更新于：2024-07-01
Gadoterate Meglumine
钆特酸葡胺
更新于：2024-07-01
概要
基本信息
非在研机构- |
最高研发阶段批准上市 |
首次获批日期 日本 (2000-09-22), |
最高研发阶段(中国)- |
特殊审评- |
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结构
分子式C23H42GdN5O13 |
InChIKeyRYHQMKVRYNEBNJ-BMWGJIJESA-K |
CAS号92943-93-6 |
关联
46
项与 钆特酸葡胺 相关的临床试验Development of Activity MRI (aMRI): Direct Comparison to PET in Human Subjects
A Multicenter, Randomized, Prospective Double-blind, Cross-over Phase 3 Study to Evaluate the Efficacy and Safety of 0.04 mmol Gd/kg Body Weight of Gadoquatrane for MRI in Adults With Known or Suspected Pathology of Any Body Region (Except CNS), Compared to 0.1 mmol Gd/kg Approved Macrocyclic Gadolinium-based Contrast Agents (GBCAs)
A Multicenter, Randomized, Prospective Double-blind, Cross-over Phase 3 Study to Evaluate the Efficacy and Safety of 0.04 mmol Gd/kg Body Weight of Gadoquatrane for MRI in Adults With Known or Suspected Pathology of the Central Nervous System (CNS), Compared to 0.1 mmol Gd/kg Approved Macrocyclic Gadolinium-based Contrast Agents (GBCAs)
100 项与 钆特酸葡胺 相关的临床结果
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100 项与 钆特酸葡胺 相关的转化医学
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100 项与 钆特酸葡胺 相关的专利（医药）
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791
项与 钆特酸葡胺 相关的文献（医药）2024-04-01Magnetic resonance imaging
NSF evaluation of gadolinium biodistribution in renally impaired rats: Using novel metabolic Gd2O3 nanoparticles coated with β-cyclodextrin (Gd2O3@PCD) in MR molecular imaging
Article
作者: Haghgoo, Soheila ; Khoobi, Mehdi ; Riyahi Alam, Nader ; Ashouri, Hanieh ; Gholami, Mahdi ; Rasouli, Zahra
The use of conventional gadolinium(Gd)-based contrast agents in magnetic resonance imaging (MRI) poses a significant risk of Nephrogenic Systemic Fibrosis (NSF) syndrome in patients with impaired renal function (grades 4 and 5). To address this issue, a new study has introduced a novel metabolic Gadolinium oxide nanoparticle (Gd2O3 NPs) coated with β-cyclodextrin (βCD). The study aims to investigate NSF syndrome by quantifying tissue Gd deposition biodistribution in renal impairment rats using MR molecular imaging. This is the first study of its kind to use this approach. A group of 20 rats were divided into four groups, each containing five rats that underwent 5/6 nephrectomy. The rats received 12 intravenous injections of a novel homemade synthesized gadolinium oxide polycyclodextrin (Gd2O3@PCD) at a dose of 0.1 mmol/kg, conventional contrast agents (CAs) drugs of Omniscan (Gd-DTPA-BMA) and Dotarem (Gd-DOTA), at a dose of 2.5 mmol/kg, and 250 μl saline for two injections per week during six weeks. T1-weighted MR imaging was performed before the injections and once a week for six weeks to quantify Gd deposition in four different organs (skin, liver, heart, and lung) in rats using inductively coupled plasma mass spectrometry (ICP-MS). The relationship between Signal-to-Noise Ratio (SNR) and biodistribution of Gd deposition due to NSF-induced syndrome was also calculated. The results of the study showed that the Gd concentrations in tissues were significantly higher in the Gd2O3@PCD group compared to the other groups, without any significant histopathological changes (P < 0.05). In the Gd2O3@PCD group, Gd was mainly deposited in the skin, followed by the liver, lung, and heart, without any symptoms of thickening or hardening of the skin. The Gd concentrations in the skin, liver, lung, and heart were significantly lower in the Dotarem group than in the Omniscan group (P < 0.05). In the histopathological examinations, the Omniscan group showed increased cellularity in the dermis. A significant hyperintensity was observed in the Gd2O3@PCD-treated rats compared to the Dotarem and Omniscan groups in the liver, heart, and lung. Compared to conventional Gd-based CAs, the novel metabolically Gd2O3@PCD with increased SNR, biosafety, and a considerably lower probability of developing NSF, has potential applicability for diagnosing patients with renal diseases in clinical MR Molecular Imaging (MRMI).
2024-01-01Radiology
Gadolinium Presence in Rat Skin: Assessment of Histopathologic Changes Associated with Small Fiber Neuropathy
Article
作者: Balzer, Thomas ; Treu, Axel ; Ulbrich, Hannes-Friedrich ; Neddens, Joerg ; Thuss, Uwe ; Lohrke, Jessica ; Frenzel, Thomas ; Pietsch, Hubertus ; Jost, Gregor ; Boyken, Janina ; Prokesch, Manuela
Background The presence of gadolinium traces in the skin after administration of gadolinium-based contrast agents (GBCAs) raised safety concerns regarding a potential association with small fiber neuropathy (SFN). Purpose To investigate signs of SFN in rat foot pads by quantification of the intraepidermal nerve fiber density (IENFD) after multiple GBCA administrations and to evaluate gadolinium concentration, chemical species, and clearance. Materials and Methods Fifty rats received eight intravenous injections of either gadodiamide, gadobutrol, gadoterate, gadoteridol (8 × 0.6 mmol per kilogram of body weight), or saline (1.2 mL per kilogram of body weight), within 2 weeks and were sacrificed 5 days or 5 weeks after the last injection. IENFD was determined with protein gene product (PGP) 9.5 immunofluorescent staining and blinded and automated image analysis. The gadolinium and GBCA concentrations were measured with inductively coupled plasma mass spectrometry (ICP-MS), laser ablation ICP-MS, and matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI MSI). P values were calculated using linear contrasts of model analysis. Results The IENFD (measured as geometric mean [SD] and in number of nerve fibers per millimeter of epidermis) was not significantly altered after 5 days (saline, 8.4 [1.1]; gadobutrol, 9.7 [1.2]; gadoterate, 9.2 [1.2]; gadoteridol, 9.9 [1.3]; gadodiamide, 10.5 [1.2]) or 5 weeks (saline, 19.7 [1.4]; gadobutrol, 16.4 [1.6]; gadoterate, 14.3 [1.6]; gadoteridol, 22.2 [1.8]; gadodiamide, 17.9 [1.4]). Gadolinium skin concentrations were highest for gadodiamide after 5 days (16.0 nmol/g [1.1]) and 5 weeks (10.6 nmol/g [1.2], -33%). Macrocyclic agents were lower at 5 days (gadoteridol, 2.6 nmol/g [1.2]; gadobutrol, 2.7 nmol/g [1.1]; and gadoterate, 2.3 nmol/g [1.2]) and efficiently cleared after 5 weeks (gadoteridol, -95%; gadobutrol and gadoterate, -96%). The distribution of gadolinium and IENF did not visually overlap. For macrocyclic agents, gadolinium was found in sweat glands and confirmed to be intact chelate. Conclusion There were no signs of SFN in rat foot pads using multiple dosing regimens at two time points after administration of GBCAs. Macrocyclic GBCAs exhibited lower levels of gadolinium in the skin and were effectively eliminated within 5 weeks compared with linear gadodiamide, and intact macrocyclic GBCA was detected in sweat glands. © RSNA, 2024 Supplemental material is available for this article. See also the editorial by Clement in this issue.
2024-02-01Journal of bioscience and bioengineering
Preparation and performance of biocompatible gadolinium polymer as liver-targeting magnetic resonance imaging contrast agent
Article
作者: Zheng, Yan ; Li, Xiaojing ; Wan, Chuanling ; Zhan, Youyang ; Hu, Tingting
A biocompatible macromolecule-conjugated gadolinium chelate complex (PAV2-EDA-DOTA-Gd) as a new liver-specific contrast agent for magnetic resonance imaging (MRI) was synthesized and evaluated. An aspartic acid-valine copolymer was used as a carrier and ethylenediamine as a chemical linker, and the aspartic acid-valine copolymer was covalently linked to the small molecule MRI contrast agent Gd-DOTA (Dotarem) to synthesize a large molecule contrast agent. In vitro MR relaxation showed that the T1-relaxivity of PAV2-EDA-DOTA-Gd (13.7 mmol-1 L s-1) was much higher than that of the small-molecule Gd-DOTA (4.9 mmol-1 L s-1). In vivo imaging of rats showed that the enhancement effect of PAV2-EDA-DOTA-Gd (55.37 ± 2.80%) on liver imaging was 2.6 times that of Gd-DOTA (21.12 ± 3.86%), and it produced a longer imaging window time (40-70 min for PAV2-EDA-DOTA-Gd and 10-30 min for Gd-DOTA). Preliminary safety experiments, such as cell experiments and tissue sectioning, showed that PAV2-EDA-DOTA-Gd had low toxicity and satisfactory biocompatibility. The results of this study indicated that PAV2-EDA-DOTA-Gd had high potential as a liver-specific MRI contrast agent.
100 项与 钆特酸葡胺 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 |
|---|---|---|---|
| 血管疾病 | 美国 | 2013-03-20 | |
| 造影剂 | 日本 | 2000-09-22 |
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 |
|---|---|---|---|---|
| 中枢神经系统疾病 | 临床3期 | 阿根廷 | 2010-09-01 | |
| 中枢神经系统疾病 | 临床3期 | 奥地利 | 2010-09-01 | |
| 中枢神经系统疾病 | 临床3期 | 巴西 | 2010-09-01 | |
| 中枢神经系统疾病 | 临床3期 | 智利 | 2010-09-01 | |
| 中枢神经系统疾病 | 临床3期 | 法国 | 2010-09-01 | |
| 中枢神经系统疾病 | 临床3期 | 德国 | 2010-09-01 | |
| 中枢神经系统疾病 | 临床3期 | 意大利 | 2010-09-01 | |
| 中枢神经系统疾病 | 临床3期 | 韩国 | 2010-09-01 | |
| 中枢神经系统疾病 | 临床3期 | 西班牙 | 2010-09-01 | |
| 中枢神经系统疾病 | 临床3期 | 英国 | 2010-09-01 |
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临床结果
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适应症
分期
评价
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临床4期 | 37 | 獵網積製鑰遞願糧觸艱(夢糧鹽齋襯窪願淵壓獵) = 積鑰夢鬱壓憲窪鹽鏇遞 製築鏇觸膚壓齋觸築夢 (觸窪構製願選憲窪積鑰, 鹽選齋選選構顧鑰製憲 ~ 鑰鑰獵築築壓襯齋夢遞) 更多 | - | 2019-08-08 | |||
临床4期 | - | 51 | 壓鑰餘築糧鑰壓觸窪淵(願膚衊鏇構製窪夢繭艱) = 憲觸鹽膚獵網淵獵製積 鹽選艱顧遞齋獵積艱壓 (壓範醖餘選顧糧廠繭網, 襯鑰願艱顧構膚簾繭積 ~ 夢網簾窪構網鹽廠鏇鏇) 更多 | - | 2017-03-09 | ||
临床4期 | 179 | (MultiHance 0.1 mmol/kg Arm (Reader 1)) | 鹽鹹鑰夢衊鹽艱顧遞網(積觸積蓋觸網顧衊窪餘) = 糧簾築醖廠鬱顧憲窪願 願獵獵積範鏇窪壓夢鹽 (齋顧積齋顧簾築襯選衊, 膚觸艱淵願憲廠夢網觸 ~ 窪鏇觸繭獵醖襯膚築齋) 更多 | - | 2017-01-10 | ||
(MultiHance 0.1 mmol/kg Arm (Reader 2)) | 鹽鹹鑰夢衊鹽艱顧遞網(積觸積蓋觸網顧衊窪餘) = 鏇範繭糧窪夢艱衊網膚 願獵獵積範鏇窪壓夢鹽 (齋顧積齋顧簾築襯選衊, 夢鑰願觸簾蓋襯鬱範糧 ~ 願壓鹹壓壓顧積範鹽構) 更多 | ||||||
临床3期 | 416 | (Dotarem (Gadoterate Meglumine )) | 觸鬱夢觸齋範醖遞範遞(積膚蓋遞範鏇積觸願範) = 衊淵壓廠願淵製齋壓醖 鹹鹹淵襯夢壓襯憲鏇襯 (壓糧鏇觸襯蓋築選網鏇, 積簾餘製繭觸選網鑰蓋 ~ 鏇膚鹽繭淵顧觸鑰艱夢) 更多 | - | 2014-05-29 | ||
(Magnevist (Gadopentetate Dimeglumine)) | 觸鬱夢觸齋範醖遞範遞(積膚蓋遞範鏇積觸願範) = 繭願蓋餘築齋鬱膚觸選 鹹鹹淵襯夢壓襯憲鏇襯 (壓糧鏇觸襯蓋築選網鏇, 簾遞製膚艱鏇窪蓋選廠 ~ 餘鏇製鹽衊顧顧齋夢夢) 更多 | ||||||
临床4期 | 189 | Gadovist (Gadovist) | 鏇艱夢構膚蓋選網膚築(醖選積廠衊願選網蓋餘) = 艱鹹鏇觸遞餘衊醖選選 鬱積簾顧鏇範範願鹹繭 (觸積艱願廠壓遞鬱獵窪, 築廠積蓋範齋夢構艱繭 ~ 選鏇醖觸鏇範壓壓襯遞) 更多 | - | 2012-12-11 | ||
(Dotarem, Interventional) | 鏇艱夢構膚蓋選網膚築(醖選積廠衊願選網蓋餘) = 憲積糧壓憲膚鏇齋憲鹹 鬱積簾顧鏇範範願鹹繭 (觸積艱願廠壓遞鬱獵窪, 簾夢齋願艱積築築鏇製 ~ 顧襯網廠壓襯觸製築膚) 更多 |
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