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[18F]AlF-NOTA-TATE的制备及初步临床应用

刘欢欢 张晓军 麻广宇 张锦明

同位素2024,Vol.37Issue(4):379-386,8.
同位素2024,Vol.37Issue(4):379-386,8.DOI:10.7538/tws.2024.youxian.015

[18F]AlF-NOTA-TATE的制备及初步临床应用

Preparation and Preliminary Clinical Application of[18F]AlF-NOTA-TATE

刘欢欢 1张晓军 2麻广宇 2张锦明2

作者信息

  • 1. 中国人民解放军总医院第一医学中心核医学科,北京 100853||解放军医学院,北京 100853
  • 2. 中国人民解放军总医院第一医学中心核医学科,北京 100853
  • 折叠

摘要

Abstract

68Ga-DOTA-TATE has been successfully applied in the diagnosis of clinical neuroendocrine tumors,but its short half-life limits its widespread use.This study aimed to develop[18F]AlF-NOTA-TATE to meet the clinical demands of patients with neuroendocrine tumors(NETs)for diagnosis and treatment evaluation.A new column chromatography purification method for[18F]AlF-NOTA-TATE was developed and automated synthesis was performed using a clinical single-vessel multi-functional fluorine synthesis module.The lipophilicity,in vitro stability,and pharmacokinetics of[18F]AlF-NOTA-TATE were studied,and biodistribution experiments and PET/CT imaging of nude mice with NCI-H69(SSTR2 positive expression)small cell lung cancer were conducted,followed by preliminary clinical evaluation on three patients with neuroendocrine tumors.The new column chromatography purification method for[18F]AlF-NOTA-TATE was simple,which was synthesized in a short time with higher than 95%of radiochemical purity and,less than 3%of.ethanol content.Pharmacokinetic and biodistribution experiments in BALB/c mice showed rapid blood clearance of the drug and renal metabolism.PET/CT imaging of tumor-bearing mice showed specific uptake of the radiotracer in SSTR-positive tumors.Preliminary clinical application showed that[18F]AlF-NOTA-TATE is well targeted in patients with long retention time and can provide better image quality.The column chromatography method for the preparation of[18F]AlF-NOTA-TATE was simple and had high radiochemical purity.Preliminary clinical results suggested that[18F]AlF-NOTA-TATE has further value for clinical research.

关键词

[18F]AlF-NOTA-TATE/柱色层纯化/神经内分泌肿瘤/临床应用

Key words

[18F]AlF-NOTA-TATE/column color layer purification/neuroendocrine tumors/clinical application

分类

能源科技

引用本文复制引用

刘欢欢,张晓军,麻广宇,张锦明..[18F]AlF-NOTA-TATE的制备及初步临床应用[J].同位素,2024,37(4):379-386,8.

基金项目

国家同位素工程技术研究中心开放课题资助项目(GJTESGCZX-202307) (GJTESGCZX-202307)

同位素

OACSTPCD

1000-7512

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