Fibroblast activation protein (FAP), expressed in the tumor microenvironment of a variety of cancers, has become a target of novel PET tracers. The purpose of this report is to evaluate the imaging characteristics of Ga-FAP-2286, present the first-to our knowledge-dosimetry analysis to date, and compare the agent with F-FDG and FAPI compounds. Patients were administered 219 ± 43 MBq of Ga-FAP-2286 and scanned after 60 min. Uptake was measured in up to 5 lesions per patient and within the kidneys, spleen, liver, and mediastinum (blood pool). Absorbed doses were evaluated using MIM Encore and OLINDA/EXM version 1.1 using the International Commission on Radiological Protection publication 103 tissue weighting factor. Forty-six patients were imaged with Ga-FAP-2286 PET. The highest average uptake was seen in sarcoma, cholangiocarcinoma, and colon cancer. The lowest uptake was found in lung cancer and testicular cancer. The average SUV was significantly higher on Ga-FAP-2286 PET than on F-FDG PET in cholangiocarcinoma (18.2 ± 6.4 vs. 9.1 ± 5.0, = 0.007), breast cancer (11.1 ± 6.8 vs. 4.1 ± 2.2, < 0.001), colon cancer (13.8 ± 2.2 vs. 7.6 ± 1.7, = 0.001), hepatocellular carcinoma (9.3 ± 3.5 vs. 4.7 ± 1.3, = 0.01), head and neck cancer (11.3 ± 3.5 vs. 7.6 ± 5.5, = 0.04), and pancreatic adenocarcinoma (7.4 ± 1.8 vs. 3.7 ± 1.0, = 0.01). The total-body effective dose was estimated at 1.16E-02 mSv/MBq, with the greatest absorbed organ dose in the urinary bladder wall (9.98E-02 mGy/MBq). Ga-FAP-2286 biodistribution, dosimetry, and tumor uptake were similar to those of previously reported FAPI compounds. Additionally,Ga-FAP-2286 PET had consistently higher uptake than F-FDG PET. These results are especially promising in the setting of small-volume disease and differentiating tumor from inflammatory uptake.
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http://dx.doi.org/10.2967/jnumed.123.267281 | DOI Listing |
Clin Nucl Med
February 2025
From the Cancer Research Center, Shahid Beheshti University of Medical Sciences, Tehran, Iran.
Fibroblast activation protein (FAP) has emerged as a promising molecular target for diagnostic and therapeutic strategies. Previous research, including our own study and other published reports, has highlighted the potential of FAP inhibitors labeled with 68 Ga as effective diagnostic radiopharmaceuticals. In this study, we present a comparative analysis of early and late PET/CT scans, using 68 Ga-FAP-2286, for the detection of tumor lesions in a patient with metastatic breast adenocarcinoma.
View Article and Find Full Text PDFEJNMMI Res
October 2024
Department of Nuclear Medicine, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou, 510120, China.
Background: Fibroblast activation protein (FAP) has gained attention as a promising molecular target with potential utility for cancer diagnosis and therapy. [Ga]Ga-labeled FAP-targeting peptides have been successfully applied to positron emission tomography (PET) imaging of various tumor types. To meet the applicable demand for peptide-based FAP tracers with high patient throughput, we herein report the radiosynthesis, preclinical evaluation, and the first-in-human imaging of a novel [F]F-labeled FAP-targeting peptide.
View Article and Find Full Text PDFPharmaceuticals (Basel)
August 2024
Department of Nuclear Medicine and Endocrinology, University Hospital Salzburg, Paracelsus Medical University, 5020 Salzburg, Austria.
[Ga]Ga-FAP-2286 is a new peptide-based radiopharmaceutical for positron-emission tomography (PET) that targets fibroblast activation protein (FAP). This article describes in detail the automated synthesis of [Ga]Ga-FAP-2286 using a commercially available synthesis tool that includes quality control for routine clinical applications. The synthesis was performed using a Scintomics GRP-3V module and a GMP grade Ge/Ga generator.
View Article and Find Full Text PDFFront Oncol
July 2024
Department of Nuclear Medicine, the Affiliated Hospital, Southwest Medical University, Luzhou, China.
Purpose: The Ga/Lu-FAP-2286 is a newly developed tumor imaging agent that shows potential for visualizing and treating tumor stroma. The objective of this research was to evaluate the effectiveness of Ga-FAP-2286 PET/CT and F-FDG PET/CT in diagnosing advanced lung cancer.
Methods: In this prospective study, patients with lung cancer who underwent Ga-FAP-2286 and F-FDG PET/CT examinations between September 2022 and June 2023 were analyzed.
Eur J Nucl Med Mol Imaging
October 2024
Department of Nuclear Medicine, The First Affiliated Hospital of Guangzhou Medical University, Guangzhou, 510120, China.
Background: The aim of the present study was to develop a novel Cu-labeled cyclic peptide ([Cu]Cu-FAP-NOX) that targets fibroblast activation protein (FAP) and may offer advantages in terms of image contrast, imaging time window, and low uptake in normal tissues.
Methods: The novel cyclic peptide featuring with a N-oxalyl modified tail was constructed and conjugated to NOTA for Cu labeling. Biochemical and cellular assays were performed with A549.
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