Background: Integrin αvβ6 has become an extremely promising theranostic target for precise delineation of fast-growing malignant cells in the recent years. The aim of the study was to validate the in-house kit-like synthesis of 68Ga-Trivehexin (integrin αvβ6) and to evaluate its uptake in patients with integrin αvβ6 expressing head and neck and pancreatic cancer. Materials and Methods: 68Ga-Trivehexin was synthesized by adding the variable amount of integrin αvβ6 (30-50 μg) to full volume (4-5 mL) Ga-68 in 0.05 M HCl and heating the reaction mixture at 90°C for 12 min at pH 3.5-4 to obtain the radiotracer with high radiochemical purity (RCP) and high yield. Quality control procedures were done to assess the RCP, stability, pyrogenicity and sterility of the radiotracer. 68Ga-Trivehexin was then administered in patients who met the eligibility criteria. Whole body PET/CT scans were done at variable time points post intravenous (i.v.) injection of 84-185 MBq of 68Ga-Trivehexin to assess its biodistribution and maximum uptake time. Results: 0.2 mCi of 68Ga/μg of Trivehexin at 90°C for 12 min was the optimal parameter to obtain 85%-88% of noncorrected yield and 99% of RCP. The 68Ga-Trivehexin showed in vitro stability upto 6 h and was also found to be sterile and pyrogen free. Intense radiotracer uptake was noticed in the tumor and no uptake was noticed in healthy tissues. PET/CT imaging at 60 min post injection was found to be the optimal time for imaging the tumors with 68Ga-Trivehexin. Conclusion: The protocol for in-house kit-like labeling of 68Ga-Trivehexin was safe, reproducible, and cost-effective. 68Ga-Trivehexin is an extremely promising agent for noninvasive molecular imaging of integrin αvβ6 expressing tumors.

中文翻译：

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验证 68Ga-Trivehexin 的内部试剂盒式合成及其针对表达整合素 αvβ6 的肿瘤的生物分布。

背景：近年来，整合素αvβ6已成为一种非常有前途的治疗诊断靶点，可用于精确描绘快速生长的恶性细胞。该研究的目的是验证 68Ga-Trivehexin（整合素 αvβ6）的内部试剂盒式合成，并评估其在表达整合素 αvβ6 的头颈癌和胰腺癌患者中的摄取情况。材料和方法：通过将不同量的整合素 αvβ6 (30-50 μg) 添加到全体积 (4-5 mL) Ga-68 的 0.05 M HCl 溶液中，并将反应混合物在 90°C 加热 12 小时，合成 68Ga-Trivehexin。分钟在pH 3.5-4下获得高放射化学纯度（RCP）和高产率的放射性示踪剂。进行质量控制程序以评估放射性示踪剂的 RCP、稳定性、热原性和无菌性。然后对符合资格标准的患者施用 68Ga-Trivehexin。在静脉内 (iv) 注射 84-185 MBq 68Ga-Trivehexin 后的不同时间点进行全身 PET/CT 扫描，以评估其生物分布和最大摄取时间。结果：0.2 mCi 68Ga/μg Trivehexin 在 90°C 下 12 分钟是获得 85%-88% 未校正产率和 99% RCP 的最佳参数。68Ga-Trivehexin 在体外表现出长达 6 小时的稳定性，并且还被发现是无菌且无热原的。在肿瘤中观察到强烈的放射性示踪剂摄取，而在健康组织中未观察到摄取。注射后 60 分钟进行 PET/CT 成像被发现是使用 68Ga-Trivehexin 对肿瘤进行成像的最佳时间。结论：68Ga-Trivehexin 的内部试剂盒式标记方案安全、可重复且具有成本效益。68Ga-Trivehexin 是一种非常有前途的药物，可用于表达整合素 αvβ6 的肿瘤的无创分子成像。