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Advance in Radiochemistry, 2nd Edition
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Advance in Radiochemistry, 2nd Edition

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

Deadline for manuscript submissions: 31 December 2026 | Viewed by 6605

Special Issue Editor

Dr. Chang-Tong Yang

E-Mail Website
Guest Editor
1. Duke-NUS Medical School, 8 College Road, Singapore 169857, Singapore
2. Department of Nuclear Medicine and Molecular Imaging, Radiological Sciences Division, Singapore General Hospital, Outram Road, Singapore 169608, Singapore
Interests: radiochemistry and radiopharmaceuticals; radiolabeling techniques and radiosynthesis; production of radioisotopes; probe (radiotracer) development for nuclear imaging; theranostics of radiopharmaceuticals; radiation dose and safety
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Radiochemistry is a branch of chemistry that studies radiation from a molecular perspective and explores isotope transformation and radioactive reaction effects, a physical and medical property of radioisotopes. Research in radiochemistry is ongoing, with radioisotopes used to label chemical compounds such as radiopharmaceuticals (radiotracers) for drug development, involving radiopharmaceutical design and preparation, in vitro and in vivo biological studies, pharmacological study, and preclinical and clinical studies. 

This Special Issue will focus on the development of radiopharmaceuticals and their theranostic applications. Radiopharmaceuticals include all physicochemically characterized molecular structures such as small organic molecules, coordination compounds, and nanomaterials. The development of radiopharmaceuticals is devoted to (1) preparation of precursors; (2) radiolabeling techniques including radiosynthesis, purification, and analysis; (3) in vitro and in vivo radiopharmaceutical research and pharmacological investigation; (4) radiotracers for PET/SPECT imaging, preclinical trials, diagnostic and therapeutic applications, and potential personalized medicine.

Dr. Chang-Tong Yang
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 250 words) can be sent to the Editorial Office for assessment.

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

  • radiochemistry
  • radionuclide (radioisotopes)
  • radiolabeling
  • radiopharmaceutical (radiotracer)
  • nuclear medicine
  • theranostics (diagnostics and therapeutics)
  • molecular imaging

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Related Special Issue

Published Papers (6 papers)

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Research

12 pages, 3296 KB  
Article
Cassette-Based Automated Production of 2-Deoxy-2-[18F]fluorocellobiose on the Trasis AllInOne with Undetectable [18F]FDG Contamination
by Falguni Basuli, Jianfeng Shi, Swati Shah, Jianhao Lai, Dima A. Hammoud and Rolf E. Swenson
Molecules 2026, 31(8), 1260; https://doi.org/10.3390/molecules31081260 - 10 Apr 2026
Viewed by 436
Abstract
The global rise in the incidence and severity of invasive fungal infections, particularly among immunocompromised and immunodeficient patients, has created an urgent need for rapid and accurate diagnostic techniques. Therefore, fungal-specific positron emission tomography imaging agents are increasingly in demand, as they offer [...] Read more.
The global rise in the incidence and severity of invasive fungal infections, particularly among immunocompromised and immunodeficient patients, has created an urgent need for rapid and accurate diagnostic techniques. Therefore, fungal-specific positron emission tomography imaging agents are increasingly in demand, as they offer the potential for early-stage detection of fungal infections. Recently, 2-deoxy-2-[18F]fluorocellobiose ([18F]FCB), a fluorine-18-labeled analog of cellobiose that is selectively metabolized by fungal pathogens possessing cellulose-degrading mechanisms (cellulolytic), was developed for the targeted imaging of Aspergillus infections. However, the final [18F]FCB contained less than 2% unreacted 2-deoxy-2-[18F]fluoroglucose ([18F]FDG), which can potentially interfere with image interpretation. Accordingly, this study aims to eliminate residual [18F]FDG from the final product by enzymatically converting it to [18F]FDG-6-phosphate through hexokinase-mediated phosphorylation. A Trasis AllInOne (Trasis AIO) module was used to automate the radiolabeling procedure. The reagent vials contain [18F]FDG, glucose-1-phosphate, cellobiose phosphorylase, adenosine triphosphate (ATP), and hexokinase. A Sep-Pak cartridge was used to purify the tracer. The overall radiochemical yield was 45–50% (n = 3, decay-corrected) in a 40 min synthesis time, with a radiochemical purity of >99% (no detectable [18F]FDG). This is a highly reliable protocol to produce current good manufacturing practice (cGMP)-compliant [18F]FCB for clinical PET imaging. Full article
(This article belongs to the Special Issue Advance in Radiochemistry, 2nd Edition)
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20 pages, 1455 KB  
Article
Preclinical Evaluation of a Radiolabeled Anti-PSMA Dimeric Aptamer in a Murine Model of Human Prostate Cancer
by Akesh Sinha, Darpan N. Pandya, Prabhakar Eeka, Olcay Boyacioglu, William H. Gmeiner and Thaddeus J. Wadas
Molecules 2026, 31(3), 493; https://doi.org/10.3390/molecules31030493 - 31 Jan 2026
Viewed by 523
Abstract
Prostate cancer is the third-leading cause of cancer death in men. Prostate-specific membrane antigen (PSMA) is a robust biomarker that is expressed in approximately 80% of patients diagnosed with prostate cancer; several theranostic strategies have emerged based upon targeting this biomarker. This report [...] Read more.
Prostate cancer is the third-leading cause of cancer death in men. Prostate-specific membrane antigen (PSMA) is a robust biomarker that is expressed in approximately 80% of patients diagnosed with prostate cancer; several theranostic strategies have emerged based upon targeting this biomarker. This report describes a dimeric aptamer complex (DAC) which is selective for PSMA+ cancer cells and is amenable to derivatization with additional diagnostic and therapeutic molecules. Confocal microscopy confirmed the selective nature of the DAC for PSMA+ LNCAP tumor cells. In addition, the affinity of the DAC for the PSMA protein was determined to be 2.16 ± 0.15 nM using biolayer interferometry (BLI). In proof-of-principle studies, this DAC was biotinylated (BioDAC; A10), complexed with streptavidin (SA), and radiolabeled with the positron-emitting radioisotope zirconium-89 (89Zr: t½ = 78.4 h, β+: 22.8%) to form the radiopharmaceutical [89Zr]Zr-Df-SA-BioDAC ([89Zr]Zr-A12). Acute biodistribution studies revealed elevated levels of radioactivity in PSMA+ tumors when compared to PSMA− tumors. Radioactivity retention in the kidney was high due to the presence of streptavidin, while radioactivity retention in the liver was comparable with that of other radiolabeled aptamer complexes. Accordingly, the data suggests that the radiopharmaceutical will need to be redesigned using a strategy that is not reliant on a biotin–streptavidin paradigm before additional preclinical assessments are made and clinical translation can be attempted. Full article
(This article belongs to the Special Issue Advance in Radiochemistry, 2nd Edition)
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16 pages, 2524 KB  
Article
Synthesis and Evaluation of Radiogallium-Labeled Peptide Probes for In Vivo Imaging of Legumain Activity
by Takeshi Fuchigami, Kohnosuke Itagaki, Sakura Yoshida, Morio Nakayama, Masayuki Munekane and Kazuma Ogawa
Molecules 2025, 30(23), 4527; https://doi.org/10.3390/molecules30234527 - 24 Nov 2025
Cited by 1 | Viewed by 891
Abstract
Legumain (LGMN), a lysosomal cysteine protease, is crucial for tumor progression, invasion, and metastasis, making it a promising target for cancer imaging and therapy. This study developed novel 67Ga-labeled 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA)-conjugated LGMN-cleavable peptide probes ([67Ga]Ga-NOTA-LCPs) composed of polyarginine and [...] Read more.
Legumain (LGMN), a lysosomal cysteine protease, is crucial for tumor progression, invasion, and metastasis, making it a promising target for cancer imaging and therapy. This study developed novel 67Ga-labeled 1,4,7-triazacyclononane-1,4,7-triacetic acid (NOTA)-conjugated LGMN-cleavable peptide probes ([67Ga]Ga-NOTA-LCPs) composed of polyarginine and polyglutamic acid sequences linked by LGMN-cleavable sites for nuclear medicine imaging of LGMN activity. The probes were synthesized via fluorenylmethoxycarbonyl solid-phase peptide synthesis and radiolabeled in high radiochemical yields. In vitro assays with HCT116 cells showed significantly higher uptake of [67Ga]Ga-NOTA-LCPs compared to non-cleavable controls, confirming efficient cleavage and cellular uptake. In vivo studies in tumor-bearing mice revealed rapid renal clearance, low non-specific binding, and favorable tumor-to-blood ratios, particularly for [67Ga]Ga-NOTA-LCP-1. These results demonstrate the potential of [67Ga]Ga-NOTA-LCPs as effective LGMN-responsive imaging agents, with further optimization needed to improve tumor specificity and reduce off-target accumulation. Full article
(This article belongs to the Special Issue Advance in Radiochemistry, 2nd Edition)
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18 pages, 1494 KB  
Article
The Evaluation of (1R,4R,7R,10R)-α,α′,α″,α‴-Tetramethyl-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic Acid (DOTMA) as a Chelator for Zirconium-89
by Darpan N. Pandya, Pere Miro, Michael A. Sinnwell, George B. Crull and Thaddeus J. Wadas
Molecules 2025, 30(20), 4129; https://doi.org/10.3390/molecules30204129 - 19 Oct 2025
Viewed by 1232
Abstract
Recently, macrocycles such as 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) have been observed to form zirconium-89 (89Zr: t½ = 78.4 h, β+: 22.8%, Eβ+max = 901 keV; EC: 77%, Eγ = 909 keV)-complexes with excellent in vivo stability. In this report, [...] Read more.
Recently, macrocycles such as 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) have been observed to form zirconium-89 (89Zr: t½ = 78.4 h, β+: 22.8%, Eβ+max = 901 keV; EC: 77%, Eγ = 909 keV)-complexes with excellent in vivo stability. In this report, we describe (1R,4R,7R,10R)-α,α′,α″,α‴-tetramethyl-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTMA) as an 89Zr chelator. Using [89Zr]ZrCl4, [89Zr]Zr-DOTMA was prepared in 99% radiochemical yield and a molar activity of 1055 ± 6 MBq/µmol. In vitro studies revealed a LogP value of −2.97± 0.02 and a radiometal complex that was inert when challenged with 1000-fold excess EDTA or high concentrations of biologically relevant metal ions. Finally, biodistribution studies revealed that the radiometal complex demonstrated in vivo behavior that was like [89Zr]Zr-DOTA and superior to [89Zr]Zr-DFO. Despite these promising observations, the elevated temperature required to form the [89Zr]Zr-DOTMA complex and the lack of derivatives available for bioconjugation will require additional ligand engineering to improve its utility for future nuclear medicine applications. Full article
(This article belongs to the Special Issue Advance in Radiochemistry, 2nd Edition)
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17 pages, 2255 KB  
Article
Engineering a Radiohybrid PSMA Ligand with an Albumin-Binding Moiety and Pharmacokinetic Modulation via an Albumin-Binding Competitor for Radiotheranostics
by Saki Hirata, Hiroaki Echigo, Masayuki Munekane, Kenji Mishiro, Kohshin Washiyama, Takeshi Fuchigami, Hiroshi Wakabayashi, Kazuhiro Takahashi, Seigo Kinuya and Kazuma Ogawa
Molecules 2025, 30(13), 2804; https://doi.org/10.3390/molecules30132804 - 29 Jun 2025
Cited by 2 | Viewed by 1658
Abstract
The prostate-specific membrane antigen (PSMA) is a well-established target for radiotheranostics in prostate cancer. We previously demonstrated that 4-(p-astatophenyl)butyric acid (APBA), an albumin-binding moiety (ABM) labeled with astatine-211 (211At), enables the modulation of pharmacokinetics and enhancement of therapeutic efficacy [...] Read more.
The prostate-specific membrane antigen (PSMA) is a well-established target for radiotheranostics in prostate cancer. We previously demonstrated that 4-(p-astatophenyl)butyric acid (APBA), an albumin-binding moiety (ABM) labeled with astatine-211 (211At), enables the modulation of pharmacokinetics and enhancement of therapeutic efficacy when combined with the post-administration of an albumin-binding competitor. However, this strategy has not been explored in PSMA-targeting ligands. We designed and synthesized [211At]6, a novel PSMA ligand structurally analogous to PSMA-617 with APBA. The compound was obtained via a tin–halogen exchange reaction from the corresponding tributylstannyl precursor. Comparative cellular uptake and biodistribution studies were conducted with [211At]6, its radioiodinated analog [125I]5, and [67Ga]Ga-PSMA-617. To assess pharmacokinetic modulation, sodium 4-(p-iodophenyl)butanoate (IPBA), an albumin-binding competitor, was administered 1 h postinjection of [125I]5 and [211At]6 at a 10-fold molar excess relative to blood albumin. The synthesis of [211At]6 gave a radiochemical yield of 15.9 ± 7.7% and a radiochemical purity > 97%. The synthesized [211At]6 exhibited time-dependent cellular uptake and internalization, with higher uptake levels than [67Ga]Ga-PSMA-617. Biodistribution studies of [211At]6 in normal mice revealed a prolonged blood retention similar to those of [125I]5. Notably, post-administration of IPBA significantly reduced blood radioactivity and non-target tissue accumulation of [125I]5 and [211At]6. We found that ABM-mediated pharmacokinetic control was applicable to PSMA-targeted radiotherapeutics, broadening its potential for the optimization of radiotheranostics. Full article
(This article belongs to the Special Issue Advance in Radiochemistry, 2nd Edition)
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11 pages, 1309 KB  
Article
Cytotoxicity Comparison of 99mTc-Labeled Peptide Antagonist and Agonist Targeting the SSTR2 Receptor in AR42J Cells
by Sahar Nosrati Shanjani, Monika Łyczko, Rafał Walczak, Przemysław Koźmiński, Emilia Majka, Jerzy Narbutt, Wioletta Wojdowska, Agnieszka Majkowska-Pilip and Aleksander Bilewicz
Molecules 2025, 30(8), 1715; https://doi.org/10.3390/molecules30081715 - 11 Apr 2025
Viewed by 1264
Abstract
Auger electrons are low-energy, high-linear-energy-transfer particles that deposit their energy over nanometers distances. Their biological impact depends heavily on where the radionuclide is localized within the cell. To verify the hypothesis that the cell membrane may be a better molecular target than the [...] Read more.
Auger electrons are low-energy, high-linear-energy-transfer particles that deposit their energy over nanometers distances. Their biological impact depends heavily on where the radionuclide is localized within the cell. To verify the hypothesis that the cell membrane may be a better molecular target than the cytoplasm in Auger electron therapy, we investigated whether the radiotoxicity of 99mTc varied depending on its location in the cell. The behavior of peptide radiopharmaceuticals 99mTc-TECANT-1 targeted the cell membrane was compared with 99mTc-TEKTROTYD directed to the cytoplasm. Our findings confirmed that 99mTc-TECANT-1 displayed greater binding to AR-42-J cells than 99mTc-TEKTROTYD. Additionally, it was demonstrated that the receptor agonist 99mTc-TEKTROTYD is localized in more than 90% of the cytoplasm, while 99mTc-TECANT-1 is found in 60–80% of the cell membrane. When evaluating cell survival using the MTS assay, we observed that toxicity was significantly higher when 99mTc was targeted to the membrane compared to the cytoplasm. This indicates that, for 99mTc, as with 161Tb, the membrane is a more sensitive target for Auger electrons than the cytoplasm. Our results also suggest that receptor antagonists labelled with therapeutic doses of 99mTc may be effective in treating certain cancers. However, further detailed studies, particularly dosimetric investigations, are necessary to validate these findings. Full article
(This article belongs to the Special Issue Advance in Radiochemistry, 2nd Edition)
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