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维生素D类似物与骨骼:依地骨化醇的临床前及临床研究

Vitamin D analogs and bone: preclinical and clinical studies with eldecalcitol.

作者信息

Matsumoto Toshio, Takano Toshiyuki, Saito Hitoshi, Takahashi Fumiaki

机构信息

Department of Medicine and Bioregulatory Sciences, University of Tokushima Graduate School of Medical Science , Tokushima, Japan.

Chugai Pharmaceutical Co. Ltd. , Tokyo, Japan.

出版信息

Bonekey Rep. 2014 Mar 5;3:513. doi: 10.1038/bonekey.2014.8. eCollection 2014.

Abstract

Eldecalcitol [1α,25-dihydroxy-2β-(3-hydroxypropyloxy)vitamin D3] is an analog of 1α,25-dihydroxyvitamin D3 [1,25(OH)2D3], bearing a hydroxypropyloxy residue at the 2β position. In preclinical studies, eldecalcitol suppressed bone resorption to a greater extent than alfacalcidol but had a similar effect on bone formation and Ca metabolism, resulting in a greater increase in bone mineral density (BMD) in ovariectomized (OVX) rats. Histological analysis in OVX rats immediately after ovariectomy revealed that eldecalcitol reduced osteoclast number and bone resorption parameters with a decrease in bone formation parameters. Eldecalcitol also promoted focal bone formation independent of bone resorption, a process known as bone minimodeling. In clinical studies, eldecalcitol showed stronger effects than alfacalcidol in increasing BMD and reducing bone resorption markers in osteoporotic patients under vitamin D supplementation. A 3-year randomized, double-blind, active-comparator clinical trial demonstrated that once-daily 0.75 μg eldecalcitol reduced vertebral fracture incidence by 26% compared with 1.0 μg alfacalcidol. Eldecalcitol also reduced the incidence of wrist fractures by 71% compared with alfacalcidol. Although this may be due to the previously reported effect of vitamin D in reducing the incidence of falls, it is not known whether eldecalcitol has a stronger effect in preventing falls than alfacalcidol. Because eldecalcitol stimulates intestinal Ca absorption and improves Ca balance in addition to its skeletal effects, combination treatment with antiresorptive agents may be able to show better effects than native vitamin D and Ca supplementation in preventing fractures in osteoporotic patients. Further studies are warranted to clarify these issues.

摘要

艾地骨化醇[1α,25 - 二羟基 - 2β - (3 - 羟基丙氧基)维生素D3]是1α,25 - 二羟基维生素D3[1,25(OH)2D3]的类似物,在2β位带有一个羟基丙氧基残基。在临床前研究中,艾地骨化醇比阿法骨化醇更能抑制骨吸收,但对骨形成和钙代谢的作用相似,导致去卵巢(OVX)大鼠的骨矿物质密度(BMD)有更大增加。对OVX大鼠在卵巢切除后立即进行的组织学分析显示,艾地骨化醇减少了破骨细胞数量和骨吸收参数,同时骨形成参数也有所下降。艾地骨化醇还能独立于骨吸收促进局部骨形成,这一过程称为骨微结构重塑。在临床研究中,在补充维生素D的骨质疏松患者中,艾地骨化醇在增加BMD和降低骨吸收标志物方面比阿法骨化醇显示出更强的效果。一项为期3年的随机、双盲、活性对照临床试验表明,每日一次服用0.75μg艾地骨化醇与1.0μg阿法骨化醇相比,椎体骨折发生率降低了26%。与阿法骨化醇相比,艾地骨化醇还使腕部骨折发生率降低了71%。尽管这可能归因于先前报道的维生素D在降低跌倒发生率方面的作用,但尚不清楚艾地骨化醇在预防跌倒方面是否比阿法骨化醇有更强的效果。由于艾地骨化醇除了对骨骼有作用外,还能刺激肠道钙吸收并改善钙平衡,因此与抗吸收剂联合治疗在预防骨质疏松患者骨折方面可能比天然维生素D和补充钙剂显示出更好的效果。有必要进一步研究以阐明这些问题。

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