68Ga-FAPI PET/CT: Biodistribution and Preliminary Dosimetry Estimate of 2 DOTA-Containing FAP-Targeting Agents in Patients with Various Cancers.
Frederik L. Giesel,Clemens Kratochwil,Thomas Lindner,Manfred M. Marschalek,Anastasia Loktev,Wencke Lehnert,Jürgen Debus,Jürgen Debus,Dirk Jäger,Paul Flechsig,Annette Altmann,Walter Mier,Uwe Haberkorn +12 more
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TLDR
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.Abstract:
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.read more
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68Ga-FAPI PET/CT: Tracer Uptake in 28 Different Kinds of Cancer
Clemens Kratochwil,Paul Flechsig,Thomas Lindner,Labidi Abderrahim,Annette Altmann,Annette Altmann,Walter Mier,Sebastian Adeberg,Hendrik Rathke,Manuel Röhrich,Hauke Winter,Peter K. Plinkert,Frederik Marmé,Matthias Lang,Hans-Ulrich Kauczor,Dirk Jäger,Dirk Jäger,Jürgen Debus,Jürgen Debus,Uwe Haberkorn,Uwe Haberkorn,Frederik L. Giesel +21 more
TL;DR: The high and rather selective tumor uptake on 68Ga-FAPI PET/CT may open up new applications for noninvasive tumor characterization, staging examinations, or radioligand therapy.
Journal ArticleDOI
Comparison of [68Ga]Ga-DOTA-FAPI-04 and [18F] FDG PET/CT for the diagnosis of primary and metastatic lesions in patients with various types of cancer.
Haojun Chen,Yizhen Pang,Jingxun Wu,Liang Zhao,Bing Hao,Jing Wu,Ji-Hong Wei,Siming Wu,Long Zhao,Zuo-Ming Luo,Xuehua Lin,Chengrong Xie,Long Sun,Qin Lin,Hua Wu +14 more
TL;DR: [68Ga]Ga-DOTA-FAPI-04 PET/CT showed a superior diagnostic efficacy than [18F] FDGPET/CT for the diagnosis of primary and metastatic lesions in patients with various types of cancer, especially in identifying liver metastases, peritoneal carcinomatosis, and brain tumours.
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ImmunoPET: Concept, Design, and Applications
TL;DR: The latest immuno PET imaging strategies and their preclinical and clinical applications are presented and current conjugation strategies that can be leveraged to develop next-generation immunoPET probes are emphasized.
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Development of Fibroblast Activation Protein–Targeted Radiotracers with Improved Tumor Retention
Anastasia Loktev,Anastasia Loktev,Thomas Lindner,Eva Maria Burger,Annette Altmann,Annette Altmann,Frederik L. Giesel,Clemens Kratochwil,Jürgen Debus,Jürgen Debus,Frederik Marmé,Dirk Jäger,Walter Mier,Uwe Haberkorn +13 more
TL;DR: In this paper, quinoline-based radiotracers were synthesized by organic chemistry and evaluated in radioligand binding assays using FAP-expressing HT-1080 cells.
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Future of Theranostics: An Outlook on Precision Oncology in Nuclear Medicine
TL;DR: This review focuses on promising novel radiopharmaceuticals and describes their preclinical and clinical status and highlights Radiolabeled antibodies, such as 131I-omburtamab directed against the B7-H3 protein on the surface of neuroblastoma cells.
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Development of Quinoline-Based Theranostic Ligands for the Targeting of Fibroblast Activation Protein
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