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艾地骨化醇:新型活性维生素 D(3)类似物,用于骨质疏松症的治疗。

Eldecalcitol: newly developed active vitamin D(3) analog for the treatment of osteoporosis.

机构信息

Tottori University, School of Health Science, 86 Nishi-Cho, Yonago, Tottori 683-8503, Japan.

出版信息

Expert Opin Pharmacother. 2013 Apr;14(6):817-25. doi: 10.1517/14656566.2013.778825. Epub 2013 Mar 11.

DOI:10.1517/14656566.2013.778825
PMID:23477453
Abstract

INTRODUCTION

Eldecalcitol is an active vitamin D(3) analog, characterized by high stability in the circulation and also in the peripheral tissues, and by strong activity in increasing bone mass in osteoporotic patients. The objective of the present review was to evaluate the effect of eldecalcitol on bone compared with active vitamin D or placebo in preclinical and clinical studies.

AREAS COVERED

Eldecalcitol increased bone mineral density and reduced bone turnover markers greater than alfacalcidol and placebo. Interestingly, in a 3-year clinical trial, bone resorption marker remained suppressed during the eldecalcitol treatment, whereas bone formation markers gradually recovered after initial suppression. The incidences of vertebral fractures and wrist fractures in eldecalcitol-treated group were significantly lower than those in alfacalcidol-treated group by 26 and 71%, respectively. In the patients whose baseline bone turnover was low, eldecalcitol treatment did not further suppress bone turnover markers during the 3-year treatment period.

EXPERT OPINION

Eldecalcitol reduced wrist fractures much greater than alfacalcidol and one of the reasons may be a stronger effect of eldecalcitol on preventing falls. Although the effect of eldecalcitol on bone turnover markers was stronger than that of alfacalcidol or placebo, eldecalcitol is not a mere antibone resorptive agent, rather act as a bone turnover modulator.

摘要

简介

艾地骨化醇是一种活性维生素 D(3)类似物,具有在血液循环中和外周组织中高度稳定的特点,并具有增加骨质疏松症患者骨量的强大活性。本综述的目的是评估艾地骨化醇与活性维生素 D 或安慰剂在临床前和临床研究中对骨骼的影响。

涵盖领域

艾地骨化醇增加骨矿物质密度并降低骨转换标志物的作用大于阿尔法骨化醇和安慰剂。有趣的是,在一项为期 3 年的临床试验中,骨吸收标志物在艾地骨化醇治疗期间仍受到抑制,而骨形成标志物在初始抑制后逐渐恢复。艾地骨化醇治疗组的椎体骨折和腕骨骨折发生率分别比阿尔法骨化醇治疗组低 26%和 71%。在基线骨转换率较低的患者中,艾地骨化醇治疗在 3 年治疗期间不会进一步抑制骨转换标志物。

专家意见

艾地骨化醇降低腕骨骨折的效果远大于阿尔法骨化醇,其原因之一可能是艾地骨化醇在预防跌倒方面的作用更强。尽管艾地骨化醇对骨转换标志物的作用强于阿尔法骨化醇或安慰剂,但它不是单纯的抗骨吸收剂,而是一种骨转换调节剂。

相似文献

1
Eldecalcitol: newly developed active vitamin D(3) analog for the treatment of osteoporosis.艾地骨化醇:新型活性维生素 D(3)类似物,用于骨质疏松症的治疗。
Expert Opin Pharmacother. 2013 Apr;14(6):817-25. doi: 10.1517/14656566.2013.778825. Epub 2013 Mar 11.
2
[Frontiers in vitamin D; basic research and clinical application. Eldecalcitol: the effect on bones and calcium metabolism].[维生素D前沿;基础研究与临床应用。 eldecalcitol:对骨骼和钙代谢的影响]
Clin Calcium. 2011 Nov;21(11):103-10.
3
Eldecalcitol is superior to alfacalcidol in maintaining bone mineral density in glucocorticoid-induced osteoporosis patients (e-GLORIA).依降钙素在维持糖皮质激素诱导骨质疏松症患者的骨密度方面优于阿法骨化醇(e-GLORIA)。
J Bone Miner Metab. 2020 Jul;38(4):522-532. doi: 10.1007/s00774-020-01091-4. Epub 2020 Mar 5.
4
Eldecalcitol for the treatment of osteoporosis.依地骨化醇用于治疗骨质疏松症。
Drugs Today (Barc). 2012 Mar;48(3):189-96. doi: 10.1358/dot.2012.48.3.1745223.
5
A new active vitamin D3 analog, eldecalcitol, prevents the risk of osteoporotic fractures--a randomized, active comparator, double-blind study.一种新型活性维生素 D3 类似物,依降钙素,可预防骨质疏松性骨折的风险 - 一项随机、活性对照、双盲研究。
Bone. 2011 Oct;49(4):605-12. doi: 10.1016/j.bone.2011.07.011. Epub 2011 Jul 19.
6
Importance of alfacalcidol in clinical conditions characterized by high rate of bone loss.阿法骨化醇在以高骨丢失率为特征的临床病症中的重要性。
J Rheumatol Suppl. 2005 Sep;76:21-5.
7
Eldecalcitol increases bone mineral density in Chinese osteoporotic patients without vitamin D or calcium supplementation.依降钙素增加中国骨质疏松症患者骨密度,无需维生素 D 或钙补充。
J Bone Miner Metab. 2019 Nov;37(6):1036-1047. doi: 10.1007/s00774-019-01009-9. Epub 2019 May 13.
8
Relationship between the effect of eldecalcitol and serum 25(OH)D level.艾地骨化醇疗效与血清 25(OH)D 水平的关系。
J Steroid Biochem Mol Biol. 2014 Oct;144 Pt A:124-7. doi: 10.1016/j.jsbmb.2013.11.005. Epub 2013 Nov 15.
9
[Current Topics on Vitamin D. Treatment of osteoporosis with eldecalcitol: Its therapeutic efficacy and adverse effect on renal function].[维生素D的当前话题。依度骨化醇治疗骨质疏松症:其治疗效果及对肾功能的不良影响]
Clin Calcium. 2015 Mar;25(3):425-32.
10
Eldecalcitol normalizes bone turnover markers regardless of their pre-treatment levels.无论骨转换标志物的基线水平如何,艾地骨化醇均可使其恢复正常。
Curr Med Res Opin. 2012 Sep;28(9):1547-52. doi: 10.1185/03007995.2012.712506. Epub 2012 Aug 23.

引用本文的文献

1
Eldecalcitol prevents muscle loss and osteoporosis in disuse muscle atrophy via NF-κB signaling in mice.依地钙醇通过 NF-κB 信号通路预防废用性肌肉萎缩小鼠的肌肉丢失和骨质疏松症。
Skelet Muscle. 2023 Dec 19;13(1):22. doi: 10.1186/s13395-023-00332-0.
2
Eldecalcitol prevents muscle loss by suppressing PI3K/AKT/FOXOs pathway in orchiectomized mice.依地骨化醇通过抑制去势小鼠的PI3K/AKT/FOXOs信号通路来预防肌肉流失。
Front Pharmacol. 2022 Oct 28;13:1018480. doi: 10.3389/fphar.2022.1018480. eCollection 2022.
3
Effects of eldecalcitol on cortical bone response to mechanical loading in rats.
艾地骨化醇对大鼠皮质骨机械负荷反应的影响。
BMC Musculoskelet Disord. 2015 Jun 30;16:158. doi: 10.1186/s12891-015-0613-3.
4
Vitamin D analogs and bone: preclinical and clinical studies with eldecalcitol.维生素D类似物与骨骼:依地骨化醇的临床前及临床研究
Bonekey Rep. 2014 Mar 5;3:513. doi: 10.1038/bonekey.2014.8. eCollection 2014.