Radioligands targeting fibroblast activation protein (FAP)

• Verfasst von: Lindner, Thomas [VerfasserIn]
• Verfasst von: Giesel, Frederik L. [VerfasserIn]
• Verfasst von: Kratochwil, Clemens [VerfasserIn]
• Verfasst von: Serfling, Sebastian E. [VerfasserIn]
• Titel: Radioligands targeting fibroblast activation protein (FAP)
• Verf.angabe: Thomas Lindner, Frederik L. Giesel, Clemens Kratochwil and Sebastian E. Serfling
• E-Jahr: 2021
• Jahr: 16 November 2021
• Umfang: 12 S.
• Fussnoten: Gesehen am 04.06.2022
• Titel Quelle: Enthalten in: Cancers
• Ort Quelle: Basel : MDPI, 2009
• Jahr Quelle: 2021
• Band/Heft Quelle: 13(2021), 22, Artikel-ID 5744, Seite 1-12
• ISSN Quelle: 2072-6694
• DOI: doi:10.3390/cancers13225744
• Datenträger: Online-Ressource
• Sprache: eng
• Sach-SW: cancer associated fibroblasts
• Sach-SW: drug discovery
• Sach-SW: FAP
• Sach-SW: radiopharmaceuticals
• K10plus-PPN: 1806076128

Abstract

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.