Synthesis of 18F-labeled glucagon-like peptide-1 receptor agonist targeting probe and its preliminary evaluation in diagnosis of insulinoma with PET/CT
10.3760/cma.j.cn321828-20231103-00094
- VernacularTitle:18F标记胰高血糖素样肽-1受体激动剂探针的合成及在胰岛素瘤PET/CT诊断中的初步评价
- Author:
Yunfei XIE
1
;
Nan LIU
;
Zhaohui LIU
;
Limeng HE
;
Huan MA
;
Hao LIU
;
Hao WANG
;
Haiyan GAO
;
Weiwei ZHANG
;
Wei ZHANG
Author Information
1. 四川省医学科学院·四川省人民医院（电子科技大学附属医院）核医学科，成都 610072
- Keywords:
Insulinoma;
Glucagon-like peptide-1 receptor agonists;
Exenatide;
Fluorine radioisotopes;
Positron-emission tomography;
Tomography, X-ray computed
- From:
Chinese Journal of Nuclear Medicine and Molecular Imaging
2024;44(11):673-677
- CountryChina
- Language:Chinese
-
Abstract:
Objective:To explore the automated synthesis of glucagon-like peptide-1 receptor agonist 18F-AlF-1, 4, 7-triazacyclononane-1, 4, 7-triacetic acid (NOTA)-maleimide (Mal)-cysteine (Cys) 39-exendin-4 ( 18F-exendin-4), and verify its diagnostic efficacy on insulinoma with PET/CT. Methods:Using NOTA-Mal-Cys 39-exendin-4 as the labeled precursor, 18F-exendin-4 was obtained by constructing Al 18F one-step reaction sequence and using All in one multifunctional chemical synthesizer for radiolabelling, purification and preparation. After the quality control, 18F-exendin-4 PET/CT imaging was performed on 1 patient (female, 55 years old) with clinical suspicion of insulinoma. Results:Radiolabelling of 18F-exendin-4 took about 40 min, with the non-decay corrected radiochemical yield of (18.03±2.67)% ( n=3), the molar activity>39.74 GBq/μmol, and the radioactivity concentration>390.00 MBq/ml. The injection was a colorless transparent liquid with pH value of 6.5, and the radiochemical purity>96%. Results of bacteria and endotoxins testing met the standards of Pharmacopoeia of the People′ s Republic of China (2020). PET/CT image analysis showed a nodular high uptake of 18F-exendin-4 in the pancreatic body. The pathological and immunohistochemical results were consistent with the characteristics of neuroendocrine neoplasm (G2). Conclusions:The automatic radiolabelling of 18F-exendin-4 is successfully realized by All in one multifunctional chemical synthesizer. 18F-exendin-4 has been proved to be of clinical value in diagnosis of insulinoma, and is suitable for promotion in medical institutions equipped with medical cyclotrons.
