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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Autores principales:	Thomas Lindner, Frederik L. Giesel, Clemens Kratochwil, Sebastian E. Serfling
Formato:	article
Lenguaje:	EN
Publicado:	MDPI AG 2021
Materias:	FAP cancer associated fibroblasts radiopharmaceuticals drug discovery Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
Acceso en línea:	https://doaj.org/article/806a99aef7c14ba2b30010100bdc293f
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spelling	oai:doaj.org-article:806a99aef7c14ba2b30010100bdc293f2021-11-25T17:03:31ZRadioligands Targeting Fibroblast Activation Protein (FAP)10.3390/cancers132257442072-6694https://doaj.org/article/806a99aef7c14ba2b30010100bdc293f2021-11-01T00:00:00Zhttps://www.mdpi.com/2072-6694/13/22/5744https://doaj.org/toc/2072-6694Targeting 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 [<sup>18</sup>F]FDG, these tracers show better tumor-to-background ratios (TBR) in many indications. Unlike [<sup>18</sup>F]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.Thomas LindnerFrederik L. GieselClemens KratochwilSebastian E. SerflingMDPI AGarticleFAPcancer associated fibroblastsradiopharmaceuticalsdrug discoveryNeoplasms. Tumors. Oncology. Including cancer and carcinogensRC254-282ENCancers, Vol 13, Iss 5744, p 5744 (2021)
institution	DOAJ
collection	DOAJ
language	EN
topic	FAP cancer associated fibroblasts radiopharmaceuticals drug discovery Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282
spellingShingle	FAP cancer associated fibroblasts radiopharmaceuticals drug discovery Neoplasms. Tumors. Oncology. Including cancer and carcinogens RC254-282 Thomas Lindner Frederik L. Giesel Clemens Kratochwil Sebastian E. Serfling Radioligands Targeting Fibroblast Activation Protein (FAP)
description	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 [<sup>18</sup>F]FDG, these tracers show better tumor-to-background ratios (TBR) in many indications. Unlike [<sup>18</sup>F]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.
format	article
author	Thomas Lindner Frederik L. Giesel Clemens Kratochwil Sebastian E. Serfling
author_facet	Thomas Lindner Frederik L. Giesel Clemens Kratochwil Sebastian E. Serfling
author_sort	Thomas Lindner
title	Radioligands Targeting Fibroblast Activation Protein (FAP)
title_short	Radioligands Targeting Fibroblast Activation Protein (FAP)
title_full	Radioligands Targeting Fibroblast Activation Protein (FAP)
title_fullStr	Radioligands Targeting Fibroblast Activation Protein (FAP)
title_full_unstemmed	Radioligands Targeting Fibroblast Activation Protein (FAP)
title_sort	radioligands targeting fibroblast activation protein (fap)
publisher	MDPI AG
publishDate	2021
url	https://doaj.org/article/806a99aef7c14ba2b30010100bdc293f
work_keys_str_mv	AT thomaslindner radioligandstargetingfibroblastactivationproteinfap AT frederiklgiesel radioligandstargetingfibroblastactivationproteinfap AT clemenskratochwil radioligandstargetingfibroblastactivationproteinfap AT sebastianeserfling radioligandstargetingfibroblastactivationproteinfap
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Radioligands Targeting Fibroblast Activation Protein (FAP)

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