Abstract：
Objective: [68Ga]Ga-DOTA-FGFR1-peptide is a novel positron emission tomography (PET) radiotracer targeting fibroblast growth factor receptor 1 (FGFR1). This study aimed to evaluate the safety, biodistribution, radiation dosimetry, and imaging potential of [68Ga]Ga-DOTA-FGFR1-peptide. Methods: The FGFR1-targeting peptide DOTA-(PEG2)-KAEWKSLGEEAWHSK was synthesized by manual solid-phase peptide synthesis and high-performance liquid chromatography purification, and labeled with 68Ga with DOTA as chelating agent. We recruited 14 participants and calculated the radiation dose of 4 of these pathologically confirmed nontumor subjects using OLINDA/EXM 2.2.0 software. At the same time, the imaging potential in 10 of these lung cancer patients was evaluated. Results: The biodistribution of [68Ga]Ga-DOTA-FGFR1-peptide in 4 subjects showed the highest uptake in the bladder and kidney. Dosimetry analysis indicated that the bladder wall received the highest effective dose (3.73E-02 mSv/MBq), followed by the lungs (2.36E-03 mSv/MBq) and red bone marrow (2.09E-03 mSv/MBq). No normal organs were found to have excess specific absorbed doses. The average systemic effective dose was 4.97E-02 mSv/MBq. The primary and metastatic tumor lesions were clearly visible on PET/computed tomography (CT) images in 10 patients. Conclusion: Our results indicate that [68Ga]Ga-DOTA-FGFR1-peptide has a good dosimetry profile and can be used safely in humans, and it has significant potential value for clinical PET/CT imaging.
摘要：
目的：[68Ga]Ga-DOTA-FGFR1-肽是一种新型的正电子发射断层扫描（PET）放射性示踪剂，靶向成纤维细胞生长因子受体1（FGFR1）。本研究旨在评估安全性，生物分布，辐射剂量测定，和[68Ga]Ga-DOTA-FGFR1-肽的成像电位。方法:采用手工固相肽合成和高效液相色谱纯化的方法合成FGFR1靶向肽DOTA-(PEG2)-KAEWKSLGEEAWHSK,并用作为螯合剂的DOTA标记68Ga。我们招募了14名参与者，并使用OLINDA/EXM2.2.0软件计算了其中4名经病理证实的非肿瘤受试者的辐射剂量。同时,对其中10例肺癌患者的影像学潜能进行了评估.结果：[68Ga]Ga-DOTA-FGFR1-肽在4位受试者中的生物分布显示在膀胱和肾脏中的摄取最高。剂量学分析表明膀胱壁接受最高有效剂量（3.73E-02mSv/MBq），其次是肺（2.36E-03mSv/MBq）和红骨髓（2.09E-03mSv/MBq）。没有发现正常器官具有过量的特定吸收剂量。平均全身有效剂量为4.97E-02mSv/MBq。在10例患者的PET/计算机断层扫描（CT）图像上清晰可见原发性和转移性肿瘤病变。结论：我们的结果表明[68Ga]Ga-DOTA-FGFR1-肽具有良好的剂量学特征，可以安全地用于人类。临床PET/CT成像具有重要的潜在价值。
