An 18 F-labelled HER2 receptor binding radiotracer is a potential tool to non-invasively identify HER2 positive tumour lesions in subjects with recurrent metastatic breast cancer. Having explored the manual radiochemistry to conjugate the Affibody molecule ZHER2:2891 with [18 F]4-fluorobenzaldehyde, we have developed and optimized a full protocol for the automated GE FASTlabTM synthesiser. Our chemometric model predicted the best radiochemical purity for a short conjugation time (2.8 min), a low temperature (65o C), and a medium Affibody molecule precursor amount (5.5 mg). Under these optimised conditions [18 F]GE-226 was produced after solid-phase extraction purification with activity yield of 30% ± 7 (n = 18) and a radiochemical purity of 94% ± 2 (n = 18). The synthesis and purification was complete after 43 minutes and provided apparent molar activities of 12-30 GBq/μmol (n = 12) at the end of synthesis.

中文翻译：

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18 F 标记的 HER2 结合 Affibody 分子 [18 F]GE-226 的 FASTlab 放射合成

18 F 标记的 HER2 受体结合放射性示踪剂是一种潜在的工具，可用于非侵入性地识别复发转移性乳腺癌患者的 HER2 阳性肿瘤病变。在探索了手动放射化学以将 Affibody 分子 ZHER2:2891 与 [18 F]4-氟苯甲醛结合后，我们开发并优化了自动化 GE FASTlabTM 合成仪的完整方案。我们的化学计量模型预测了在较短的结合时间 (2.8 分钟)、低温 (65o C) 和中等 Affibody 分子前体量 (5.5 mg) 下的最佳放射化学纯度。在这些优化条件下，[18 F]GE-226 在固相萃取纯化后产生，活性产率为 30% ± 7 (n = 18)，放射化学纯度为 94% ± 2 (n = 18)。