(68)Ga-FAPI PET/CT: Biodistribution and Preliminary Dosimetry Estimate of 2 DOTA-Containing FAP-Targeting Agents in Patients with Various Cancers.
(68)Ga-FAPI PET/CT: Biodistribution and Preliminary Dosimetry Estimate of 2 DOTA-Containing FAP-Targeting Agents in Patients with Various Cancers.
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DOI：
10.2967/jnumed.118.215913
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发表时间：
2019-03
期刊：
影响因子：
--
通讯作者：
Haberkorn U
中科院分区：
文献类型：
--
作者：
Giesel FL;Kratochwil C;Lindner T;Marschalek MM;Loktev A;Lehnert W;Debus J;Jäger D;Flechsig P;Altmann A;Mier W;Haberkorn U
成纤维细胞活化蛋白（FAP）在几种肿瘤实体的癌症相关成纤维细胞中过表达。作为FAP抑制剂（FAPI）的基于喹啉的PET示踪剂的最新发展在临床前和在一些临床病例中显示出有希望的结果。因此，这些示踪剂现在应用于我们医院，以修改面临标准检查限制的癌症患者的诊断。在这里，我们分析的组织生物分布和初步剂量测定的2名成员，这一类新的PET放射性药物。研究方法：68 Ga-FAPI-2和68 Ga-FAPI-4的初步剂量测定估计基于使用QDOSE剂量测定软件套装在示踪剂注射后0.2、1和3小时检查的2名患者。在注射68 Ga-FAPI-2（n = 25）或68 Ga-FAPI-4（n = 25）后1小时获得肿瘤患者的进一步PET/CT扫描;对于6名患者，可获得个体内相关的18F-FDG扫描（也在注射后1小时获得）。对于16个器官的正常组织，将2 cm球形感兴趣体积放置在实质中;对于肿瘤病变，使用阈值分割的感兴趣体积来量化SUVmean和SUVmax。结果如下：与18F-FDG、68 Ga-DOTATATE和68 Ga-PSMA-11的文献值类似，用200 MBq的68 Ga-FAPI-2或68 Ga-FAPI-4进行检查对应于约3-4 mSv的等效剂量。在通过肾脏快速清除后，正常器官显示出低示踪剂摄取，注射后10分钟至3小时之间仅发生最小变化。在68 Ga-FAPI-2中，注射后1至3小时的肿瘤摄取减少了75%，而68 Ga-FAPI-4延长了肿瘤保留（25%洗脱）。关于肿瘤与背景比率，在注射后1小时，两种68 Ga-FAPI示踪剂表现相同。与18 F-FDG相比，肿瘤摄取几乎相等（平均SUVmax，18 F-FDG为7.41，68 Ga-FAPI-2为7.37;无统计学显著性）; 68 Ga-FAPI在脑（11.01 vs. 0.32）、肝（2.77 vs. 1.69）和口腔/咽粘膜（4.88 vs. 2.57）中的背景摄取显著较低。其他器官在18F-FDG和68 Ga-FAPI之间没有相关差异。结论：FAPI PET/CT是一种新的肿瘤影像诊断方法。与18F-FDG相比，在检查准备过程中不需要节食或禁食，并且可以在示踪剂应用后几分钟开始图像采集。肿瘤与背景的对比度等于或甚至优于18F-FDG。
Fibroblast activation protein (FAP) is overexpressed in cancer-associated fibroblasts of several tumor entities. The recent development of quinoline-based PET tracers that act as FAP inhibitors (FAPIs) demonstrated promising results preclinically and already in a few clinical cases. Consequently, these tracers are now applied in our hospital to amend the diagnostics of cancer patients facing the limitations of standard examinations. Here, we analyze the tissue biodistribution and preliminary dosimetry of 2 members of this new class of PET radiopharmaceutical. Methods: A preliminary dosimetry estimate for 68Ga-FAPI-2 and 68Ga-FAPI-4 was based on 2 patients examined at 0.2, 1, and 3 h after tracer injection using the QDOSE dosimetry software suit. Further PET/CT scans of tumor patients were acquired 1 h after injection of either 68Ga-FAPI-2 (n = 25) or 68Ga-FAPI-4 (n = 25); for 6 patients an intraindividual related 18F-FDG scan (also acquired 1 h after injection) was available. For the normal tissue of 16 organs, a 2-cm spheric volume of interest was placed in the parenchyma; for tumor lesions, a threshold-segmented volume of interest was used to quantify SUVmean and SUVmax. Results: Similar to literature values for 18F-FDG, 68Ga-DOTATATE, and 68Ga-PSMA-11, an examination with 200 MBq of 68Ga-FAPI-2 or 68Ga-FAPI-4 corresponds to an equivalent dose of approximately 3–4 mSv. After a fast clearance via the kidneys, the normal organs showed a low tracer uptake with only minimal changes between 10 min and 3 h after injection. In 68Ga-FAPI-2, the tumor uptake from 1 to 3 h after injection decreased by 75%, whereas the tumor retention was prolonged with 68Ga-FAPI-4 (25% washout). Regarding tumor-to-background ratios, at 1 h after injection both 68Ga-FAPI tracers performed equally. In comparison to 18F-FDG, the tumor uptake was almost equal (average SUVmax, 7.41 for 18F-FDG and 7.37 for 68Ga-FAPI-2; not statistically significant); the background uptake in brain (11.01 vs. 0.32), liver (2.77 vs. 1.69), and oral/pharyngeal mucosa (4.88 vs. 2.57) was significantly lower with 68Ga-FAPI. Other organs did not relevantly differ between 18F-FDG and 68Ga-FAPI. Conclusion: FAPI PET/CT is a new diagnostic method in imaging cancer patients. In contrast to 18F-FDG, no diet or fasting in preparation for the examination is necessary, and image acquisition can potentially be started a few minutes after tracer application. Tumor-to-background contrast ratios were equal to or even better than those of 18F-FDG.
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影响因子：
7.3
作者：
Poplawski, Sarah E.;Lai, Jack H.;Li, Youhua;Jin, Zhiping;Liu, Yuxin;Wu, Wengen;Wu, Yong;Zhou, Yuhong;Sudmeier, James L.;Sanford, David G.;Bachovchin, William W.
通讯作者：
Bachovchin, William W.
影响因子：
3.2
作者：
Andersson M;Johansson L;Eckerman K;Mattsson S
通讯作者：
Mattsson S
影响因子：
--
作者：
Bolch, W. E.;Jokisch, D.;Petoussi-Henss, N.
通讯作者：
Petoussi-Henss, N.
DOI：
10.1007/s00259-016-3419-0
发表时间：
2016-08-01
影响因子：
9.1
作者：
Afshar-Oromieh, Ali;Hetzheim, Henrik;Haberkorn, Uwe
通讯作者：
Haberkorn, Uwe
影响因子：
5
作者：
Tillmanns, Jochen;Hoffmann, Daniel;Bauersachs, Johann
通讯作者：
Bauersachs, Johann