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Updated: Jan 8, 2026
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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
Recent clinical advances in fibroblast activation protein targeted radioligand therapy for solid tumors
Xiaolong Wu1, Yu Wang2, Yingchun Li2
1Thoracic Oncology Ward, Cancer Center, and State Key Laboratory of Biotherapy, West China Hospital, Sichuan University, Chengdu, China.
Abstract:
Fibroblast activation protein (FAP) is a type II transmembrane serine protease predominantly expressed by cancer-associated fibroblasts (CAFs) in more than 90% of epithelial malignancies. The advent of FAP inhibitor (FAPI)-based positron emission tomography (PET) imaging has established FAP as a promising pan-tumor target for radioligand therapy (RLT). This review summarizes the current clinical landscape of FAP-targeted RLT in solid tumors, while also discussing existing challenges and future directions in this rapidly evolving field.
Insights
Fibroblast activation protein (FAP) is a key target in cancer. FAP inhibitor (FAPI)-based radioligand therapy shows promise for treating solid tumors, with ongoing research addressing challenges and future directions.
Area of Science:
- Oncology
- Radiochemistry
- Molecular Imaging
Background:
- Fibroblast activation protein (FAP) is highly expressed in cancer-associated fibroblasts (CAFs) within most epithelial cancers.
- FAP plays a significant role in tumor microenvironment modulation and progression.
Purpose of the Study:
- To review the current clinical applications of FAP-targeted radioligand therapy (RLT) in solid tumors.
- To discuss the challenges and future prospects of FAP-targeted RLT.
Main Methods:
- Review of current clinical data on FAP inhibitor (FAPI)-based positron emission tomography (PET) imaging and RLT.
- Analysis of FAP expression patterns in various malignancies.
Main Results:
- FAPI-based PET imaging has confirmed FAP as a viable pan-tumor target.
- FAP-targeted RLT is emerging as a promising therapeutic strategy for solid tumors.
Conclusions:
- FAP-targeted RLT represents a rapidly advancing field with significant therapeutic potential.
- Addressing current challenges is crucial for optimizing FAP-targeted RLT efficacy and clinical translation.
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