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Molecular Imaging in Neurology and Oncology: Radiopharmaceuticals for PET and...
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Molecular Imaging in Neurology and Oncology: Radiopharmaceuticals for PET and SPECT

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

Deadline for manuscript submissions: closed (30 November 2021) | Viewed by 15449

Special Issue Editor

Dr. Guillaume Becker

E-Mail Website
Guest Editor
1 CarMeN Laboratory, INSERM, INRA, INSA Lyon, University Claude Bernard Lyon 1, Lyon, France
2 GIGA-Cyclotron Research Center-in vivo imaging, University of Liège, Allée du 6 Août, B30, 4000 Liege, Belgium
Interests: positrons emission tomography; radiotracers; neurodegeneratives diseases; neurosciences; neuro-immunology; oncology

Special Issue Information

Dear Colleagues,

Molecular imaging methods that use radionuclide-labelled compounds to assess in vivo biological functions are constantly evolving thanks to innovations in related sciences such as chemistry and radiochemistry, biochemistry, and bioengineering. Therefore, non-invasive nuclear medicine techniques, namely, positron emission tomography (PET) and single-photon emission computed tomography (SPECT), can image a broad spectrum of pathophysiological processes by means of the large diversity of available radiotracers ranging  from radionuclide ions to small inorganic and organic molecules, and further to biomolecules and particles.  The journal Pharmaceuticals invites both reviews and original articles shedding light upon the latest developments in radiopharmaceutical sciences applied to neurology and oncology, two medical specialties that are particularly benefiting from nuclear medicine technologies.

Dr. Guillaume Becker
Guest Editor

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

  • Positron emission tomography
  • Single-photon emission computed tomography
  • Radiopharmaceuticals
  • Radiochemistry
  • Radiopharmacy
  • Neurology
  • Oncology

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Published Papers (5 papers)

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Research

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12 pages, 1625 KiB  
Article
Influence of Semiquantitative [18F]FDG PET and Hematological Parameters on Survival in HNSCC Patients Using Neural Network Analysis
by Paulina Cegla, Geoffrey Currie, Joanna P. Wróblewska, Witold Cholewiński, Joanna Kaźmierska, Andrzej Marszałek, Anna Kubiak, Pawel Golusinski, Wojciech Golusiński and Ewa Majchrzak
Pharmaceuticals 2022, 15(2), 224; https://doi.org/10.3390/ph15020224 - 14 Feb 2022
Cited by 5 | Viewed by 1961
Abstract
The aim of this study is to assess the influence of semiquantitative PET-derived parameters as well as hematological parameters in overall survival in HNSCC patients using neural network analysis. Retrospective analysis was performed on 106 previously untreated HNSCC patients. Several PET-derived parameters (SUV [...] Read more.
The aim of this study is to assess the influence of semiquantitative PET-derived parameters as well as hematological parameters in overall survival in HNSCC patients using neural network analysis. Retrospective analysis was performed on 106 previously untreated HNSCC patients. Several PET-derived parameters (SUVmax, SUVmean, TotalSUV, MTV, TLG, TLRmax, TLRmean, TLRTLG, and HI) for primary tumor and lymph node with highest activity were assessed. Additionally, hematological parameters (LEU, LEU%, NEU, NEU%, MON, MON%, PLT, PLT%, NRL, and LMR) were also assessed. Patients were divided according to the diagnosis into the good and bad group. The data were evaluated using an artificial neural network (Neural Analyzer version 2.9.5) and conventional statistic. Statistically significant differences in PET-derived parameters in 5-year survival rate between group of patients with worse prognosis and good prognosis were shown in primary tumor SUVmax (10.0 vs. 7.7; p = 0.040), SUVmean (5.4 vs. 4.4; p = 0.047), MTV (23.2 vs. 14.5; p = 0.010), and TLG (155.0 vs. 87.5; p = 0.05), and mean liver TLG (27.8 vs. 30.4; p = 0.031), TLRmax (3.8 vs. 2.6; p = 0.019), TLRmean (2.8 vs. 1.9; p = 0.018), and in TLRTLG (5.6 vs. 2.3; p = 0.042). From hematological parameters, only LMR showed significant differences (2.5 vs. 3.2; p = 0.009). Final neural network showed that for ages above 60, primary tumors SUVmax, TotalSUV, MTV, TLG, TLRmax, and TLRmean over (9.7, 2255, 20.6, 145, 3.6, 2.6, respectively) are associated with worse survival. Our study shows that the neural network could serve as a supplement to PET-derived parameters and is helpful in finding prognostic parameters for overall survival in HNSCC. Full article
(This article belongs to the Special Issue Molecular Imaging in Neurology and Oncology: Radiopharmaceuticals for PET and SPECT)
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13 pages, 2182 KiB  
Article
Differences in Distribution and Detection Rate of the [68Ga]Ga-PSMA Ligands PSMA-617, -I&T and -11—Inter-Individual Comparison in Patients with Biochemical Relapse of Prostate Cancer
by Falk Gühne, Stefanie Radke, Thomas Winkens, Christian Kühnel, Julia Greiser, Philipp Seifert, Robert Drescher and Martin Freesmeyer
Pharmaceuticals 2022, 15(1), 9; https://doi.org/10.3390/ph15010009 - 22 Dec 2021
Cited by 8 | Viewed by 3072
Abstract
The biochemical relapse of prostate cancer is diagnostically challenging but of high clinical impact for subsequent patient treatment. PET/CT with radiolabeled PSMA ligands outperforms conventional diagnostic methods in the detection of tumor recurrence. Several radiopharmaceuticals were and are available for use. The aim [...] Read more.
The biochemical relapse of prostate cancer is diagnostically challenging but of high clinical impact for subsequent patient treatment. PET/CT with radiolabeled PSMA ligands outperforms conventional diagnostic methods in the detection of tumor recurrence. Several radiopharmaceuticals were and are available for use. The aim of this study was to investigate whether the routinely applied [68Ga]Ga-PSMA ligands PSMA-617, -I&T and -11 (HBED-CC) differ in physiological and pathological distribution, or in tumor detection rate. A retrospective evaluation of 190 patients (39 patients received PSMA-617, 68 patients PSMA-I&T and 83 patients PSMA-11) showed significant differences in tracer accumulation within all organs examined. The low retention within the compartments blood pool, bone and muscle tissue is a theoretical advantage of PSMA-11. Evaluation of tumor lesion uptake and detection rate did not reveal superiority of one of the three radiopharmaceuticals, neither in the whole population, nor in particularly challenging subgroups like patients with very low PSA levels. We conclude that all three [68Ga]Ga-PSMA ligands are equally feasible in this clinically important scenario, and may replace each other in case of unavailability or production restrictions. Full article
(This article belongs to the Special Issue Molecular Imaging in Neurology and Oncology: Radiopharmaceuticals for PET and SPECT)
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13 pages, 1640 KiB  
Article
[18F]F-PSMA-1007 Radiolabelling without an On-Site Cyclotron: A Quality Issue
by Valentina Di Iorio, Stefano Boschi, Anna Sarnelli, Cristina Cuni, David Bianchini, Manuela Monti, Giancarlo Gorgoni, Giovanni Paganelli, Federica Matteucci and Carla Masini
Pharmaceuticals 2021, 14(7), 599; https://doi.org/10.3390/ph14070599 - 22 Jun 2021
Cited by 4 | Viewed by 4457
Abstract
Radiopharmaceuticals targeting the prostate-specific membrane antigen (PSMA) has become the gold standard for PET imaging of prostate cancer. [68Ga]Ga-PSMA-11 has been the forerunner but a [18F]F-PSMA ligand has been developed because of the intrinsic advantages of Fluorine-18. Fluorine-18 labelled [...] Read more.
Radiopharmaceuticals targeting the prostate-specific membrane antigen (PSMA) has become the gold standard for PET imaging of prostate cancer. [68Ga]Ga-PSMA-11 has been the forerunner but a [18F]F-PSMA ligand has been developed because of the intrinsic advantages of Fluorine-18. Fluorine-18 labelled compounds are usually prepared in centers with an on-site cyclotron. Since our center has not an on-site cyclotron, we decided to verify the feasibility of producing the experimental 18F-labelled radiopharmaceutical [18F]F-PSMA-1007 with [18F]F- from different external suppliers. A quality agreement has been signed with two different suppliers, and a well-established and correctly implemented quality assurance protocol has been followed. The [18F]F- was produced with cyclotrons, on Nb target, but with different beam energy and current. Extensive validation of the [18F]F-PSMA-1007 synthesis process has been performed. The aim of this paper was the description of all the quality documentation which allowed the submission and approval of the Investigational Medicinal Product Dossier (IMPD) to the Competent Authority, addressing the quality problems due to different external suppliers. The result indicates that no significant differences have been found between the [18F]F- from the two suppliers in terms of radionuclidic and radiochemical purity and [18F]F- impacted neither the radiochemical yield of the labelling reaction nor the quality control parameters of the IMP [18F]F-PSMA-1007. These results prove how a correct quality assurance system can overcome some Regulatory Authorities issue that may represent an obstacle to the clinical use of F-18-labelled radiopharmaceuticals without an on-site cyclotron. Full article
(This article belongs to the Special Issue Molecular Imaging in Neurology and Oncology: Radiopharmaceuticals for PET and SPECT)
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19 pages, 4522 KiB  
Article
Species Differences in Microsomal Metabolism of Xanthine-Derived A1 Adenosine Receptor Ligands
by Daniela Schneider, Dirk Bier, Marcus Holschbach, Andreas Bauer and Bernd Neumaier
Pharmaceuticals 2021, 14(3), 277; https://doi.org/10.3390/ph14030277 - 18 Mar 2021
Cited by 3 | Viewed by 2170
Abstract
Tracer development for positron emission tomography (PET) requires thorough evaluation of pharmacokinetics, metabolism, and dosimetry of candidate radioligands in preclinical animal studies. Since variations in pharmacokinetics and metabolism of a compound occur in different species, careful selection of a suitable model species is [...] Read more.
Tracer development for positron emission tomography (PET) requires thorough evaluation of pharmacokinetics, metabolism, and dosimetry of candidate radioligands in preclinical animal studies. Since variations in pharmacokinetics and metabolism of a compound occur in different species, careful selection of a suitable model species is mandatory to obtain valid data. This study focuses on species differences in the in vitro metabolism of three xanthine-derived ligands for the A1 adenosine receptor (A1AR), which, in their 18F-labeled form, can be used to image A1AR via PET. In vitro intrinsic clearance and metabolite profiles of 8-cyclopentyl-3-(3-fluoropropyl)-1-propylxanthine (CPFPX), an established A1AR-ligand, and two novel analogs, 8-cyclobutyl-3-(3-fluoropropyl)-1-propylxanthine (CBX) and 3-(3-fluoropropyl)-8-(1-methylcyclobutyl)-1-propylxanthine (MCBX), were determined in liver microsomes from humans and preclinical animal species. Molecular mechanisms leading to significant differences between human and animal metabolite profiles were also examined. The results revealed significant species differences regarding qualitative and quantitative aspects of microsomal metabolism. None of the tested animal species fully matched human microsomal metabolism of the three A1AR ligands. In conclusion, preclinical evaluation of xanthine-derived A1AR ligands should employ at least two animal species, preferably rodent and dog, to predict in vivo behavior in humans. Surprisingly, rhesus macaques appear unsuitable due to large differences in metabolic activity towards the test compounds. Full article
(This article belongs to the Special Issue Molecular Imaging in Neurology and Oncology: Radiopharmaceuticals for PET and SPECT)
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Review

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11 pages, 2829 KiB  
Review
Primary and Metastatic Brain Tumours Assessed with the Brain and Torso [18F]FDG PET/CT Study Protocol—10 Years of Single-Institutional Experiences
by Agata Pietrzak, Andrzej Marszałek, Tomasz Piotrowski, Adrianna Medak, Katarzyna Pietrasz, Julia Wojtowicz, Hubert Szweda, Krzysztof Matuszewski and Witold Cholewiński
Pharmaceuticals 2021, 14(8), 722; https://doi.org/10.3390/ph14080722 - 26 Jul 2021
Cited by 1 | Viewed by 2842
Abstract
According to the international societies’ recommendations, the 2-deoxy-2-[18F]fluoro-D-glucose positron emission tomography/computed tomography ([18F]FDG PET/CT) technique should not be used as the method of choice in brain tumour diagnosis. Therefore, the brain region can be omitted during standard [18 [...] Read more.
According to the international societies’ recommendations, the 2-deoxy-2-[18F]fluoro-D-glucose positron emission tomography/computed tomography ([18F]FDG PET/CT) technique should not be used as the method of choice in brain tumour diagnosis. Therefore, the brain region can be omitted during standard [18F]FDG PET/CT scanning. We performed comprehensive literature research and analysed results from 14,222 brain and torso [18F]FDG PET/CT studies collected in 2010–2020. We found 131 clinically silent primary and metastatic brain tumours and 24 benign lesions. We concluded that the brain and torso [18F]FDG PET/CT study provides valuable data that may support therapeutic management by detecting clinically silent primary and metastatic brain tumours. Full article
(This article belongs to the Special Issue Molecular Imaging in Neurology and Oncology: Radiopharmaceuticals for PET and SPECT)
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