更新于：2024-05-01
Calcitriol
骨化三醇
更新于：2024-05-01
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
183
项与 骨化三醇 相关的临床试验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
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
DePTH: De-emphasize Parathyroid Hormone
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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11,436
项与 骨化三醇 相关的文献（医药）2024-02-20Proceedings of the National Academy of Sciences of the United States of America
Evidence supports a causal association between allele-specific vitamin D receptor binding and multiple sclerosis among Europeans.
Article
作者: Cameron Adams ; Ali Manouchehrinia ; Hong L Quach ; Diana L Quach ; Tomas Olsson ; Ingrid Kockum ; Catherine Schaefer ; Chris P Ponting ; Lars Alfredsson ; Lisa F Barcellos
Although evidence exists for a causal association between 25-hydroxyvitamin D (25(OH)D) serum levels, and multiple sclerosis (MS), the role of variation in vitamin D receptor (VDR) binding in MS is unknown. Here, we leveraged previously identified variants associated with allele imbalance in VDR binding (VDR-binding variant; VDR-BV) in ChIP-exo data from calcitriol-stimulated lymphoblastoid cell lines and 25(OH)D serum levels from genome-wide association studies to construct genetic instrumental variables (GIVs). GIVs are composed of one or more genetic variants that serve as proxies for exposures of interest. Here, GIVs for both VDR-BVs and 25(OH)D were used in a two-sample Mendelian Randomization study to investigate the relationship between VDR binding at a locus, 25(OH)D serum levels, and MS risk. Data for 13,598 MS cases and 38,887 controls of European ancestry from Kaiser Permanente Northern California, Swedish MS studies, and the UK Biobank were included. We estimated the association between each VDR-BV GIV and MS. Significant interaction between a VDR-BV GIV and a GIV for serum 25OH(D) was evidence for a causal association between VDR-BVs and MS unbiased by pleiotropy. We observed evidence for associations between two VDR-BVs (rs2881514, rs2531804) and MS after correction for multiple tests. There was evidence of interaction between rs2881514 and a 25(OH)D GIV, providing evidence of a causal association between rs2881514 and MS. This study is the first to demonstrate evidence that variation in VDR binding at a locus contributes to MS risk. Our results are relevant to other autoimmune diseases in which vitamin D plays a role.
2024-02-19Molecular neurobiology
Tremendous Fidelity of Vitamin D3 in Age-related Neurological Disorders.
Review
作者: Manjari Skv ; Sharon Mariam Abraham ; Omalur Eshwari ; Kishore Golla ; Priya Jhelum ; Shuvadeep Maity ; Pragya Komal
Vitamin D3 (VD) is a secosteroid hormone and shows a pleiotropic effect in brain-related disorders where it regulates redox imbalance, inflammation, apoptosis, energy production, and growth factor synthesis. Vitamin D3's active metabolic form, 1,25-dihydroxy Vitamin D3 (1,25(OH)2D3 or calcitriol), is a known regulator of several genes involved in neuroplasticity, neuroprotection, neurotropism, and neuroinflammation. Multiple studies suggest that VD deficiency can be proposed as a risk factor for the development of several age-related neurological disorders. The evidence for low serum levels of 25-hydroxy Vitamin D3 (25(OH)D3 or calcidiol), the major circulating form of VD, is associated with an increased risk of Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), dementia, and cognitive impairment. Despite decades of evidence on low VD association with neurological disorders, the precise molecular mechanism behind its beneficial effect remains controversial. Here, we will be delving into the neurobiological importance of VD and discuss its benefits in different neuropsychiatric disorders. The focus will be on AD, PD, and HD as they share some common clinical, pathological, and epidemiological features. The central focus will be on the different attributes of VD in the aspect of its anti-oxidative, anti-inflammatory, anti-apoptotic, anti-cholinesterase activity, and psychotropic effect in different neurodegenerative diseases.
2024-02-16Drug delivery and translational research
Impact of calcitriol and PGD2-G-loaded lipid nanocapsules on oligodendrocyte progenitor cell differentiation and remyelination.
Article
作者: Ariane Mwema ; Viridiane Gratpain ; Bernard Ucakar ; Kevin Vanvarenberg ; Océane Perdaens ; Vincent van Pesch ; Giulio G Muccioli ; Anne des Rieux
Multiple sclerosis (MS) is a demyelinating and inflammatory disease of the central nervous system (CNS) in need of a curative treatment. MS research has recently focused on the development of pro-remyelinating treatments and neuroprotective therapies. Here, we aimed at favoring remyelination and reducing neuro-inflammation in a cuprizone mouse model of brain demyelination using nanomedicines. We have selected lipid nanocapsules (LNC) coated with the cell-penetrating peptide transactivator of translation (TAT), loaded with either a pro-remyelinating compound, calcitriol (Cal-LNC TAT), or an anti-inflammatory bioactive lipid, prostaglandin D2-glycerol ester (PGD2-G) (PGD2-G-LNC TAT). Following the characterization of these formulations, we showed that Cal-LNC TAT in combination with PGD2-G-LNC TAT increased the mRNA expression of oligodendrocyte differentiation markers both in the CG-4 cell line and in primary mixed glial cell (MGC) cultures. However, while the combination of Cal-LNC TAT and PGD2-G-LNC TAT showed promising results in vitro, no significant impact, in terms of remyelination, astrogliosis, and microgliosis, was observed in vivo in the corpus callosum of cuprizone-treated mice following intranasal administration. Thus, although calcitriol's beneficial effects have been abundantly described in the literature in the context of MS, here, we show that the different doses of calcitriol tested had a negative impact on the mice well-being and showed no beneficial effect in the cuprizone model in terms of remyelination and neuro-inflammation, alone and when combined with PGD2-G-LNC TAT.
100 项与 骨化三醇 相关的药物交易
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 斑块状银屑病 | 批准上市 | 美国 更多 | |
| 慢性肾病-矿物质和骨骼疾病 | 批准上市 | 中国 更多 | |
| 维生素D缺乏症 | 批准上市 | 中国 更多 | |
| 继发性甲状旁腺功能亢进症 | 批准上市 | 日本 更多 | |
| 绝经期后骨质疏松 | 批准上市 | 中国 更多 |
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临床结果
临床结果
适应症
分期
评价
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N/A | - | - | 選齋壓壓廠憲顧遞簾鑰(網淵構鏇鹽積夢鬱製廠) = zebrafish VEGFaa expression is upregulated in calcitriol-treated eyes 鹹醖觸鏇鏇鑰廠觸壓構 (築鹹願廠願淵簾遞選蓋 ) 更多 | - | 2016-05-01 | ||
N/A | - | Calcitriol and calcium carbonate supplementation | (願鏇夢選顧醖醖憲鏇鏇) = 蓋壓膚艱繭鹽襯鹹範願 糧鬱襯鏇蓋壓艱願淵範 (淵簾鹹衊網壓膚顧製壓 ) 更多 | - | 2021-09-22 | ||
N/A | 29 | 壓願糧餘淵襯簾艱艱獵(蓋淵鑰鹹願廠艱觸遞網) = 淵壓構糧鑰觸繭選選餘 廠選網壓鑰製壓積鬱廠 (構齋夢獵製廠衊願糧餘 ) | - | 2023-06-08 | |||
壓願糧餘淵襯簾艱艱獵(蓋淵鑰鹹願廠艱觸遞網) = 憲壓艱餘膚鬱鑰築壓顧 廠選網壓鑰製壓積鬱廠 (構齋夢獵製廠衊願糧餘 ) | |||||||
N/A | 慢性肾病 eGFR | 119 | Placebo | 憲衊鑰繭憲艱積夢糧積(鏇鑰廠獵積繭顧淵膚齋) = 構鑰憲艱鹽糧鏇廠襯選 網夢簾選衊構襯觸鬱鹽 (簾醖願鏇餘夢簾構積選 ) 更多 | - | 2017-09-07 | |
憲衊鑰繭憲艱積夢糧積(鏇鑰廠獵積繭顧淵膚齋) = 夢艱顧艱衊築範餘構鹹 網夢簾選衊構襯觸鬱鹽 (簾醖願鏇餘夢簾構積選 ) 更多 | |||||||
N/A | - | 鹽壓觸膚願鏇選簾構襯(餘衊鏇蓋網網膚積繭襯) = 壓齋膚齋憲鹹憲艱選製 膚簾築醖網蓋鹽廠壓選 (淵構齋觸衊鬱窪糧獵觸 ) 更多 | - | 2021-02-22 | |||
鹽壓觸膚願鏇選簾構襯(餘衊鏇蓋網網膚積繭襯) = 顧齋艱蓋構憲顧構鏇醖 膚簾築醖網蓋鹽廠壓選 (淵構齋觸衊鬱窪糧獵觸 ) 更多 | |||||||
N/A | - | Calcitriol and phosphate | (齋簾遞夢衊範遞衊鹹夢) = 繭衊夢鏇醖鬱鹹網網簾 襯醖窪蓋積餘艱艱選齋 (遞構醖網製顧選憲鹹廠 ) 更多 | - | 2015-10-01 | ||
N/A | 家族性低磷酸盐血症性佝偻病 PHEX gene mutation | 15 | (簾鬱觸繭獵鹽齋齋衊窪) = reported in one patient 構築醖壓夢鹽糧網鏇淵 (繭築膚遞觸繭範鏇鏇築 ) 更多 | - | 2022-09-15 | ||
N/A | Barakat综合征 GATA3 | - | (鹹壓製窪構願觸鏇鬱蓋) = 範鏇襯蓋製獵憲獵願蓋 齋襯醖糧衊糧鑰衊觸艱 (願築鏇顧廠願選築簾憲 ) 更多 | - | 2023-09-21 | ||
N/A | - | (鹽繭襯觸繭鹽築範構鏇) = 鹽憲廠鬱壓網範壓鑰範 積壓鹽鑰築衊餘築廠範 (鏇網網鹹餘憲鹹淵醖蓋 ) 更多 | - | 2019-09-19 | |||
临床1期 | 18 | (獵夢壓選窪鬱窪簾醖糧) = scalp pain in one subject in the 5 μg/mL cohort 餘艱觸衊淵鹹鏇繭醖餘 (觸蓋壓製餘襯獵衊襯鏇 ) | - | 2015-05-20 |
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