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New Advances in Radiopharmaceutical Sciences

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 31 January 2025 | Viewed by 5902

Special Issue Editor

Dr. Elisabeth Eppard

E-Mail Website
Guest Editor
Department of Nuclear Medicine, University Hospital Magdeburg, Magdeburg, Germany
Interests: radiopharmaceutical sciences; radiolabeling chemistry; radiometals for medicinal purposes; PET tracers; dosimetry for individualized treatment-planning; nuclide production; automatization
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

The different steps of developing radiopharmaceuticals, from the basic idea to their final clinical application (and approval), represent the strongly interdisciplinary character of nuclear medicine.

Preclinical as well as clinical evaluation of any novel radiopharmaceutical (antibodies, peptides, small molecules) deals with all subjects related to the identification of new molecular targets and their specific utilization for efficient nuclear medical imaging and therapy options in a variety of medical conditions such as neurodegenerative or cardiovascular metabolic disorders, cancer or other immune-associated diseases. This includes in vitro and in vivo measurements and modeling of radiotracer binding, distribution and pharmacokinetics as well as dosimetry studies. Sophisticated investigations and advances in clinical research have increasingly opened up new attractive areas of application for radiopharmaceuticals. Examples are the imaging-based patient selection and their use as theranostic tool for a personalized treatment.

The core of the design of a radiopharmaceutical is the choice of the adequate radiochemistry, which includes the choice of the radionuclide due its chemical and physical properties, its production and purification, the choice of suitable labeling strategies and precursors, which takes the chemistry and pharmacokinetics of the target vector into account. All this finally leads to an optimized automated synthesis of pharmaceutical grade radiopharmaceuticals.

The editors of this Special Issue of Molecules welcome all contributions (communications, research papers and review articles) on new advances concerning the manifold facets of radiopharmaceuticals and their development.

Dr. Elisabeth Eppard
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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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

  • radiopharmacy/radiopharmaceuticals
  • radiochemistry
  • radionuclide therapy
  • theranostics
  • PET
  • SPECT
  • radiolabeling techniques
  • radionuclide production
  • nuclear medicine

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Published Papers (4 papers)

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Research

12 pages, 1706 KiB  
Article
Synthesis and Evaluation of the First 68Ga-Labeled C-Terminal Hydroxamate-Derived Gastrin-Releasing Peptide Receptor-Targeted Tracers for Cancer Imaging with Positron Emission Tomography
by Lei Wang, Hsiou-Ting Kuo, Chao-Cheng Chen, Devon Chapple, Nadine Colpo, Pauline Ng, Wing Sum Lau, Shireen Jozi, François Bénard and Kuo-Shyan Lin
Molecules 2024, 29(13), 3102; https://doi.org/10.3390/molecules29133102 - 28 Jun 2024
Viewed by 1026
Abstract
Gastrin-releasing peptide receptor (GRPR), overexpressed in many solid tumors, is a promising imaging marker and therapeutic target. Most reported GRPR-targeted radioligands contain a C-terminal amide. Based on the reported potent antagonist D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-NHOH, we synthesized C-terminal hydroxamate-derived [68Ga]Ga-LW02075 ([68 [...] Read more.
Gastrin-releasing peptide receptor (GRPR), overexpressed in many solid tumors, is a promising imaging marker and therapeutic target. Most reported GRPR-targeted radioligands contain a C-terminal amide. Based on the reported potent antagonist D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-NHOH, we synthesized C-terminal hydroxamate-derived [68Ga]Ga-LW02075 ([68Ga]Ga-DOTA-pABzA-DIG-D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-NHOH) and [68Ga]Ga-LW02050 ([68Ga]Ga-DOTA-Pip-D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-NHOH), and compared them with the closely related and clinically validated [68Ga]Ga-SB3 ([68Ga]Ga-DOTA-pABzA-DIG-D-Phe-Gln-Trp-Ala-Val-Gly-His-Leu-NHEt). Binding affinities (Ki) of Ga-SB3, Ga-LW02075, and Ga-LW02050 were 1.20 ± 0.31, 1.39 ± 0.54, and 8.53 ± 1.52 nM, respectively. Both Ga-LW02075 and Ga-LW02050 were confirmed to be GRPR antagonists by calcium release assay. Imaging studies showed that PC-3 prostate cancer tumor xenografts were clearly visualized at 1 h post injection by [68Ga]Ga-SB3 and [68Ga]Ga-LW02050 in PET images, but not by [68Ga]Ga-LW02075. Ex vivo biodistribution studies conducted at 1 h post injection showed that the tumor uptake of [68Ga]Ga-LW02050 was comparable to that of [68Ga]Ga-SB3 (5.38 ± 1.00 vs. 6.98 ± 1.36 %ID/g), followed by [68Ga]Ga-LW02075 (3.97 ± 1.71 %ID/g). [68Ga]Ga-SB3 had the highest pancreas uptake (37.3 ± 6.90 %ID/g) followed by [68Ga]Ga-LW02075 (17.8 ± 5.24 %ID/g), while the pancreas uptake of [68Ga]Ga-LW02050 was only 0.53 ± 0.11 %ID/g. Our data suggest that [68Ga]Ga-LW02050 is a promising PET tracer for detecting GRPR-expressing cancer lesions. Full article
(This article belongs to the Special Issue New Advances in Radiopharmaceutical Sciences)
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21 pages, 5431 KiB  
Article
Increasing Analytical Quality by Designing a Thin-Layer Chromatography Scanner Method for the Determination of the Radiochemical Purity of Radiopharmaceutical Sodium Iodide 131I Oral Solution
by Miguel Vasquez-Huaman, Américo Castro-Luna, Norma Julia Ramos-Cevallos, Donald Ramos-Perfecto, Mario Alcarraz-Curi, Jacqueline Segura-Vasquez and Danny Cáceres-Antaurco
Molecules 2024, 29(8), 1883; https://doi.org/10.3390/molecules29081883 - 20 Apr 2024
Viewed by 1307
Abstract
The goal of this study was to apply the principles of analytical quality by design (AQbD) to the analytical method for determining the radiochemical purity (PQR) of the radiopharmaceutical sodium iodide 131I oral solution, utilizing thin-layer chromatography (TLC) with a radio–TLC scanner, [...] Read more.
The goal of this study was to apply the principles of analytical quality by design (AQbD) to the analytical method for determining the radiochemical purity (PQR) of the radiopharmaceutical sodium iodide 131I oral solution, utilizing thin-layer chromatography (TLC) with a radio–TLC scanner, which also enables the evaluation of product quality. For AQbD, the analytical target profile (ATP), critical quality attributes (CQA), risk management, and the method operable design region (MODR) were defined through response surface methodology to optimize the method using MINITAB® 19 software. This study encompassed the establishment of a control strategy and the validation of the method, including the assessment of selectivity, linearity, precision, robustness, detection limit, quantification limit, range, and the stability of the sample solution. Under the experimental conditions, the method parameters of the TLC scanner were experimentally demonstrated and optimized with an injection volume of 3 µL, a radioactive concentration of 10 mCi/mL, and a carrier volume of 40 µL. Statistical analysis confirmed the method’s selectivity for the 131I iodide band Rf of 0.8, a radiochemical impurity IO3− Rf of 0.6, a linearity from 6.0 to 22.0 mCi/mL, and an intermediate precision with a global relative standard deviation (RSD) of 0.624%. The method also exhibited robustness, with a global RSD of 0.101%, a detection limit of 0.09 mCi/mL, and a quantification limit of 0.53 Ci/mL, meeting the prescribed range and displaying stability over time (at 0, 2, and 20 h) with a global RSD of 0.362%, resulting in consistent outcomes. The development of a method based on AQbD facilitated the creation of a design space and an operational space, with comprehensive knowledge of the method’s characteristics and limitations. Additionally, throughout all operations, compliance with the acceptance criteria was verified. The method’s validity was confirmed under the established conditions, making it suitable for use in the manufacturing process of sodium iodide 131I and application in nuclear medicine services. Full article
(This article belongs to the Special Issue New Advances in Radiopharmaceutical Sciences)
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19 pages, 2865 KiB  
Article
[18F]fluoride Activation and 18F-Labelling in Hydrous Conditions—Towards a Microfluidic Synthesis of PET Radiopharmaceuticals
by Olga Ovdiichuk, Salla Lahdenpohja, Quentin Béen, Laurent Tanguy, Bertrand Kuhnast and Charlotte Collet-Defossez
Molecules 2024, 29(1), 147; https://doi.org/10.3390/molecules29010147 - 26 Dec 2023
Cited by 1 | Viewed by 1755
Abstract
18F-labelled radiopharmaceuticals are indispensable in positron emission tomography. The critical step in the preparation of 18F-labelled tracers is the anhydrous F-18 nucleophilic substitution reaction, which involves [18F]F− anions generated in aqueous media by the cyclotron. For this, azeotropic [...] Read more.
18F-labelled radiopharmaceuticals are indispensable in positron emission tomography. The critical step in the preparation of 18F-labelled tracers is the anhydrous F-18 nucleophilic substitution reaction, which involves [18F]F− anions generated in aqueous media by the cyclotron. For this, azeotropic drying by distillation is widely used in standard synthesisers, but microfluidic systems are often not compatible with such a process. To avoid this step, several methods compatible with aqueous media have been developed. We summarised the existing approaches and two of them have been studied in detail. [18F]fluoride elution efficiencies have been investigated under different conditions showing high 18F-recovery. Finally, a large scope of precursors has been assessed for radiochemical conversion, and these hydrous labelling techniques have shown their potential for tracer production using a microfluidic approach, more particularly compatible with iMiDEV™ cassette volumes. Full article
(This article belongs to the Special Issue New Advances in Radiopharmaceutical Sciences)
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Graphical abstract

13 pages, 3663 KiB  
Article
Synthesis and Evaluation of Compound Targeting α7 and β2 Subunits in Nicotinic Acetylcholinergic Receptor
by Karanveer Singh, Allyson Ngo, Oshini V. Keerthisinghe, Krystal K. Patel, Christopher Liang and Jogeshwar Mukherjee
Molecules 2023, 28(24), 8128; https://doi.org/10.3390/molecules28248128 - 16 Dec 2023
Cited by 1 | Viewed by 1182
Abstract
Nicotinic acetylcholine receptors (nAChRs) are involved in various central nervous system functions and have also been implicated in several neurodegenerative disorders. The heteromeric α4β2* and homomeric α7 are two major nAChR subtypes which have been studied in the brain using positron emission tomography [...] Read more.
Nicotinic acetylcholine receptors (nAChRs) are involved in various central nervous system functions and have also been implicated in several neurodegenerative disorders. The heteromeric α4β2* and homomeric α7 are two major nAChR subtypes which have been studied in the brain using positron emission tomography (PET). Our comparative autoradiographic studies of the two receptor types in the mouse and rat brains show major differences in the thalamus (α4β2* >> α7), hippocampus (α7 >> α4β2*), and subiculum (α4β2* >> α7). A relatively newer heteromeric α7β2 nAChR subtype has been identified in the brain which may have a greater role in neurodegeneration. We report the development of KS7 (3-(2-(S)-azetidinylmethoxy)-5-(1,4-diaza-bicyclo[3.2.2]nonane)pyridine) which incorporates structural features of Nifzetidine (high affinity for α4β2* nAChR) and ASEM (high affinity for α7 nAChR) in an effort to target α7 and β2 subunits in α7β2 nAChR. KS7 exhibited higher affinities (IC50 = 50 to 172 nM) for [3H]cytisine radiolabeled sites and weaker affinities (IC50 = 10 μM) for [125I]-α-bungarotoxin radiolabeled rat brain sites in several brain regions. The weaker affinity of KS7 to α7 nAChR may suggest lack of binding at the α7 subunit of α7β2 nAChR. A radiolabeled derivative of KS7 may be required to identify any specific binding to brain regions suggested to contain α7β2 nAChR. Full article
(This article belongs to the Special Issue New Advances in Radiopharmaceutical Sciences)
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