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European Journal of Nuclear Medicine and Molecular Imaging

Erschienen in:

02.06.2023 | Original Article

Noninvasive imaging of FAP expression using positron emission tomography: A comparative evaluation of a [¹⁸F]-labeled glycopeptide-containing FAPI with [¹⁸F]FAPI-42

verfasst von: Jiawen Huang, LiLan Fu, XiaoJun Zhang, Shun Huang, Ye Dong, Kongzhen Hu, YanJiang Han, Kemin Zhou, Cao Min, YanChao Huang, Ganghua Tang

Erschienen in: European Journal of Nuclear Medicine and Molecular Imaging | Ausgabe 11/2023

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Abstract

Purpose

Research on fibroblast activating protein (FAP)-targeting inhibitor (FAPI) has become an important focus for cancer imaging and radiotherapy. Quinoline-based tracers [⁶⁸ Ga]FAPI-04 and [¹⁸F]FAPI-42 have been widely used for positron emission tomography (PET) imaging of most tumors. However, there exist some limitations of these tracers with high uptake in biliary duct system and unstable uptake in pancreas, unsuitable for abdominal tumors PET imaging. Here we developed a [¹⁸F]-labeled glycopeptide-containing FAPI tracer (named [¹⁸F]FAPT) for PET imaging of FAP in cancers.

Methods

[¹⁸F]FAPT was synthesized manually and automatically. The competitive binding to FAP, cellular internalization, and efflux characteristics were examined in vitro using A549-FAP cells. Dynamic MicroPET and biodistribution studies of [¹⁸F]FAPT were then conducted in A549-FAP and U87MG xenograft tumor mouse models compared with [¹⁸F]FAPI-42. Five healthy volunteers and three patients with cancer underwent [¹⁸F]FAPT PET/CT.

Results

Preclinical and clinical studies showed specific binding of [¹⁸F]FAPT to FAP and favorable pharmacokinetic properties with better hydrophilicity, lower uptake in biliary duct system, higher tumor uptake and longer tumor retention compared with [¹⁸F]FAPI-42. The biodistribution of [¹⁸F]FAPT in healthy volunteers and patients with cancer displayed low uptake in most normal tissues except for pancreas, thyroid and salivary gland, which could contribute to high tumor-to-background ratios in most cancers.

Conclusion

[¹⁸F]FAPT is better PET tracer than [¹⁸F]FAPI-42 for imaging of biliary duct system cancer, potentially providing a tool to examine FAP expression in most cancers with high tumor-to-background ratios.

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Titel: Noninvasive imaging of FAP expression using positron emission tomography: A comparative evaluation of a [18F]-labeled glycopeptide-containing FAPI with [18F]FAPI-42
verfasst von: Jiawen Huang
LiLan Fu
XiaoJun Zhang
Shun Huang
Ye Dong
Kongzhen Hu
YanJiang Han
Kemin Zhou
Cao Min
YanChao Huang
Ganghua Tang
Publikationsdatum: 02.06.2023
Verlag: Springer Berlin Heidelberg
Erschienen in: European Journal of Nuclear Medicine and Molecular Imaging / Ausgabe 11/2023
Print ISSN: 1619-7070
Elektronische ISSN: 1619-7089
DOI: https://doi.org/10.1007/s00259-023-06282-5

Live-Webinar "Urologie und Sexualmedizin in der Praxis"

Springer Medizin

Noninvasive imaging of FAP expression using positron emission tomography: A comparative evaluation of a [¹⁸F]-labeled glycopeptide-containing FAPI with [¹⁸F]FAPI-42

Abstract

Purpose

Methods

Results

Conclusion

Live-Webinar "Urologie und Sexualmedizin in der Praxis"

Springer Medizin

Abstract

Purpose

Methods

Results

Conclusion

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