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Updated: Oct 7, 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
Dimeric FAPI with potential for tumor theranostics
Chunxia Qin1,2, Yangmeihui Song1,2, Weibo Cai3
1Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology Wuhan 430022, Hubei, China.
Abstract:
Radionuclide-labeled fibroblast activation protein inhibitors (FAPIs) are popular nuclear imaging probes in recent years. It's of great significance for tumor diagnosis and has great potential in tumor treatment. However, optimization of the probes is needed to further increase tumor uptake and prolong tumor retention for improved treatment efficacy and fewer side effects. In this issue of AJNMMI, Moon et al. reported two squaramide coupled FAPI conjugates (DOTA.(SA.FAPi)2 and DOTAGA.(SA.FAPi)2) and labeled them with 68Ga. The resulted tracers showed increased tumor accumulation and persistent retention, which led to an advance in PET imaging. The use of dimeric structures provides a feasible strategy to develop radiotherapeutic analogs of FAP inhibitors.
Insights
New fibroblast activation protein inhibitors (FAPI) probes show enhanced tumor uptake and retention for improved nuclear imaging and potential cancer treatment. Dimeric structures offer a promising strategy for developing targeted radiotherapies.
Area of Science:
- Nuclear medicine
- Radiochemistry
- Oncology
Background:
- Fibroblast activation protein inhibitors (FAPI) are crucial for tumor diagnosis and treatment.
- Current FAPI probes require optimization for increased tumor uptake and retention.
- Dimeric FAPI conjugates offer a potential strategy to enhance imaging and therapeutic efficacy.
Discussion:
- Moon et al. developed two novel squaramide-coupled FAPI conjugates (DOTA.(SA.FAPi)2 and DOTAGA.(SA.FAPi)2).
- These conjugates were labeled with Gallium-68 (68Ga) for positron emission tomography (PET) imaging.
- The dimeric tracers demonstrated superior tumor accumulation and prolonged retention compared to existing probes.
Key Insights:
- Dimeric FAPI structures significantly improve tumor targeting and retention in preclinical models.
- The enhanced accumulation and retention of 68Ga-labeled dimeric FAPI tracers advance PET imaging capabilities for cancer.
- This strategy holds promise for developing more effective FAPI-based radiotherapeutics.
Outlook:
- Further research into dimeric FAPI conjugates could lead to improved cancer diagnostics and therapeutics.
- The development of radiotherapeutic analogs based on FAPI inhibitors is a key future direction.
- Optimized FAPI probes may reduce side effects and increase treatment efficacy in oncology.
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