表皮生长因子受体显像剂18F-FEA-Erlotinib的自动化合成

Translated title of the contribution: Automated synthesis of EGFR imaging tracer 18F-FEA-Erlotinib

Shun Huang, Yanjiang Han, Kongzhen Hu, Meng Wang, Penghui Sun, Hubing Wu, Quanshi Wang, Suqing Zhao, Xi Zheng

Research output: Contribution to journalArticlepeer-review

Abstract

Background: PET imaging of 11C-Erlotinib was used to distinguish responders from nonresponders in the targeted therapy for non-small cell lung cancer (NSCLC). However, the short half-life (20 min) of carbon-11 limits its widespread use as a tool for community-based diagnostic screening and therapeutic evaluation. We proposed that this shortcoming could be overcome by the development of a fluorine-18 (half-life is 109 min) labeled Erlotinib. Purpose: We automatically labelled Erlotinib with flurorine-18 through the "click chemistry" and explored its preliminary evaluation. Methods: 18F-FEA-Erlotinib was synthesized from 2-18F-fluorine azide ethane (18F-FEA), a radiochemical intermediate, through the "click chemistry" in the PET-MF-2V-IT-I synthesis module and purified by semi-preparative high performance liquid chromatography (HPLC). The stability of 18F-FEA-Erlotinib was performed in phosphate buffer saline (PBS) and fetal bovine serum (FBS). The octanol/water partition coefficient and routine quality control were tested. Results: 18F-FEA-Erlotinib was achieved within 70 min with (54±2)% radiochemical yield (decay corrected), an average specific activity over 200MBq∙μmol-1, and over 99% radiochemical purity. The logP of 18F-FEA-Erlotinib was 2.36±0.01. The final injection was free of bacteria and pyrogen, and the K2.2.2 concentration was lower than 10 mg∙L-1. Conclusion: 18F-FEA-Erlotinib was easy to be prepared by the "click chemistry" in an automatic synthesis system. 18F-FEA-Erlotinib has a similar lipophilicity to Erlotinib and a high metabolic stability in vitro.

Translated title of the contributionAutomated synthesis of EGFR imaging tracer 18F-FEA-Erlotinib
Original languageChinese
Article number010301
JournalHe Jishu/Nuclear Techniques
Volume41
Issue number1
DOIs
StatePublished - Jan 10 2018
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Radiation
  • Nuclear and High Energy Physics
  • Nuclear Energy and Engineering

Keywords

  • Click chemistry
  • Epidermal growth factor receptor
  • F-FEA-Erlotinib
  • Fully automated synthesis

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