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Gadoteric acid

目录号 : GC67668

Gadoteric acid 是一种大环、顺磁性、基于钆的造影剂,可以用于大脑、脊柱和相关组织的磁共振成像 (MRI)。特别是,Gadoteric acid 能够检测和可视化血脑屏障破坏和异常血管分布的区域。

Gadoteric acid Chemical Structure

Cas No.:72573-82-1

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产品描述

Gadoteric acid is a macrocyclic, paramagnetic, gadolinium-based contrast agent that can be used for magnetic resonance imaging (MRI) of the brain, spine, and related tissues. In particular, Gadoteric acid is able to detect and visualize areas of blood-brain barrier disruption and abnormal vascular distribution[1][2].

在肝细胞癌(尤其是高血管病变)的 DCE-MRI 中,Gadoteric acid 提供了更好的,更明显的对比度,以及早期增强的可感知性和更强的冲洗性[1]

[1]. Federico Collettini, et al. MR imaging of hepatocellular carcinoma: prospective intraindividual head-to-head comparison of the contrast agents gadoxetic acid and gadoteric acid. Sci Rep. 2022 Nov 3;12(1):18583.
[2]. Martin Maurer, et al. Tolerability and diagnostic value of gadoteric acid in the general population and in patients with risk factors: results in more than 84,000 patients. Eur J Radiol. 2012 May;81(5):885-90.

Chemical Properties

Cas No. 72573-82-1 SDF Download SDF
分子式 C16H25GdN4O8 分子量 558.64
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Research Update

Effects of gadodiamide and Gadoteric acid on lung tissue: A comparative study

J Biochem Mol Toxicol 2022 Sep;36(9):e23133.PMID:35686328DOI:10.1002/jbt.23133.

We set out to investigate the effects of gadodiamide and Gadoteric acid, used for magnetic resonance imaging, on the lungs. In this study, 32 male Sprague Dawley rats were used. These were allocated into four groups; The first group (control) was untreated. The second group received isotonic saline on the first and fourth days of the week for 5 weeks. Following the same schedule, the third and fourth groups received a total of 2 mg/kg gadodiamide and Gadoteric acid, respectively, in place of saline. The alveolar Wall thickness was evaluated. Gadodiamide and Gadoteric acid significantly increased the numbers of collagen-3 and caspase-3 positive cells in the lung tissue (p < 0.05). In addition, these two substances increased the alveolar Wall thickness (p < 0.05). Furthermore, they increased the levels of malondialdehyde and glutathione (p < 0.05). This study demonstrates that both linear and macrocyclic contrast agents are toxic for the lungs in rats.

Repeated Gadoteric acid and gadobutrol exposure causes deterioration of behavior and memory functions in rats: MRI, histopathological and biochemical evidence

Brain Res 2021 Mar 1;1754:147256.PMID:33422532DOI:10.1016/j.brainres.2020.147256.

Gadolinium-based contrast agents (GBCAs) exert effects in different regions of the brain; however, studies on this topic are mostly focused on radiological outcomes of GBCA exposure. This paper is a preliminary attempt to identify whether there are changes in behavioral, cognitive, histopathological, radiological and biochemical characteristics with repeated exposure to gadobutrol and Gadoteric acid. The effects of GBCAs were tested with the assessment of 4 groups -each comprised of 6 rats [controls, gadobutrol, Gadoteric acid (Doteram), and Gadoteric acid (Clariscan)]. Respective treatments of 0.1 ml/kg were administered for 3 weeks, followed by a recovery period of 1 week without any treatment. At the end of this regimen, behavioral tests (open field and passive learning test) were performed. Additionally, histopathological analysis of the hippocampal CA1 and CA3 regions (GFAP measurement and total neuron count), biochemical measurements [TNF-a, Malondialdehyde (MDA), Superoxide dismutase (SOD), homovalinic acid (HVA) and choline acetyl transferase (ChAT) levels], and radiological findings (MRI-region of interest) were carried out in each group. There was a significant impairment in all groups that had received gadolinium in open field and passive avoidance learning tests. Oxidative stress and inflammation markers were significantly elevated in all gadolinium groups. Additionally, increased hippocampal gliosis and decreased MRI-ROIs were observed in rats exposed to gadolinium. Chronic Gadoteric acid and gadobutrol exposure causes hippocampal gliosis and elevates oxidative stress and inflammation in rats. Radiological outcomes are also consistent with these findings. Long-term studies might be required to conclude whether gadolinium deposition in the brain causes subtle neurological deficits.

Safety and efficacy of Gadoteric acid in pediatric magnetic resonance imaging: overview of clinical trials and post-marketing studies

Pediatr Radiol 2015 Nov;45(12):1831-41.PMID:26045036DOI:10.1007/s00247-015-3394-9.

Background: Gadoteric acid is a paramagnetic gadolinium macrocyclic contrast agent approved for use in MRI of cerebral and spinal lesions and for body imaging. Objective: To investigate the safety and efficacy of Gadoteric acid in children by extensively reviewing clinical and post-marketing observational studies. Materials and methods: Data were collected from 3,810 children (ages 3 days to 17 years) investigated in seven clinical trials of central nervous system (CNS) imaging (n = 141) and six post-marketing observational studies of CNS, musculoskeletal and whole-body MR imaging (n = 3,669). Of these, 3,569 children were 2-17 years of age and 241 were younger than 2 years. Gadoteric acid was generally administered at a dose of 0.1 mmol/kg. We evaluated image quality, lesion detection and border delineation, and the safety of Gadoteric acid. We also reviewed post-marketing pharmacovigilance experience. Results: Consistent with findings in adults, Gadoteric acid was effective in children for improving image quality compared with T1-W unenhanced sequences, providing diagnostic improvement, and often influencing the therapeutic approach, resulting in treatment modifications. In studies assessing neurological tumors, Gadoteric acid improved border delineation, internal morphology and contrast enhancement compared to unenhanced MR imaging. Gadoteric acid has a well-established safety profile. Among all studies, a total of 10 children experienced 20 adverse events, 7 of which were thought to be related to Gadoteric acid. No serious adverse events were reported in any study. Post-marketing pharmacovigilance experience did not find any specific safety concern. Conclusion: Gadoteric acid was associated with improved lesion detection and delineation and is an effective and well-tolerated contrast agent for use in children.

Effects of Gadodiamide and Gadoteric acid on Rat Kidneys: A Comparative Study

J Magn Reson Imaging 2019 Feb;49(2):382-389.PMID:30209850DOI:10.1002/jmri.26266.

Background: Gadolinium-based contrast agents are complex chelates to provide contrast in NRI. However, recent studies have highlighted the deposition of free Gd+3 ion in various tissues. Purpose: To evaluate the histopathological and immunohistochemical changes on rat kidney tissue following both macrocyclic (Gadoteric acid) and linear (gadodiamide) agents under the hypothesis that gadolinium-based contrast agents (GBCA) lead to toxic, free Gd+3 accumulation in tissues. Study type: The local Animal Care Committee approved the prospective animal study. Animal model: Thirty-two healthy Sprague-Dawley male rats were administered 2 mmol/kg gadodiamide and Gadoteric acid for the first 4 days for 5 weeks. Group 1 received no drug (control, n = 8) and Group 2 (n = 8) was administered 0.1 ml/kg saline. Group 3 was administered 0.1 mmol/kg gadodiamide and Group 4 (n = 8) was administered 2 mmol/kg Gadoteric acid. Assessment: Biochemical, histopathological, and immunohistochemical changes in testis kidney tissue were evaluated at the end of 10 weeks. Statistical tests: Differences between groups were analyzed using the nonparametric Kruskal-Wallis test followed by one-way analysis of variance and the Tamhane test, also followed by Turkey's HSD test. Results: Gadolinium increased serum urea, Ca+2 , and Caspase-3 positive tubular cell number. Larger Bowman capsules shrank proximal and distal tubules were revealed in the gadodiamide and Gadoteric acid groups compared to the control group (P < 0.05). Histopathologic examination showed significantly more interstitial fibrosis, amyloid deposits, and vasocongestion in the gadodiamide group than the Gadoteric acid and control groups, while the Gadoteric acid group demonstrated significantly more leukocytic infiltration with atrophied proximal and distal tubules than the gadodiamide and control groups (P < 0.05). Data conclusion: GBCA administration causes significant histopathologic changes in kidney tissue. This study advocates additional investigation to assess the in vivo safety of GBCAs. Level of evidence: 1 Technical Efficacy: Stage 2 J. Magn. Reson. Imaging 2019;49:382-389.

Intraventricular Gadoteric acid Intoxication: First Report

World Neurosurg 2018 Mar;111:264-268.PMID:29292188DOI:10.1016/j.wneu.2017.12.130.

Background: Gadolinium-based contrast agents are relatively safe for use in magnetic resonance imaging (MRI) of nervous system pathology. Few reports have been reported regarding the severe adverse effects. These are mostly mild anaphylactoid reactions, especially in the vulnerable group. Case description: We report a case of an adverse effect of Gadoteric acid concerning the misuse as intraventricular administration. To our knowledge, this is the first report related to intraventricular spillage and its results. A 38-year-old male patient with a complaint of headache and drowsiness was admitted to the hospital, after which cranial MRI revealed that he had a posterior fossa mass. An operation was performed with the catheterization of the lateral ventricule as a safety device at the beginning, and later mass was evacuated gross totally. Frozen pathology result showed the tumor was medulloblastoma. On the first postoperative day a control contrasted cranial and total spinal MRI was planned. He was observed to have a tonic-clonic generalized seizure soon after returning to the ward. After giving the acute management with antiepileptics, the patient was stabilized and it was recognized that the patient was administered contrast media by the intraventricular route. Symptomatic treatment and cerebrospinal fluid irrigation by external ventricular drainage helped the patient's improvement. After a week his symptoms were relieved and he had no complications during outpatient controls. Conclusions: In addition to formal basic supportive treatment, cerebrospinal fluid irrigation of the toxic contrast material is the best management method in case of such an unexpected misadministration of Gadoteric acid.