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Updated: Oct 11, 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
Fibroblast-Activated Protein Inhibitor PET/CT: Cancer Diagnosis and Management
Serkan Kuyumcu1, Yasemin Sanli1, Rathan M Subramaniam2,3
1Department of Nuclear Medicine, Istanbul Faculty of Medicine, Istanbul University, Istanbul, Turkey.
Abstract:
Fibroblast activation protein (FAP), overexpressed on cancer-associated fibroblasts (CAFs), is a novel target for molecular imaging of various tumors. Recently, the development of several small-molecule FAP inhibitors for radiolabeling with 68Ga has resulted in the emergence of studies evaluating its clinical role in cancer imaging. Preliminary findings have demonstrated that, in contrast to radiotracers taking advantage of cancer-specific targets such as PSMA and DOTATATE, FAPs as a target are the most promising that can compete with 18FDG in terms of widespread indications. They also have the potential to overcome the shortcomings of 18FDG, particularly false-positive uptake due to inflammatory or infectious processes, low sensitivity in certain cancer types, and radiotherapy planning. In addition, the attractive theranostic properties may facilitate the treatment of many refractory cancers. This review summarizes the current FAP variants and related clinical studies, focusing on radiopharmacy, dosimetry, and diagnostic and theranostic applications.
Insights
Fibroblast activation protein (FAP) imaging shows promise for various cancers, potentially outperforming 18FDG by reducing false positives and improving radiotherapy planning. This review explores FAP inhibitors for diagnostics and theranostics.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging
Background:
- Fibroblast activation protein (FAP) is overexpressed on cancer-associated fibroblasts (CAFs).
- Small-molecule FAP inhibitors labeled with 68Ga are emerging for molecular imaging.
- FAP imaging offers potential advantages over 18FDG, including fewer false positives and broader applications.
Purpose of the Study:
- To review current FAP variants and clinical studies.
- To focus on radiopharmacy, dosimetry, and diagnostic/theranostic applications of FAP imaging.
Main Methods:
- Review of recent literature on FAP inhibitors and their clinical use.
- Analysis of radiolabeling strategies, dosimetry, and diagnostic performance.
- Evaluation of theranostic potential for refractory cancers.
Main Results:
- 68Ga-labeled FAP inhibitors are a promising new class of radiotracers.
- FAP imaging may offer improved specificity compared to 18FDG, especially in inflammatory conditions.
- FAP-targeted agents show potential for both diagnosis and therapy (theranostics).
Conclusions:
- FAP inhibitors represent a significant advancement in molecular imaging for oncology.
- FAP-targeted imaging has the potential to compete with and overcome limitations of 18FDG.
- Further research into FAP variants and theranostic applications is warranted.
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