[68Ga]Ga-FAP-2286, a novel promising theragnostic approach for PET/CT imaging in patients with various type of metastatic cancers

Background Fibroblast activation protein (FAP) has emerged as a promising target for diagnosis and therapeutic intervention due to high expression and accumulation in the stromal compartments of a variety of malignant tumors. FAP-2286 utilizes cyclic peptides with FAP-binding characteristics to enha...

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Published in:European journal of nuclear medicine and molecular imaging 2024-06, Vol.51 (7), p.1981-1988
Main Authors: Banihashemian, Seyedeh Somayyeh, Divband, Ghasemali, Pirayesh, Elahe, Nikkholgh, Babak, Amini, Hamidreza, Shahrnoy, Abdolghafar Abolhosseini, Nami, Reza, Akbari, Mohammad Esmaeil
Format: Article
Language:English
Subjects:
Adenocarcinoma
Adult
Aged
Blood pressure
Cancer
Cardiology
Computed tomography
Diagnosis
Endopeptidases
Female
Fibroblast activation protein
Gallium
Gallium Radioisotopes
Heart rate
Humans
Imaging
Lesions
Male
Medical imaging
Medicine
Medicine & Public Health
Membrane Proteins
Mesothelium
Metastases
Metastasis
Middle Aged
Neoplasm Metastasis
Neoplasms - diagnostic imaging
Nuclear Medicine
Oncology
Original Article
Orthopedics
Peptides
Peptides, Cyclic - chemistry
Peptides, Cyclic - pharmacokinetics
Pharmacology
Positron emission
Positron Emission Tomography Computed Tomography - methods
Radiology
Radiopharmaceuticals - pharmacokinetics
Sarcoma
Solid tumors
Tumors
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Summary:Background Fibroblast activation protein (FAP) has emerged as a promising target for diagnosis and therapeutic intervention due to high expression and accumulation in the stromal compartments of a variety of malignant tumors. FAP-2286 utilizes cyclic peptides with FAP-binding characteristics to enhance the retention of the imaging agent within tumors, in contrast to the small-molecule FAP inhibitors (FAPI) like FAPI-04/46. The aim of this study was to quantify the tumor uptake of [ 68 Ga] Gallium-FAP-2286 within primary solid tumors, adjacent excised tissues, and metastatic lesions. Methods In this prospective study, 21 patients (average age 51.9) with various diagnoses of remaining and metastatic cancers participated. Among them, six had metastatic sarcoma, and 14 had adenocarcinoma, including eight breast, two rectum, two lung, two pancreas, and one thyroid cases. The patients underwent a [ 68 Ga]Ga-FAP-2286 PET/CT scan. An hour post-administration of [ 68 Ga]Ga-FAP-2286, a visual assessment of whole body scans and semi-quantification of the PET/CT results were carried out. The standardized uptake values (SUV) max of [ 68 Ga]Ga-FAP-2286 in tumor lesions and the tumor-to-background ratio (TBR) were then calculated. Results The vital signs of the patients, such as heart rate, blood pressure, and temperature, were observed before, during, and after the diagnostic procedure during the 4-h follow-up. All individuals underwent the [ 68 Ga]Ga-FAP-2286 PET/CT scans without any signs of drug-associated pharmacological effects. The PET/CT scans displayed substantial absorption of [ 68 Ga]Ga-FAP-2286 in tumor lesions in all patients (100% (21/21)). Irrespective of the tumors’ origins (epithelial or mesothelium) and whether they exhibited local recurrence, distant recurrence, or metastatic lesions, the PET/CT scans revealed the uptake of [ 68 Ga]Ga-FAP-2286 in these lesions. Conclusion Overall, these data suggest that [ 68 Ga]Ga-FAP-2286 is a promising FAP derivative for efficient metastatic cancer diagnosis and being considered as a potential compound for therapeutic application in patients with advanced metastatic cancers.
ISSN:1619-7070
1619-7089
DOI:10.1007/s00259-024-06635-8