FAPI-74 PET/CT Using Either (18)F-AlF or Cold-Kit (68)Ga Labeling: Biodistribution, Radiation Dosimetry, and Tumor Delineation in Lung Cancer Patients.
FAPI-74 PET/CT Using Either (18)F-AlF or Cold-Kit (68)Ga Labeling: Biodistribution, Radiation Dosimetry, and Tumor Delineation in Lung Cancer Patients.
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使用（18）F-AlF或冷试剂盒（68）Ga标记的FAPI-74 PET/CT：肺癌患者的生物分布，辐射剂量测定和肿瘤描述。
DOI：
10.2967/jnumed.120.245084
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发表时间：
2021-03
期刊：
影响因子：
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通讯作者：
Kratochwil C
中科院分区：
文献类型：
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作者：
Giesel FL;Adeberg S;Syed M;Lindner T;Jiménez-Franco LD;Mavriopoulou E;Staudinger F;Tonndorf-Martini E;Regnery S;Rieken S;El Shafie R;Röhrich M;Flechsig P;Kluge A;Altmann A;Debus J;Haberkorn U;Kratochwil C
68 Ga-成纤维细胞活化蛋白抑制剂（FAPI）2、4和46已经被提出作为有前景的PET示踪剂。然而，68 Ga的半衰期短（68分钟），在生产和运输方面产生了问题。18F（半衰期，110分钟）标记将导致更实际的大规模生产，冷盒制剂将提高自发可用性。NOTA螯合剂配体FAPI-74可以用18F-AlF和68 Ga两者标记。在这里，我们描述了18F-FAPI-74的体内评价和在环境温度下标记的68 Ga-FAPI-74的机制的证据。方法：10例肺癌患者，在给予259 ± 26 MBq的18 F-FAPI-74后10 min、1 h和3 h进行PET扫描。在每个时间点基于SUV半定量评价生理生物分布和肿瘤摄取。使用OLINDA/EXM（版本1.1）和QDOSE剂量测定软件（带有剂量计算器IDAC-Dose（版本2.1））评价吸收剂量。使用相同的方法评价注射263 MBq 68 Ga-FAPI-74后的一次检查。结果如下：在注射后1小时，原发性肿瘤、淋巴结和远处转移瘤中实现了最高对比度，SUVmax超过10。18F-FAPI-74的每100-MBq给药活性的有效剂量为1.4 ± 0.2 mSv，68 Ga-FAPI-74的有效剂量为1.6 mSv。因此，诊断性18F-FAPI-74 PET扫描的辐射负荷甚至低于使用18F-FDG和其他18F示踪剂的PET扫描的辐射负荷; 68 Ga-FAPI-74与其他68 Ga配体相当。FAPI PET/CT支持的靶体积定义，用于指导放射治疗。结论：FAPI-74 PET/CT的高对比度和低辐射负荷有利于多种临床应用。18F-FAPI-74的集中式大规模生产或68 Ga-FAPI-74的分散式冷试剂盒标记允许灵活的常规使用。
68Ga-fibroblast activation protein inhibitors (FAPIs) 2, 4, and 46 have already been proposed as promising PET tracers. However, the short half-life of 68Ga (68 min) creates problems with manufacture and delivery. 18F (half-life, 110 min) labeling would result in a more practical large-scale production, and a cold-kit formulation would improve the spontaneous availability. The NOTA chelator ligand FAPI-74 can be labeled with both 18F-AlF and 68Ga. Here, we describe the in vivo evaluation of 18F-FAPI-74 and a proof of mechanism for 68Ga-FAPI-74 labeled at ambient temperature. Methods: In 10 patients with lung cancer, PET scans were acquired at 10 min, 1 h, and 3 h after administration of 259 ± 26 MBq of 18F-FAPI-74. Physiologic biodistribution and tumor uptake were semiquantitatively evaluated on the basis of SUV at each time point. Absorbed doses were evaluated using OLINDA/EXM, version 1.1, and QDOSE dosimetry software with the dose calculator IDAC-Dose, version 2.1. Identical methods were used to evaluate one examination after injection of 263 MBq of 68Ga-FAPI-74. Results: The highest contrast was achieved in primary tumors, lymph nodes, and distant metastases at 1 h after injection, with an SUVmax of more than 10. The effective dose per a 100-MBq administered activity of 18F-FAPI-74 was 1.4 ± 0.2 mSv, and for 68Ga-FAPI-74 it was 1.6 mSv. Thus, the radiation burden of a diagnostic 18F-FAPI-74 PET scan is even lower than that of PET scans with 18F-FDG and other 18F tracers; 68Ga-FAPI-74 is comparable to other 68Ga ligands. FAPI PET/CT supported target volume definition for guiding radiotherapy. Conclusion: The high contrast and low radiation burden of FAPI-74 PET/CT favor multiple clinical applications. Centralized large-scale production of 18F-FAPI-74 or decentralized cold-kit labeling of 68Ga-FAPI-74 allows flexible routine use.