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Pharmaceuticals
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The Medical Applications of Novel PET Radiopharmaceuticals
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The Medical Applications of Novel PET Radiopharmaceuticals

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Radiopharmaceutical Sciences".

Deadline for manuscript submissions: 20 June 2025 | Viewed by 8314

Special Issue Editors

Dr. Jonathan Vigne

E-Mail Website
Guest Editor
1. Department of Nuclear Medicine, CHU de Caen Normandie, Normandie Université, UNICAEN, 14000 Caen, France
2. PhIND, Centre Cyceron, Institut Blood and Brain @ Caen-Normandie, INSERM U1237, 14000 Caen, France
Interests: nuclear medicine; radiopharmaceuticals; molecular imaging; radiopharmacy; theranostics
Dr. Florent L. Besson

E-Mail Website
Guest Editor
School of Medicine, Université Paris-Saclay, 94270 Le Kremlin-Bicêtre, France
Interests: nuclear medicine; PET imaging

Special Issue Information

Dear Colleagues,

This medical field is constantly seeking innovative solutions to improve diagnostic and treatment using tailored approaches. One such advancement lies in the utilization of novel positron emission tomography (PET) radiotracers. These cutting-edge radiotracers have shown immense potential in revolutionizing medical applications. With the rapid development of medical imaging technologies, PET has emerged as a powerful tool for visualizing and quantifying physiological processes within the human body. Traditional PET radiotracers have been widely used to diagnose and monitor various conditions, including cancer, cardiovascular diseases, and neurological disorders. However, the introduction of novel PET radiotracers has taken medical imaging to new heights.These innovative radiotracers are designed to target specific molecular and cellular processes, allowing for more accurate and precise imaging. By leveraging the unique properties of these radiotracers, medical professionals can gain valuable insight in the molecular mechanisms underlying these diseases. This knowledge facilitates early detection, personalized treatment planning, and therapeutic monitoring.The medical applications of novel PET radiotracers span across multiple disciplines. In oncology, these radiotracers enable the identification of specific tumor markers, aiding in tumor characterization, staging, and treatment response assessment. In cardiology, they can assess myocardial perfusion, monitor metabolism, and identify atherosclerotic plaques. Furthermore, in neurology, novel PET radiotracers facilitate the visualization of neuroreceptors, neurotransmitters, and amyloid plaques, assisting in the diagnosis and management of neurodegenerative disorders.This Special Issue aims to explore the significance and impact of novel PET radiotracers toward various medical applications. It is open to original research and review articles. We look forward to receiving your contributions.

Dr. Jonathan Vigne
Dr. Florent L. Besson
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • nuclear medicine
  • radiotracers
  • radiopharmaceuticals
  • positron emission tomography
  • diagnostics
  • medical applications

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Published Papers (5 papers)

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Research

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14 pages, 5739 KiB  
Article
[68Ga]FAPI PET for Imaging and Treatment Monitoring in a Preclinical Model of Pulmonary Fibrosis: Comparison to [18F]FDG PET and CT
by Hao Ji, Xiangming Song, Xiaoying Lv, Fuqiang Shao, Yu Long, Yangmeihui Song, Wenyu Song, Pengxin Qiao, Yongkang Gai, Dawei Jiang and Xiaoli Lan
Pharmaceuticals 2024, 17(6), 726; https://doi.org/10.3390/ph17060726 - 3 Jun 2024
Cited by 4 | Viewed by 1627
Abstract
Purpose: This study aimed to evaluate the feasibility of using [68Ga]-fibroblast-activating protein inhibitor (FAPI) positron emission tomography (PET) imaging for diagnosing pulmonary fibrosis in a mouse model. We also examined its value in monitoring treatment response and compared it with traditional [...] Read more.
Purpose: This study aimed to evaluate the feasibility of using [68Ga]-fibroblast-activating protein inhibitor (FAPI) positron emission tomography (PET) imaging for diagnosing pulmonary fibrosis in a mouse model. We also examined its value in monitoring treatment response and compared it with traditional [18F]-fluorodeoxyglucose (FDG) PET and computed tomography (CT) imaging. Methods: A model of idiopathic pulmonary fibrosis was established using intratracheal injection of bleomycin (BLM, 2 mg/kg) into C57BL/6 male mice. For the treatment of IPF, a daily oral dose of 400 mg/kg/day of pirfenidone was administered from 9 to 28 days after the establishment of the model. Disease progression and treatment efficacy were assessed at different stages of the disease every week for four weeks using CT, [18F]FDG PET, and [68Ga]FAPI PET (baseline imaging performed at week 0). Mice were sacrificed and lung tissues were harvested for hematoxylin-eosin staining, picrosirius red staining, and immunohistochemical staining for glucose transporter 1 (GLUT1) and FAP. Expression levels of GLUT1 and FAP in pathological sections were quantified. Correlations between imaging parameters and pathological quantitative values were analyzed. Results: CT, [18F]FDG PET and [68Ga]FAPI PET revealed anatomical and functional changes in the lung that reflected progression of pulmonary fibrosis. In untreated mice with pulmonary fibrosis, lung uptake of [18F]FDG peaked on day 14, while [68Ga]FAPI uptake and mean lung density peaked on day 21. In mice treated with pirfenidone, mean lung density and lung uptake of both PET tracers decreased. Mean lung density, [18F]FDG uptake, and [68Ga]FAPI uptake correlated well with quantitative values of picrosirius red staining, GLUT1 expression, and FAP expression, respectively. Conclusions: Although traditional CT and [18F]FDG PET reflect anatomical and metabolic status in fibrotic lung, [68Ga]FAPI PET provides a means of evaluating fibrosis progression and monitoring treatment response. Full article
(This article belongs to the Special Issue The Medical Applications of Novel PET Radiopharmaceuticals)
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Review

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28 pages, 2087 KiB  
Review
Fibroblast Activation Protein Inhibitor (FAPI)-Based Theranostics
by William Serumula, Venesen Pillay, Bawinile Hadebe and Mariza Vorster
Pharmaceuticals 2025, 18(4), 522; https://doi.org/10.3390/ph18040522 - 3 Apr 2025
Viewed by 109
Abstract
Fibroblast activation protein (FAP) is a serine protease selectively expressed in cancer-associated fibroblasts (CAFs), fibrotic tissues, and areas of active tissue remodeling, making it an attractive target for diagnostic imaging across a spectrum of disease. FAP inhibitors (FAPIs) labeled with PET tracers have [...] Read more.
Fibroblast activation protein (FAP) is a serine protease selectively expressed in cancer-associated fibroblasts (CAFs), fibrotic tissues, and areas of active tissue remodeling, making it an attractive target for diagnostic imaging across a spectrum of disease. FAP inhibitors (FAPIs) labeled with PET tracers have rapidly advanced as a novel imaging modality with broad clinical applications that offers several advantages, including rapid tumor accumulation, low background uptake, and high tumor-to-background ratios. In oncology, FAPI PET has demonstrated excellent performance in visualizing a wide range of malignancies, including those with low glycolytic activity, such as pancreatic cancer, cholangiocarcinoma, and certain sarcomas. Its high sensitivity and specificity for the stromal component enables improved tumor delineation, staging, and response assessment. Additionally, the potential to guide theranostic approaches, where the same tracer can be labeled with therapeutic radionuclides, positions FAPI as a key player in precision oncology. Beyond oncology, FAPI PET has shown promise in imaging conditions characterized by fibrotic and inflammatory processes. In the cardiovascular field, FAPI PET imaging is being investigated for its ability to detect myocardial fibrosis and active cardiac remodeling, crucial in conditions like heart failure, post-myocardial infarction remodeling, and hypertrophic cardiomyopathy. This review highlights the expanding clinical applications of FAPI-based PET imaging across oncology, inflammation, and cardiovascular disease. While the current data are promising, further large-scale studies and multicenter trials are essential to validate these findings and establish standardized protocols. The versatility and broad applicability of FAPI PET underscore its potential as a transformative tool in precision medicine. Full article
(This article belongs to the Special Issue The Medical Applications of Novel PET Radiopharmaceuticals)
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62 pages, 1217 KiB  
Review
Contribution of [18F]FET PET in the Management of Gliomas, from Diagnosis to Follow-Up: A Review
by Jade Apolline Robert, Arthur Leclerc, Mathilde Ducloie, Evelyne Emery, Denis Agostini and Jonathan Vigne
Pharmaceuticals 2024, 17(9), 1228; https://doi.org/10.3390/ph17091228 - 18 Sep 2024
Cited by 1 | Viewed by 1838
Abstract
Gliomas, the most common type of primary malignant brain tumors in adults, pose significant challenges in diagnosis and management due to their heterogeneity and potential aggressiveness. This review evaluates the utility of O-(2-[18F]fluoroethyl)-L-tyrosine ([18F]FET) positron emission tomography (PET), a [...] Read more.
Gliomas, the most common type of primary malignant brain tumors in adults, pose significant challenges in diagnosis and management due to their heterogeneity and potential aggressiveness. This review evaluates the utility of O-(2-[18F]fluoroethyl)-L-tyrosine ([18F]FET) positron emission tomography (PET), a promising imaging modality, to enhance the clinical management of gliomas. We reviewed 82 studies involving 4657 patients, focusing on the application of [18F]FET in several key areas: diagnosis, grading, identification of IDH status and presence of oligodendroglial component, guided resection or biopsy, detection of residual tumor, guided radiotherapy, detection of malignant transformation in low-grade glioma, differentiation of recurrence versus treatment-related changes and prognostic factors, and treatment response evaluation. Our findings confirm that [18F]FET helps delineate tumor tissue, improves diagnostic accuracy, and aids in therapeutic decision-making by providing crucial insights into tumor metabolism. This review underscores the need for standardized parameters and further multicentric studies to solidify the role of [18F]FET PET in routine clinical practice. By offering a comprehensive overview of current research and practical implications, this paper highlights the added value of [18F]FET PET in improving management of glioma patients from diagnosis to follow-up. Full article
(This article belongs to the Special Issue The Medical Applications of Novel PET Radiopharmaceuticals)
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17 pages, 741 KiB  
Review
The Role of Fibroblast Activation Protein Inhibitor Positron Emission Tomography in Inflammatory and Infectious Diseases: An Updated Systematic Review
by Domenico Albano, Alessio Rizzo, Riemer H. J. A. Slart, Søren Hess, Edel Noriega-Álvarez, Cristina Gamila Wakfie-Corieh, Lucia Leccisotti, Andor W. J. M. Glaudemans, Olivier Gheysens and Giorgio Treglia
Pharmaceuticals 2024, 17(6), 716; https://doi.org/10.3390/ph17060716 - 31 May 2024
Cited by 3 | Viewed by 1819
Abstract
The role of fibroblast activation protein inhibitor (FAPI) positron emission tomography/computed tomography (PET/CT) is emerging for the assessment of non-oncological diseases, such as inflammatory and infectious diseases, even if the evidence in the literature is still in its initial phases. We conducted a [...] Read more.
The role of fibroblast activation protein inhibitor (FAPI) positron emission tomography/computed tomography (PET/CT) is emerging for the assessment of non-oncological diseases, such as inflammatory and infectious diseases, even if the evidence in the literature is still in its initial phases. We conducted a systematic search of Scopus, PubMed/MEDLINE, Embase, and Cochrane library databases for studies published before 31 December 2023 reporting infectious and inflammatory disease imaging with FAPI PET/CT. We included twenty-one studies for a total of 1046 patients. The most frequent disease studied was lung interstitial disease, investigated in six studies for a total of 200 patients, followed by bone and joint diseases in two studies and 185 patients, IgG4-related disease in 53 patients, and Crohn’s disease in 30 patients. Despite the heterogeneity of studies in terms of study design and technical features, FAPI PET/CT showed a high detection rate and diagnostic role. Moreover, when compared with 2-[18F]FDG PET/CT (n = 7 studies), FAPI PET/CT seems to have better diagnostic performances. The presence of chronic inflammation and tissue remodeling, typical of immune-mediated inflammatory conditions, may be the underlying mechanism of FAPI uptake. Full article
(This article belongs to the Special Issue The Medical Applications of Novel PET Radiopharmaceuticals)
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20 pages, 3480 KiB  
Review
Diagnostic Accuracy of [68Ga]Ga Labeled Fibroblast-Activation Protein Inhibitors in Detecting Head and Neck Cancer Lesions Using Positron Emission Tomography: A Systematic Review and a Meta-Analysis
by Alessio Rizzo, Alberto Miceli, Manuela Racca, Matteo Bauckneht, Silvia Morbelli, Domenico Albano, Francesco Dondi, Francesco Bertagna, Danilo Galizia, Barbara Muoio, Salvatore Annunziata and Giorgio Treglia
Pharmaceuticals 2023, 16(12), 1664; https://doi.org/10.3390/ph16121664 - 30 Nov 2023
Cited by 7 | Viewed by 2063
Abstract
Several studies have examined the use of positron emission tomography (PET) using [68Ga]Ga-radiolabeled fibroblast-activation protein inhibitors (FAPi) across multiple subtypes of head and neck cancer (HNC). The purpose of the present study was to evaluate the diagnostic accuracy of a newly [...] Read more.
Several studies have examined the use of positron emission tomography (PET) using [68Ga]Ga-radiolabeled fibroblast-activation protein inhibitors (FAPi) across multiple subtypes of head and neck cancer (HNC). The purpose of the present study was to evaluate the diagnostic accuracy of a newly developed molecular imaging approach in the context of HNC through a comprehensive review and meta-analysis. A thorough literature review was conducted to identify scholarly articles about the diagnostic effectiveness of FAP-targeted PET imaging. The present study incorporates original publications assessing the efficacy of this innovative molecular imaging test in both newly diagnosed and previously treated HNC patients. This systematic review examined eleven investigations, of which nine were deemed suitable for inclusion in the subsequent meta-analysis. The quantitative synthesis yielded a pooled detection rate of 99% for primary HNC lesions. Additionally, on a per patient-based analysis, the pooled sensitivity and specificity for regional lymph node metastases were found to be 90% and 84%, respectively. The analysis revealed a statistical heterogeneity among the studies for the detection rate of primary HNC lesions. The quantitative findings presented in this study indicate a favorable diagnostic performance of FAP-targeted PET imaging in detecting primary HNC tumors. In contrast, discordant results concerning the diagnostic accuracy of lymph node metastases were found. However, further multicentric trials are required to validate the efficacy of FAP-targeted PET in this specific group of patients. Full article
(This article belongs to the Special Issue The Medical Applications of Novel PET Radiopharmaceuticals)
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