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Updated: Sep 8, 2025
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Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment
Published on: April 25, 2025
FAPI-PET/CT in Cancer Imaging: A Potential Novel Molecule of the Century
Rong Huang1, Yu Pu2, Shun Huang3
1Department of PET/CT Center, Yunnan Cancer Hospital, The Third Affiliated Hospital of Kunming Medical University, Cancer Center of Yunnan Province, Kunming, China.
Abstract:
Fibroblast activation protein (FAP), a type II transmembrane serine protease, is highly expressed in more than 90% of epithelial tumors and is closely associated with various tumor invasion, metastasis, and prognosis. Using FAP as a target, various FAP inhibitors (FAPIs) have been developed, most of which have nanomolar levels of FAP affinity and high selectivity and are used for positron emission tomography (PET) imaging of different tumors. We have conducted a systematic review of the available data; summarized the biological principles of FAPIs for PET imaging, the synthesis model, and metabolic characteristics of the radiotracer; and compared the respective values of FAPIs and the current mainstream tracer 18F-Fludeoxyglucose (18F-FDG) in the clinical management of tumor and non-tumor lesions. Available research evidence indicates that FAPIs are a molecular imaging tool complementary to 18F-FDG and are expected to be the new molecule of the century with better imaging effects than 18F-FDG in a variety of cancers, including gastrointestinal tumors, liver tumors, breast tumors, and nasopharyngeal carcinoma.
Insights
Fibroblast activation protein inhibitors (FAPIs) show promise for positron emission tomography (PET) imaging in various cancers. FAPIs offer superior tumor visualization compared to 18F-FDG, aiding clinical management.
Area of Science:
- Oncology
- Molecular Imaging
- Radiochemistry
Background:
- Fibroblast activation protein (FAP) is highly expressed in most epithelial tumors, correlating with invasion, metastasis, and prognosis.
- FAP plays a crucial role in tumor progression, making it a significant therapeutic and diagnostic target.
Purpose of the Study:
- To systematically review and summarize the biological principles, synthesis, and metabolic characteristics of FAP inhibitors (FAPIs) for PET imaging.
- To compare the clinical utility of FAPIs with the current standard tracer, 18F-Fludeoxyglucose (18F-FDG), in managing tumor and non-tumor lesions.
Main Methods:
- Systematic review of existing data on FAPIs for PET imaging.
- Analysis of FAPIs' biological principles, synthesis models, and radiotracer characteristics.
- Comparative evaluation of FAPIs and 18F-FDG in clinical applications.
Main Results:
- FAPIs demonstrate high affinity and selectivity for FAP, enabling effective PET imaging of diverse tumors.
- FAPIs serve as a valuable molecular imaging tool, complementing 18F-FDG.
- Evidence suggests FAPIs may offer superior imaging performance over 18F-FDG in various cancers.
Conclusions:
- FAPIs represent a promising advancement in molecular imaging for oncology.
- FAPIs are expected to enhance the diagnostic and prognostic capabilities in managing a wide range of cancers.
- FAPIs are poised to become a significant tool in clinical practice, potentially surpassing 18F-FDG in certain applications.
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