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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
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Structure-guided design and clinical evaluation of 68Ga-GP01 for FAP-targeted PET imaging in solid tumors
Xingyu Mu1, Zihao Chen2, Hoi Yee Chow3
1Department of Nuclear Medicine, The First Affiliated Hospital, Guilin Medical University, Guilin 541001, China.
Summary
A novel radiotracer, 68Ga-GP01, demonstrates superior stability and tumor detection compared to 68Ga-FAPI-46 for fibroblast activation protein (FAP)-expressing cancers. Clinical trials show promising results for FAP-targeted PET imaging.
Area of Science:
- Nuclear Medicine
- Oncology
- Radiochemistry
Background:
- Fibroblast activation protein (FAP)-targeted radioligands are effective for detecting FAP-expressing cancers.
- The quinoline-based agent 68Ga-FAPI-46 has limitations in vivo stability and pharmacokinetics.
Purpose of the Study:
- To design and evaluate a novel FAP-targeted radioligand, 68Ga-GP01, with improved properties over 68Ga-FAPI-46.
- To assess the diagnostic performance of 68Ga-GP01 in preclinical tumor models and clinical trials for solid tumors.
Main Methods:
- GP01 was synthesized by modifying FAPI-46 with an N-methyl-benzenesulfonic acid side chain.
- In vitro assays, in vivo PET/CT imaging in tumor models, and clinical evaluation in 35 patients were performed.
- Direct comparison with 18F-FDG was conducted.
Main Results:
- 68Ga-GP01 exhibited high radiochemical purity, excellent in vitro stability, and specific binding to FAP.
- Preclinical studies showed enhanced uptake, internalization, and slower efflux compared to 68Ga-FAPI-46, with improved tumor-to-background ratios.
- Clinical evaluation demonstrated optimal pharmacokinetics, persistent target engagement, promising lesion detection, and a low effective dose.
- 68Ga-GP01 detected more lesions than 18F-FDG with higher uptake and tumor-to-background ratios.
Conclusions:
- 68Ga-GP01 is a clinically translatable FAP-targeted PET tracer with superior performance to 68Ga-FAPI-46.
- Its ability to augment or surpass metabolic imaging warrants further investigation in stromal imaging applications.
- 68Ga-GP01 shows potential as a valuable tool in oncology for FAP-positive solid tumors.
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