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Research ArticleTheranostics
Open Access

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, Dirk Jäger, Paul Flechsig, Annette Altmann, Walter Mier and Uwe Haberkorn
Journal of Nuclear Medicine March 2019, 60 (3) 386-392; DOI: https://doi.org/10.2967/jnumed.118.215913
Frederik L. Giesel
1Department of Nuclear Medicine, University Hospital Heidelberg, Heidelberg Germany
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Clemens Kratochwil
1Department of Nuclear Medicine, University Hospital Heidelberg, Heidelberg Germany
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Thomas Lindner
1Department of Nuclear Medicine, University Hospital Heidelberg, Heidelberg Germany
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Manfred M. Marschalek
1Department of Nuclear Medicine, University Hospital Heidelberg, Heidelberg Germany
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Anastasia Loktev
1Department of Nuclear Medicine, University Hospital Heidelberg, Heidelberg Germany
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Wencke Lehnert
2ABX-CRO Advanced Pharmaceutical Services Forschungsgesellschaft m.b.H, Dresden, Germany
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Jürgen Debus
3Department of Radiation Oncology, University Hospital Heidelberg, Heidelberg, Germany
4Clinical Cooperation Unit Radiation Oncology, German Cancer Research Center, Heidelberg, Germany
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Dirk Jäger
5Department of Medical Oncology, National Center for Tumor Diseases, Heidelberg, Germany
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Paul Flechsig
1Department of Nuclear Medicine, University Hospital Heidelberg, Heidelberg Germany
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Annette Altmann
1Department of Nuclear Medicine, University Hospital Heidelberg, Heidelberg Germany
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Walter Mier
1Department of Nuclear Medicine, University Hospital Heidelberg, Heidelberg Germany
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Uwe Haberkorn
1Department of Nuclear Medicine, University Hospital Heidelberg, Heidelberg Germany
6Clinical Cooperation Unit Nuclear Medicine, German Cancer Research Center, Heidelberg, Germany; and
7Translational Lung Research Center Heidelberg, German Center for Lung Research, Heidelberg, Germany
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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.

  • radiotracer tissue kinetics
  • cancer-associated fibroblasts
  • PET/CT
  • biodistribution
  • dosimetry
  • fibroblast activation protein

Footnotes

  • Published online Aug. 2, 2018.

  • © 2019 by the Society of Nuclear Medicine and Molecular Imaging.

Immediate Open Access: Creative Commons Attribution 4.0 International License (CC BY) allows users to share and adapt with attribution, excluding materials credited to previous publications. License: https://creativecommons.org/licenses/by/4.0/. Details: http://jnm.snmjournals.org/site/misc/permission.xhtml.

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Journal of Nuclear Medicine: 60 (3)
Journal of Nuclear Medicine
Vol. 60, Issue 3
March 1, 2019
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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, Dirk Jäger, Paul Flechsig, Annette Altmann, Walter Mier, Uwe Haberkorn
Journal of Nuclear Medicine Mar 2019, 60 (3) 386-392; DOI: 10.2967/jnumed.118.215913

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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, Dirk Jäger, Paul Flechsig, Annette Altmann, Walter Mier, Uwe Haberkorn
Journal of Nuclear Medicine Mar 2019, 60 (3) 386-392; DOI: 10.2967/jnumed.118.215913
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Keywords

  • radiotracer tissue kinetics
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