时间较短,建议警惕与骨以外组织中假定的 RANKL 抑制以及与过度抑制骨转换相关的不良事件。