Related Experiment Video
Updated: Oct 5, 2025
![Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F68356.jpg&w=3840&q=50)
Automated Preparation of [68Ga]Ga-3BP-3940 on a Synthesis Module for PET Imaging of the Tumor Microenvironment
Published on: April 25, 2025
Clinical summary of fibroblast activation protein inhibitor-based radiopharmaceuticals: cancer and beyond
Mengting Li1,2, Muhsin H Younis3, Yongxue Zhang1,2
1Department of Nuclear Medicine, Union Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan, China.
Abstract:
Fibroblast activation protein (FAP) is a type II membrane-bound glycoprotein which is overexpressed in cancer-associated fibroblasts and activated fibroblasts at wound healing/inflammatory sites. Since the first clinical application of quinoline-based FAP ligands in 2018, FAP inhibitor (FAPI)-based PET imaging and radiotherapy have been investigated for a wide variety of diseases, both cancerous and non-cancerous. As a consequence, promising strides have been made in particular to improve the understanding of FAPI-based PET imaging and the potential value of FAPI-based tumor radiotherapy. Herein, we present a comprehensive review of radiolabeled FAPI, including their clinical translation, in order to clarify the current and potential future role of this class of molecules in nuclear medicine. In particular, this review underlines the value of FAPI radiopharmaceuticals in the diagnosis or therapy of tumors or benign conditions. However, limitations in present studies have hampered a precise evaluation of FAPI radiopharmaceuticals. Despite this, it will likely be worthwhile to further explore the clinical value of FAPI in diagnosis and therapy through better-designed and larger-population clinical trials in the future.
Insights
Fibroblast Activation Protein (FAP) inhibitors (FAPI) show promise for PET imaging and radiotherapy in various diseases. Further clinical trials are needed to fully evaluate FAPI radiopharmaceuticals for diagnosis and therapy.
Area of Science:
- Nuclear Medicine
- Oncology
- Radiochemistry
Background:
- Fibroblast Activation Protein (FAP) is a glycoprotein overexpressed in cancer-associated fibroblasts and activated fibroblasts.
- FAP inhibitor (FAPI)-based agents have emerged for PET imaging and radiotherapy since 2018.
- FAPI applications span both cancerous and non-cancerous conditions, including wound healing and inflammatory sites.
Purpose of the Study:
- To provide a comprehensive review of radiolabeled FAPI, focusing on their clinical translation.
- To clarify the current and potential future roles of FAPI radiopharmaceuticals in nuclear medicine.
- To highlight the diagnostic and therapeutic potential of FAPI in both oncological and benign diseases.
Main Methods:
- Review of existing literature on radiolabeled FAPI.
- Analysis of clinical translation and applications of FAPI-based agents.
- Synthesis of findings regarding FAPI's role in diagnosis and therapy.
Main Results:
- FAPI-based PET imaging and radiotherapy have shown promising results across diverse diseases.
- Significant progress has been made in understanding FAPI's utility in tumor imaging and radiotherapy.
- The review underscores the value of FAPI radiopharmaceuticals for diagnosing and treating various conditions.
Conclusions:
- FAPI radiopharmaceuticals hold considerable potential for the diagnosis and therapy of tumors and benign conditions.
- Limitations in current studies necessitate further investigation to precisely evaluate FAPI radiopharmaceuticals.
- Future well-designed, large-population clinical trials are essential to fully explore the clinical value of FAPI.
![An Automated Radiosynthesis of [68Ga]Ga-FAPI-46 for Routine Clinical Use](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F66708.jpg&w=3840&q=50)
