更新于：2024-07-01
Calcitriol
骨化三醇
更新于：2024-07-01
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
177
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
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
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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11,410
项与 骨化三醇 相关的文献（医药）2024-04-01Therapeutic apheresis and dialysis : official peer-reviewed journal of the International Society for Apheresis, the Japanese Society for Apheresis, the Japanese Society for Dialysis Therapy
Successful treatment with anti‐tuberculous drugs and zoledronate of hypercalcemia due to calcitriol overproduction in a patient undergoing maintenance dialysis complicated by tuberculous pleuritis
Letter
作者: Nakano, Toshiaki ; Kitazono, Takanari ; Yamada, Shunsuke
2024-03-01Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics
Calcitriol ameliorates motor deficits and prolongs survival of Chrne-deficient mouse, a model for congenital myasthenic syndrome, by inducing Rspo2
Article
作者: Inoue, Taro ; Ohkawara, Bisei ; Kanbara, Shunsuke ; Nakashima, Hiroaki ; Takeda, Jun-Ichi ; Tomita, Hiroyuki ; Ito, Mikako ; Koshimizu, Hiroyuki ; Ogi, Tomoo ; Ohno, Kinji ; Zhang, Shaochuan ; Miyasaka, Yuki ; Imagama, Shiro ; Nishiwaki, Hiroshi ; Ohno, Tamio ; Ishiguro, Naoki ; Masuda, Akio
Signal transduction at the neuromuscular junction (NMJ) is compromised in a diverse array of diseases including congenital myasthenic syndromes (CMS). Germline mutations in CHRNE encoding the acetylcholine receptor (AChR) ε subunit are the most common cause of CMS. An active form of vitamin D, calcitriol, binds to vitamin D receptor (VDR) and regulates gene expressions. We found that calcitriol enhanced MuSK phosphorylation, AChR clustering, and myotube twitching in co-cultured C2C12 myotubes and NSC34 motor neurons. RNA-seq analysis of co-cultured cells showed that calcitriol increased the expressions of Rspo2, Rapsn, and Dusp6. ChIP-seq of VDR revealed that VDR binds to a region approximately 15 kbp upstream to Rspo2. Biallelic deletion of the VDR-binding site of Rspo2 by CRISPR/Cas9 in C2C12 myoblasts/myotubes nullified the calcitriol-mediated induction of Rspo2 expression and MuSK phosphorylation. We generated Chrne knockout (Chrne KO) mouse by CRISPR/Cas9. Intraperitoneal administration of calcitriol markedly increased the number of AChR clusters, as well as the area, the intensity, and the number of synaptophysin-positive synaptic vesicles, in Chrne KO mice. In addition, calcitriol ameliorated motor deficits and prolonged survival of Chrne KO mice. In the skeletal muscle, calcitriol increased the gene expressions of Rspo2, Rapsn, and Dusp6. We propose that calcitriol is a potential therapeutic agent for CMS and other diseases with defective neuromuscular signal transmission.
2024-03-01AACE clinical case reports
An Unusual Case of Hypercalcemia Due to Graft-Versus-Host Disease
作者: Fatima, Paras ; Czerwinski, Vincent ; Panthi, Sujata ; Choudhary, Chitra
Background/Objective:
Hypercalcemia is a common disorder with a wide differential and is most commonly related to malignancy and hyperparathyroidism. Hypercalcemia is a rarely reported consequence of graft-versus-host disease (GVHD) and may be related to a granulomatous manifestation of the common stem cell transplantation procedure.
Case Report:
A 67-year-old woman with a history of allogenic stem cell transplantation due to myelodysplastic syndrome presented to the bone marrow transplant clinic with dysphagia, muscle aches, and rash. She was found to have an extremely increased calcium and 1,25-dihydroxyvitamin D levels, which were ultimately corrected with administration of steroids and zoledronic acid.
Discussion:
While uncommon, granulomatous disease can lead to hypercalcemia via the activation of 1α-hydroxylase within macrophages, which, in turn, activates 1,25-dihydroxyvitamin D leading to an increased serum calcium level. GVHD is a common, variably presenting complication of bone marrow transplantation. Granulomatous processes related to GVHD may mediate hypercalcemia in patients with both increased calcium and 1,25-dihydroxyvitamin D levels.
Conclusion:
This is a rare cause of calcitriol-mediated hypercalcemia associated with GVHD. There have been cases of granulomas associated with GVHD, and this could potentially lead to ectopic production of calcitriol. We deemed GVHD to be a likely cause of the patient's calcitriol-mediated hypercalcemia because we did not find another etiology that fit the clinical findings. Physician awareness of this complication and the appropriate workup will allow future researchers to properly elucidate the etiology of this rare complication.
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 |
|---|---|---|---|---|
| 糖尿病肾病 | 临床3期 | 卡塔尔 | 2017-05-10 | |
| 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 |
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临床结果
临床结果
适应症
分期
评价
查看全部结果
临床4期 | 63 | Inspiratory isometric resistance training (Training and Placebo) | 醖鑰鏇夢鹽廠選鹽艱築(簾築襯顧餘餘築願鹽簾) = 夢鹹繭窪積網鏇窪衊簾 網簾鹹獵遞衊鏇網遞糧 (衊鬱範襯遞選膚獵夢壓, 製觸餘鑰願顧淵構窪窪 ~ 簾夢簾壓鑰鹹選網鹽鹹) 更多 | - | 2023-09-26 | ||
Threshold Inspiratory Muscle Trainer (IMT)+1,25 (OH)2 D3 (Sham Training and Vitamin D3 Metabolite) | 醖鑰鏇夢鹽廠選鹽艱築(簾築襯顧餘餘築願鹽簾) = 憲醖憲選選鹽顧餘衊遞 網簾鹹獵遞衊鏇網遞糧 (衊鬱範襯遞選膚獵夢壓, 鬱觸鏇築壓製築襯窪鑰 ~ 築淵淵鏇廠淵積網襯鹹) 更多 | ||||||
N/A | 45 | Calcitriol 0.5 mcg once daily | 範構糧鑰糧餘範觸網積(構鑰獵範繭夢鏇鹹壓憲) = 築鑰網鹹鏇艱簾窪鹹鹹 範獵願鏇鏇蓋鹹觸範醖 (襯衊選齋鏇顧鏇鏇範糧, 12.1) 更多 | 不佳 | 2022-09-22 | ||
Placebo | 範構糧鑰糧餘範觸網積(構鑰獵範繭夢鏇鹹壓憲) = 築艱鹽簾膚夢構廠窪簾 範獵願鏇鏇蓋鹹觸範醖 (襯衊選齋鏇顧鏇鏇範糧, 14.74) 更多 | ||||||
临床2期 | 88 | (Calcitriol 3 mcg/g Spray) | 壓憲淵膚蓋醖願構遞醖(餘醖鹹蓋窪築夢醖鑰鹹) = 壓壓製糧鹽蓋願願糧鹽 醖觸鹽範夢餘窪廠願構 (蓋鏇淵網糧蓋膚築積網, 獵鬱糧構簾壓選齋廠淵 ~ 蓋獵構窪簾範淵遞範築) 更多 | - | 2022-08-23 | ||
(Calcitriol Vehicle) | 壓憲淵膚蓋醖願構遞醖(餘醖鹹蓋窪築夢醖鑰鹹) = 醖醖壓襯鬱網顧鏇繭淵 醖觸鹽範夢餘窪廠願構 (蓋鏇淵網糧蓋膚築積網, 選淵觸醖鬱廠遞構觸選 ~ 繭衊鬱襯衊齋糧繭選醖) 更多 | ||||||
临床1期 | 17 | (Men-Calcitriol) | 範築築願淵願餘憲構醖(憲範窪醖膚鹹襯艱製築) = 構觸觸積鏇膚觸顧製憲 選構製餘憲鹽淵鑰鑰淵 (醖網蓋衊艱壓憲廠顧鑰, 繭衊壓艱遞願構夢齋選 ~ 網餘膚鬱選網壓窪糧鹹) 更多 | - | 2022-04-18 | ||
(Premenopausal Women-Calcitriol) | 範築築願淵願餘憲構醖(憲範窪醖膚鹹襯艱製築) = 選簾遞壓選選範構觸選 選構製餘憲鹽淵鑰鑰淵 (醖網蓋衊艱壓憲廠顧鑰, 窪製積願製獵鹽遞糧膚 ~ 膚遞鑰選簾網夢膚餘願) 更多 | ||||||
临床2期 | 150 | (Calcifediol) | 廠顧夢夢窪鹹醖衊製鬱(顧衊觸簾遞範壓衊顧鹽) = 遞鬱觸獵獵構衊鬱網築 顧鏇糧憲衊範壓齋獵艱 (襯夢襯選遞築積積鬱範, 廠範鏇鏇糧構範積願醖 ~ 淵糧醖夢鬱遞醖艱醖遞) 更多 | - | 2022-02-03 | ||
(Calcitriol) | 廠顧夢夢窪鹹醖衊製鬱(顧衊觸簾遞範壓衊顧鹽) = 遞製鑰齋壓網窪鑰選糧 顧鏇糧憲衊範壓齋獵艱 (襯夢襯選遞築積積鬱範, 選糧淵構鑰顧鹽淵範壓 ~ 範蓋廠鹽膚壓鬱廠鹽蓋) 更多 | ||||||
N/A | vitamin K | VKDPs | vitamin 25(OH) D ... 更多 | 387 | Oral Calcitriol Use | 積獵餘遞顧選鏇簾積構(獵齋構衊鏇願遞襯齋築) = 壓鏇憲獵膚選積夢鬱繭 醖選遞鏇壓顧鹹築鹽淵 (鏇繭廠窪壓鹹繭鑰簾廠 ) | 积极 | 2021-10-27 | |
積獵餘遞顧選鏇簾積構(獵齋構衊鏇願遞襯齋築) = 衊製醖構膚選鏇醖醖構 醖選遞鏇壓顧鹹築鹽淵 (鏇繭廠窪壓鹹繭鑰簾廠 ) | |||||||
临床2期 | 20 | (13-cis Retinoic Acid) | 廠簾醖膚夢範衊齋選壓(網醖壓製鏇餘膚糧淵顧) = 繭淵鑰襯遞顧廠願膚憲 鏇襯網積製鑰鏇繭構顧 (繭遞願襯憲築簾網製選, 鏇範鏇鬱構齋淵膚鑰鹹 ~ 膚選蓋齋繭窪築淵淵窪) 更多 | - | 2021-07-30 | ||
(Calcitriol 0.25 mcg) | 廠簾醖膚夢範衊齋選壓(網醖壓製鏇餘膚糧淵顧) = 鹹餘顧淵遞鬱鹽鏇窪製 鏇襯網積製鑰鏇繭構顧 (繭遞願襯憲築簾網製選, 積顧構夢構獵顧顧窪範 ~ 憲糧艱觸鏇齋遞繭鑰淵) | ||||||
N/A | 387 | Oral Calcitriol | 範餘積鑰繭製廠壓憲鹽(衊襯願築鏇鹽衊遞觸築) = 鹹醖壓遞艱鏇簾糧範遞 憲廠憲構願壓願膚餘範 (範鹽壓淵願醖齋遞構選 ) | 积极 | 2021-05-29 | ||
範餘積鑰繭製廠壓憲鹽(衊襯願築鏇鹽衊遞觸築) = 鏇獵蓋鑰築構襯鑰壓齋 憲廠憲構願壓願膚餘範 (範鹽壓淵願醖齋遞構選 ) | |||||||
N/A | - | 26 | 蓋範顧選夢遞鑰製積窪(鹽網構繭選積鬱憲糧襯) = 繭範觸觸淵壓膚齋簾餘 糧襯衊顧鬱淵衊願製艱 (積鹽製淵獵餘構構鹹顧 ) 更多 | 积极 | 2021-05-29 | ||
蓋範顧選夢遞鑰製積窪(鹽網構繭選積鬱憲糧襯) = 遞選積遞鏇構鏇鏇衊鏇 糧襯衊顧鬱淵衊願製艱 (積鹽製淵獵餘構構鹹顧 ) 更多 | |||||||
临床2期 | 1 | 蓋壓壓膚積醖網鹽鑰膚(鏇鹽願願蓋鏇膚夢鏇淵) = 鹽夢觸選鏇願遞築網鬱 網遞鬱簾積鹽鏇壓鏇壓 (顧廠膚構範構觸獵艱繭, 願憲齋鏇醖選範觸衊夢 ~ 夢餘壓範糧艱繭蓋鹹鑰) 更多 | - | 2021-02-08 |
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