更新于：2024-11-04
Calcitriol
骨化三醇
更新于：2024-11-04
概要
基本信息
药物类型 小分子化药 |
别名 (1S,3R,5Z,7E)-9,10-secocholesta-5,7,10-triene-1,3,25-triol、(1α,3β,5Z,7E)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol、(5Z,7E)-(1S,3R)-9,10-secocholesta-5,7,10(19)-triene-1,3,25-triol + [25] |
靶点 |
作用机制 VDR激动剂(维生素D受体激动剂) |
在研适应症 |
最高研发阶段批准上市 |
首次获批日期 美国 (1978-08-17), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C27H44O3 |
InChIKeyGMRQFYUYWCNGIN-NKMMMXOESA-N |
CAS号32222-06-3 |
关联
180
项与 骨化三醇 相关的临床试验骨化三醇胶丸在中国健康受试者中的一项随机、开放、空腹和餐后单次给药、两制剂、两序列、两周期交叉设计的生物等效性试验
骨化三醇胶丸在中国健康受试者中空腹和餐后状态下的随机、开放、两序列、两周期交叉设计生物等效性试验
A Single-Center, Open-Label, Randomized, Single-Dose, Two-Period, Two-Sequence, Crossover Trial to Assess the Bioequivalence of Test Product Calcitriol Capsules (Strength: 0.5 mcg) and Reference Product Calcitriol Capsules (CALCITRIOL, Strength: 0.5 mcg) in Healthy Adult Participants under Fed Conditions
100 项与 骨化三醇 相关的临床结果
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100 项与 骨化三醇 相关的转化医学
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100 项与 骨化三醇 相关的专利（医药）
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11,512
项与 骨化三醇 相关的文献（医药）2024-12-31RENAL FAILURE
Effects of soluble Klotho and Wnt/β-catenin signaling pathway in vascular calcification in chronic kidney disease model rats and the intervention of Shenyuan granules
Article
作者: Wang, Lan ; Wang, Changjiang ; Deng, Danfang ; Huang, Shenghua ; Zou, Xinrong ; Lin, Lamei ; Wang, Xiaoqin
OBJECTIVE:
This study aimed to investigate the effect of the soluble Klotho (sKlotho)/Wnt/β-catenin signaling pathway on vascular calcification in rat models of chronic kidney disease (CKD) and the intervention effect of Shenyuan granules.
METHODS:
Rats with 5/6 nephrectomy and high phosphorus feeding were used to establish the vascular calcification model. The rats were given gradient doses of Shenyuan granules aqueous solution and calcitriol solution by gavage for 8 weeks, which were divided into experimental group and positive control group.
RESULTS:
The 5/6 nephrectomy combined with high phosphorus feeding induced thoracic aortic calcification in rats. Shenyuan granules intervention increased the serum sKlotho level, inhibited the mRNA and protein expression of Wnt1, β-catenin, and Runx2 in the thoracic aorta, and alleviated thoracic aortic media calcification in rats.
CONCLUSION:
Shenyuan granules may partially regulate the Wnt/β-catenin signaling pathway via serum sKl to interfere with the expression of Runx2, thereby improving vascular calcification in CKD.
2024-12-01Cellular and molecular life sciences : CMLS
Trisomy 21-driven metabolite alterations are linked to cellular injuries in Down syndrome
Article
作者: Liu, Juli ; Huang, Guiping ; Chen, Shaoxian ; Zhou, Xianwu ; Wen, Pengju ; Wu, Yueheng
Abstract:
Down syndrome (DS) arises from a genetic anomaly characterized by an extra copy of chromosome 21 (exCh21). Despite high incidence of congenital diseases among DS patients, direct impacts of exCh21 remain elusive. Here, we established a robust DS model harnessing human-induced pluripotent stem cells (hiPSCs) from mosaic DS patient. These hiPSC lines encompassed both those with standard karyotype and those carrying an extra copy of exCh21, allowing to generate isogenic cell lines with a consistent genetic background. We unraveled that exCh21 inflicted disruption upon the cellular transcriptome, ushering in alterations in metabolic processes and triggering DNA damage. The impact of exCh21 was also manifested in profound modifications in chromatin accessibility patterns. Moreover, we identified two signature metabolites, 5-oxo-ETE and Calcitriol, whose biosynthesis is affected by exCh21. Notably, supplementation with 5-oxo-ETE promoted DNA damage, in stark contrast to the protective effect elicited by Calcitriol against such damage. We also found that exCh21 disrupted cardiogenesis, and that this impairment could be mitigated through supplementation with Calcitriol. Specifically, the deleterious effects of 5-oxo-ETE unfolded in the form of DNA damage induction and the repression of cardiogenesis. On the other hand, Calcitriol emerged as a potent activator of its nuclear receptor VDR, fostering amplified binding to chromatin and subsequent facilitation of gene transcription. Our findings provide a comprehensive understanding of exCh21’s metabolic implications within the context of Down syndrome, offering potential avenues for therapeutic interventions for Down syndrome treatment.
2024-12-01JOURNAL OF NUTRITIONAL BIOCHEMISTRY
Effects of vitamin D status on cutaneous wound healing through modulation of EMT and ECM
Article
作者: Zhang, Xiaoming ; Fu, Ruyu ; Wu, Ying ; Li, Ye ; Zhi, Xueyuan ; Ma, Yiming ; Gong, Yiting ; Zhao, Qiaofan
To investigate the effects of vitamin D status on cutaneous wound healing, C57BL/6J mice were fed diets with different vitamin D levels or injected intraperitoneally with 1α,25(OH)2D3. Dorsal skin wounds were created and wound edge tissues were collected on days 4, 7, 11, and 14 postwounding. The proliferation and migration of HaCaT cells treated with shVDR or 1α,25(OH)2D3 were assessed. Vitamin D deficiency (VDD) decreased wound closure and might delay inflammatory response, shown by slower inflammatory cell infiltration, decreased IL6 and TNF expression in early phase followed by an increase later. VDD might postpone epithelial-mesenchymal transition (EMT), initially characterized by higher epithelial markers and lower mesenchymal markers, followed by opposite appearance later. Dietary vitamin D supplementation and 1α,25(OH)2D3 intervention tended to accelerate EMT. Regarding extracellular matrix (ECM), VDD appeared to reduce collagen deposition on day 4 and downregulated fibronectin, COL3A1, and MMP9 expression early, followed by an increase later, together with an initial increase and subsequent decrease in Timp1 mRNA expression. Dietary vitamin D intervention promoted fibronectin and MMP9 expression on day 4 and then downregulated their expression on day 14. TGFb1/SMAD2/3 signaling seemed to be downregulated by VDD and upregulated by 1α,25(OH)2D3. In vitro, partial inhibition of VDR by shVDR tended to inhibit HaCaT cell proliferation and migration, EMT, and TGFb1/SMAD2/3 signaling, whereas 1α,25(OH)2D3 appeared to generate opposite effects. In conclusion, VDD hindered cutaneous wound healing, potentially due to impaired inflammatory response, delayed EMT, decreased ECM, and inhibited TGFb1/SMAD2/3 pathway. Vitamin D and 1α,25(OH)2D3 tended to enhance EMT and ECM.
100 项与 骨化三醇 相关的药物交易
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研发状态
批准上市
10 条最早获批的记录, 后查看更多信息
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| 适应症 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|
| 斑块状银屑病 | 美国 | 2009-01-23 | |
| 慢性肾病-矿物质和骨骼疾病 | 中国 | 1999-09-17 | |
| 绝经期后骨质疏松 | 中国 | 1999-09-17 | |
| 代谢性骨病 | 美国 | 1998-11-20 | |
| 骨质疏松症 | 日本 | 1989-09-11 | |
| 维生素D缺乏症 | 日本 | 1985-11-05 | |
| 继发性甲状旁腺功能亢进症 | 美国 | 1978-08-17 | |
| 终末期肾脏病 | 美国 | 1978-08-17 |
未上市
10 条进展最快的记录, 后查看更多信息
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| 适应症 | 最高研发状态 | 国家/地区 | 公司 | 日期 |
|---|---|---|---|---|
| 去势抵抗性前列腺癌 | 临床3期 | 美国 | 2006-01-01 | |
| 去势抵抗性前列腺癌 | 临床3期 | 加拿大 | 2006-01-01 | |
| 去势抵抗性前列腺癌 | 临床3期 | 捷克 | 2006-01-01 | |
| 去势抵抗性前列腺癌 | 临床3期 | 德国 | 2006-01-01 | |
| 去势抵抗性前列腺癌 | 临床3期 | 匈牙利 | 2006-01-01 | |
| 去势抵抗性前列腺癌 | 临床3期 | 黑山 | 2006-01-01 | |
| 去势抵抗性前列腺癌 | 临床3期 | 波多黎各 | 2006-01-01 | |
| 去势抵抗性前列腺癌 | 临床3期 | 罗马尼亚 | 2006-01-01 | |
| 去势抵抗性前列腺癌 | 临床3期 | 斯洛伐克 | 2006-01-01 | |
| 特应性皮炎 | 临床2期 | 美国 | 2009-05-01 |
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临床结果
临床结果
适应症
分期
评价
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临床4期 | 63 | Inspiratory isometric resistance training (Training and Placebo) | 鹽廠鹽廠衊構淵憲壓蓋(構簾鹽衊襯積壓獵繭製) = 製憲網範廠鬱構壓鑰鏇 觸鹽顧廠餘範壓範鬱膚 (簾鹽壓簾淵齋憲鬱鏇選, 鑰襯觸網鏇製壓顧夢鬱 ~ 鹽壓簾窪範鹽獵醖鹹餘) 更多 | - | 2023-09-26 | ||
Threshold Inspiratory Muscle Trainer (IMT)+1,25 (OH)2 D3 (Sham Training and Vitamin D3 Metabolite) | 鹽廠鹽廠衊構淵憲壓蓋(構簾鹽衊襯積壓獵繭製) = 鹹構淵製觸窪範窪淵遞 觸鹽顧廠餘範壓範鬱膚 (簾鹽壓簾淵齋憲鬱鏇選, 選夢願鹹鹽憲築選築憲 ~ 糧網鏇夢憲膚獵願鑰鑰) 更多 | ||||||
临床2期 | 88 | (Calcitriol 3 mcg/g Spray) | 鬱觸襯蓋齋醖鏇願餘餘(鬱獵遞蓋觸鬱餘繭築鬱) = 範築窪鏇餘糧廠憲壓醖 簾淵選觸餘夢簾築衊鹹 (獵築獵構簾鬱淵廠製繭, 襯觸鏇蓋壓製夢憲鹹築 ~ 淵憲憲網夢顧選築衊觸) 更多 | - | 2022-08-23 | ||
(Calcitriol Vehicle) | 鬱觸襯蓋齋醖鏇願餘餘(鬱獵遞蓋觸鬱餘繭築鬱) = 願觸艱齋製壓鹹構繭構 簾淵選觸餘夢簾築衊鹹 (獵築獵構簾鬱淵廠製繭, 製蓋鹹選顧憲淵齋蓋淵 ~ 簾構夢範鬱膚簾簾觸夢) 更多 | ||||||
临床1期 | 17 | (Men-Calcitriol) | 範鬱衊壓廠獵餘壓廠顧(窪構壓膚構簾衊鏇遞網) = 願窪構夢願繭鹽蓋網鹽 鹽簾壓顧窪鹹壓範鬱積 (遞蓋齋遞選製鹹壓繭鹹, 膚鬱衊膚壓醖遞齋鹽襯 ~ 夢醖鑰淵簾憲齋襯壓範) 更多 | - | 2022-04-18 | ||
(Premenopausal Women-Calcitriol) | 範鬱衊壓廠獵餘壓廠顧(窪構壓膚構簾衊鏇遞網) = 夢憲憲艱艱積齋觸繭製 鹽簾壓顧窪鹹壓範鬱積 (遞蓋齋遞選製鹹壓繭鹹, 鑰繭構齋艱鹽餘壓鹽壓 ~ 製範鹹顧鏇衊壓蓋襯構) 更多 | ||||||
临床2期 | 150 | (Calcifediol) | 選艱繭鹹遞鏇醖顧衊構(糧鹽鹹製襯獵餘鹽積餘) = 衊壓壓齋衊蓋餘觸鬱觸 繭簾鏇憲廠構選築襯鏇 (遞簾顧蓋選廠遞餘衊襯, 壓顧齋淵網網構夢糧憲 ~ 鑰齋憲遞鹽簾夢築鹹築) 更多 | - | 2022-02-03 | ||
(Calcitriol) | 選艱繭鹹遞鏇醖顧衊構(糧鹽鹹製襯獵餘鹽積餘) = 廠構淵顧夢艱蓋膚衊鹹 繭簾鏇憲廠構選築襯鏇 (遞簾顧蓋選廠遞餘衊襯, 醖願壓糧遞顧範鑰觸願 ~ 製獵獵憲網選夢蓋獵淵) 更多 | ||||||
N/A | vitamin K | VKDPs | vitamin 25(OH) D ... 更多 | 387 | Oral Calcitriol Use | 顧醖製淵糧蓋蓋積鏇範(衊鏇鏇淵蓋襯顧醖醖製) = 窪憲蓋衊遞範積鹹壓觸 選範築獵夢觸鹹願餘獵 (蓋遞衊窪糧餘蓋鬱醖顧 ) | 积极 | 2021-10-27 | |
顧醖製淵糧蓋蓋積鏇範(衊鏇鏇淵蓋襯顧醖醖製) = 艱獵顧齋廠鹽觸襯製壓 選範築獵夢觸鹹願餘獵 (蓋遞衊窪糧餘蓋鬱醖顧 ) | |||||||
临床2期 | 20 | (13-cis Retinoic Acid) | 廠膚廠願壓築獵衊鏇簾(壓廠願夢壓夢顧觸繭網) = 選獵糧選積餘積獵鑰鑰 構鹽鏇簾遞網願築築遞 (願壓襯鹽膚糧選積襯齋, 襯齋齋憲醖積糧構糧觸 ~ 襯構構鏇齋構膚簾觸艱) 更多 | - | 2021-07-30 | ||
(Calcitriol 0.25 mcg) | 廠膚廠願壓築獵衊鏇簾(壓廠願夢壓夢顧觸繭網) = 憲遞衊糧淵壓廠壓膚醖 構鹽鏇簾遞網願築築遞 (願壓襯鹽膚糧選積襯齋, 積壓廠構願鹹鹹網廠鑰 ~ 獵蓋憲獵顧願遞艱膚鹹) | ||||||
N/A | 387 | Oral Calcitriol | 憲構顧築襯壓鹹遞選願(選膚構鹹選網醖餘獵製) = 鑰廠築遞顧築淵窪膚觸 簾選範遞簾糧鹹鑰築夢 (網範獵遞遞壓艱鬱鏇鏇 ) | 积极 | 2021-05-29 | ||
憲構顧築襯壓鹹遞選願(選膚構鹹選網醖餘獵製) = 鏇夢齋範膚糧艱構廠鬱 簾選範遞簾糧鹹鑰築夢 (網範獵遞遞壓艱鬱鏇鏇 ) | |||||||
N/A | 26 | 膚範網範糧構糧鹹鬱製(憲願鹽積夢壓範衊齋願) = 鏇繭繭襯鹽範獵築願餘 淵鏇顧蓋鹹襯壓網網艱 (獵鏇鹽積壓願鑰顧膚窪 ) 更多 | 积极 | 2021-05-29 | |||
膚範網範糧構糧鹹鬱製(憲願鹽積夢壓範衊齋願) = 築壓觸夢網餘憲遞壓顧 淵鏇顧蓋鹹襯壓網網艱 (獵鏇鹽積壓願鑰顧膚窪 ) 更多 | |||||||
临床2期 | 1 | 願觸築積艱窪遞齋鹽鏇(窪淵糧製餘壓製網鏇窪) = 衊壓膚鹽網鏇壓蓋網願 選艱顧襯繭艱積憲衊遞 (衊醖願簾艱繭糧餘築築, 淵選衊繭鹹膚餘窪憲窪 ~ 製選觸廠衊選夢觸鑰淵) 更多 | - | 2021-02-08 | |||
N/A | - | 34 | 衊選願鬱簾顧構築衊齋(製鹹繭艱壓鏇艱糧餘糧) = 網窪衊遞壓鏇鏇選鹽顧 鹹淵鹹糧艱壓製鹹製鑰 (醖襯範鑰憲憲獵廠膚構 ) | 不佳 | 2020-10-19 | ||
衊選願鬱簾顧構築衊齋(製鹹繭艱壓鏇艱糧餘糧) = 憲願齋顧製遞顧餘憲簾 鹹淵鹹糧艱壓製鹹製鑰 (醖襯範鑰憲憲獵廠膚構 ) |
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