Radioligands targeting fibroblast activation protein (FAP)

Targeting fibroblast activation protein (FAP) in cancer-associated fibroblasts (CAFs) has attracted significant attention in nuclear medicine. Since these cells are present in most cancerous tissues and FAP is rarely expressed in healthy tissues, anti-FAP tracers have a potential as pan-tumor agents...

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Hauptverfasser: Lindner, Thomas (VerfasserIn) , Giesel, Frederik L. (VerfasserIn) , Kratochwil, Clemens (VerfasserIn) , Serfling, Sebastian E. (VerfasserIn)
Dokumenttyp: Article (Journal)
Sprache:Englisch
Veröffentlicht: 16 November 2021
In: Cancers
Year: 2021, Jahrgang: 13, Heft: 22, Pages: 1-12
ISSN:2072-6694
DOI:10.3390/cancers13225744
Online-Zugang:Verlag, lizenzpflichtig, Volltext: https://doi.org/10.3390/cancers13225744
Verlag, lizenzpflichtig, Volltext: https://www.mdpi.com/2072-6694/13/22/5744
Volltext
Verfasserangaben:Thomas Lindner, Frederik L. Giesel, Clemens Kratochwil and Sebastian E. Serfling

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520 |a Targeting fibroblast activation protein (FAP) in cancer-associated fibroblasts (CAFs) has attracted significant attention in nuclear medicine. Since these cells are present in most cancerous tissues and FAP is rarely expressed in healthy tissues, anti-FAP tracers have a potential as pan-tumor agents. Compared to the standard tumor tracer [18F]FDG, these tracers show better tumor-to-background ratios (TBR) in many indications. Unlike [18F]FDG, FAP-targeted tracers do not require exhausting preparations, such as dietary restrictions on the part of the patient, and offer the possibility of radioligand therapy (RLT) in a theragnostic approach. Although a radiolabeled antibody was clinically investigated as early as the 1990s, the breakthrough event for FAP-targeting in nuclear medicine was the introduction and clinical application of the so-called FAPI-tracers in 2018. From then, the development and application of FAP-targeted tracers became hot topics for the radiopharmaceutical and nuclear medicine community, and attracted the interest of pharmaceutical companies. The aim of this review is to provide a comprehensive overview of the development of FAP-targeted radiopharmaceuticals and their application in nuclear medicine. 
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