Gallium-68 fibroblast activation protein inhibitor positron emission tomography in cardiovascular disease.

Front Nucl Med

Division of Cardiology, Department of Internal Medicine, Faculty of Health Sciences, University of the Witwatersrand, Johannesburg, South Africa.

Published: July 2023

Gallium-68 fibroblast activation protein inhibitor [(Ga)Ga-FAPI] is a new radiopharmaceutical positioning itself as the preferred agent in patients with malignant tumours, competing with 2-Deoxy-2-[18F]fluoro-d-glucose [2-(F)FDG] using positron emission tomography (PET). While imaging oncology patients with [Ga]Ga-FAPI PET, incidental uptake of [Ga]Ga-FAPI has been detected in the myocardium. This review summarises original research studies associating the visualisation of FAPI-based tracers in the myocardium with underlying active cardiovascular disease.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11440833PMC
http://dx.doi.org/10.3389/fnume.2023.1224905DOI Listing

Publication Analysis

Top Keywords

gallium-68 fibroblast
8
fibroblast activation
8
activation protein
8
protein inhibitor
8
positron emission
8
emission tomography
8
cardiovascular disease
8
inhibitor positron
4
tomography cardiovascular
4
disease gallium-68
4

Similar Publications

Conventional imaging techniques, while essential, occasionally fall short in identifying elusive metastatic lesions, leading to delayed diagnoses and compromised patient outcomes. Gallium-68 fibroblast activating protein inhibitor (Ga-FAPI) positron emission tomography/computed tomography (PET/CT), leveraging the distinct affinity of fibroblast activation protein for cancer-associated fibroblasts, emerges as a promising solution to bridge this diagnostic gap. Parotid gland adenocarcinoma is a relatively rare malignancy with metastasis typically occurring in regional lymph nodes and distant sites such as the lungs and bones.

View Article and Find Full Text PDF

Background: Myocardial fibrosis is a key healing response after myocardial infarction driven by activated fibroblasts. Gallium-68-labeled fibroblast activation protein inhibitor ([Ga]-FAPI) is a novel positron-emitting radiotracer that binds activated fibroblasts.

Objectives: The aim of this study was to investigate the intensity, distribution, and time-course of fibroblast activation after acute myocardial infarction.

View Article and Find Full Text PDF

Fibroblast activation protein inhibitors (FAPIs) labeled with gallium-68 and lutetium-177 show potential for use in the diagnosis and treatment of various cancers expressing FAP. However, Lu-labeled FAPIs often exhibit short tumor retention time, limiting their therapeutic applications. To improve tumor retention, we synthesized three radiolabeled dimeric FAPIs, [F], [Cu], and [Ga].

View Article and Find Full Text PDF

Fibroblast activation protein (FAP), which is overexpressed in cancer-associated fibroblasts (CAFs), represents a promising target for cancer diagnosis and therapy. Hypoxia is a common feature of solid tumors. A bivalent agent, DOTA-NI-FAPI-04 (), was developed by incorporating hypoxia-sensitive nitroimidazole (NI) into the FAP-targeting agent FAPI-04.

View Article and Find Full Text PDF

Development of ibuprofen-modified fibroblast activation protein radioligands to improve cancer therapy.

Eur J Med Chem

February 2025

GDMPA Key Laboratory for Quality Control and Evaluation of Radiopharmaceuticals, Department of Nuclear Medicine, Nanfang Hospital, Southern Medical University, Guangzhou, 510515, China; School of Pharmaceutical Sciences, Southern Medical University, Guangzhou, 510515, China. Electronic address:

Article Synopsis
  • The study focused on creating new FAP-targeting radioligands using an optimized amino acid linker and ibuprofen to enhance their effectiveness in cancer diagnosis and therapy.
  • Three novel quinoline-based FAP ligands, labeled with gallium-68 and lutetium-177, showed strong binding affinity and stability, along with improved tumor accumulation in imaging studies.
  • Among these ligands, [Lu]Lu-FAPI-Ibu3 demonstrated significantly better tumor-to-kidney dose ratios and longer survival in endoradiotherapy tests, positioning it as the most promising candidate for future clinical applications.
View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!