经济合成O-(2-[18F]氟乙基)-L-酪氨酸(18FFET)方法的研究

IF 0.9 4区 医学 Q4 BIOCHEMICAL RESEARCH METHODS Journal of labelled compounds & radiopharmaceuticals Pub Date : 2023-07-06 DOI:10.1002/jlcr.4052
Aishwarya Kumar, Raman Kumar Joshi, Riptee Thakur, Dinesh Kumar, Chandana Nagaraj, Pardeep Kumar
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引用次数: 0

摘要

使用O-(2-[18F]氟乙基)-L-酪氨酸([18F]FET)的正电子发射断层扫描(PET)在区分肿瘤复发和坏死方面取得了巨大成功。在本研究中,我们报告了通过改变不同化学模块中TET前体的浓度来合成[18F]FET的经验。TET前体(2–10 mg)用于在自动化(MX Tracerlab)模块中合成[18F]FET(n = 6) 和半自动(FX2N Tracerlab)模块(n = 19) 。对所有制剂进行了质量控制。对于人体成像,220 ± 50 将[18F]FET的MBq短暂注射到患者体内以获取PET-MR图像。两个模块中最终产品的放射化学纯度均大于95%。衰变校正后的平均产率为10.7 ± 4.7%(10 mg,n = 3) 和8.2 ± 2.6%(2 mg,n = 3) 带有自动化化学模块和36.7 ± 7.3%(8-10 mg,n = 12) ,26.4 ± 3.1%(5–7 mg,n = 4) 和35.1 ± 3.8%(2-4 mg,n = 3) 具有半自动化学模块。PET成像显示病变部位的摄取(SUVmax = 7.5 ± 2.6)并且与MR图像一致。[18F]FET是用2.0mg的前体以较高的放射化学产率生产的,具有显著的产率,并且适合于脑肿瘤成像。
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Development of an economical method to synthesize O-(2-[18F]fluoroethyl)-L-tyrosine (18FFET)

Positron emission tomography (PET) using O-(2-[18F]fluoroethyl)-L-tyrosine ([18F]FET) has shown great success in differentiating tumor recurrence from necrosis. In this study, we are reporting the experience of synthesis [18F]FET by varying the concentration of TET precursor in different chemistry modules. TET precursor (2–10 mg) was used for the synthesis of [18F]FET in an automated (MX Tracerlab) module (n = 6) and semiautomated (FX2N Tracerlab) module (n = 19). The quality control was performed for all the preparations. For human imaging, 220 ± 50 MBq of [18F]FET was briefly injected into the patient to acquire PET-MR images. The radiochemical purity was greater than 95% for the final product in both modules. The decay corrected average yield was 10.7 ± 4.7% (10 mg, n = 3) and 8.2 ± 2.6% (2 mg, n = 3) with automated chemistry module and 36.7 ± 7.3% (8–10 mg, n = 12), 26.4 ± 3.1% (5–7 mg, n = 4), and 35.1 ± 3.8% (2–4 mg, n = 3) with semiautomated chemistry modules. The PET imaging showed uptake at the lesion site (SUVmax = 7.5 ± 2.6) and concordance with the MR image. The [18F]FET was produced with a higher radiochemical yield with 2.0 mg of the precursor with substantial yield and is suitable for brain tumor imaging.

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来源期刊
CiteScore
3.30
自引率
0.00%
发文量
57
审稿时长
1 months
期刊介绍: The Journal of Labelled Compounds and Radiopharmaceuticals publishes all aspects of research dealing with labeled compound preparation and applications of these compounds. This includes tracer methods used in medical, pharmacological, biological, biochemical and chemical research in vitro and in vivo. The Journal of Labelled Compounds and Radiopharmaceuticals devotes particular attention to biomedical research, diagnostic and therapeutic applications of radiopharmaceuticals, covering all stages of development from basic metabolic research and technological development to preclinical and clinical studies based on physically and chemically well characterized molecular structures, coordination compounds and nano-particles.
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