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New Insights into Radiopharmaceuticals
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New Insights into Radiopharmaceuticals

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

Deadline for manuscript submissions: closed (31 October 2024) | Viewed by 2395

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, as well as the physical and medical properties of radioisotopes. In radiochemistry, research is being carried out using radioisotopes to label chemical compounds as radiopharmaceuticals (radiotracers) for drug development, such as 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 physicochemically characterized molecular structures such as small organic molecules, coordination compounds, and nanomaterials. The development of radiopharmaceuticals comprises (1) the preparation of precursors and the production of radioisotopes; (2) radiolabeling techniques such as radiosynthesis, purification, and analysis; (3) in vitro and in vivo radiopharmaceutical research and pharmacological investigation; (4) radiotracers for PET/SPECT imaging, preclinical or clinical trials, diagnostic and therapeutic applications, and potential personalized medicine; and (5) radiation dose safety and toxicity.

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 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

  • radiochemistry and radiopharmaceuticals
  • radiolabeling techniques and radiosynthesis
  • production of radioisotopes
  • probe (radiotracer) development for nuclear imaging
  • theranostics of radiopharmaceuticals
  • radiation dose and safety

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Further information on MDPI's Special Issue policies can be found here.

Published Papers (2 papers)

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Research

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14 pages, 4428 KiB  
Article
Development of 111In-Labeled Monoclonal Antibodies Targeting SFTSV Structural Proteins for Molecular Imaging of SFTS Infectious Diseases by SPECT
by Takeshi Fuchigami, Mya Myat Ngwe Tun, Yusuke Tanahara, Kodai Nishi, Sakura Yoshida, Kazuma Ogawa, Morio Nakayama and Daisuke Hayasaka
Molecules 2025, 30(1), 38; https://doi.org/10.3390/molecules30010038 - 26 Dec 2024
Viewed by 898
Abstract
No effective vaccines or treatments are currently available for severe fever with thrombocytopenia syndrome (SFTS), a fatal tick-borne infectious disease caused by the SFTS virus (SFTSV). This study evaluated the potential of 111In-labeled anti-SFTSV antibodies targeting SFTSV structural proteins as single-photon emission [...] Read more.
No effective vaccines or treatments are currently available for severe fever with thrombocytopenia syndrome (SFTS), a fatal tick-borne infectious disease caused by the SFTS virus (SFTSV). This study evaluated the potential of 111In-labeled anti-SFTSV antibodies targeting SFTSV structural proteins as single-photon emission computed tomography (SPECT) imaging agents for the selective visualization of SFTSV-infected sites. This study used nuclear medicine imaging to elucidate the pathology of SFTS and assess its therapeutic efficacy. Immunostaining experiments confirmed that the anti-SFTSV antibody (N-mAb), which targets the N protein, specifically accumulated in SFTSV-infected Vero E6 cells. 111In-labeled N-mAb was successfully prepared using a diethylenetriaminepentaacetic acid (DTPA) chelator, resulting in [111In]In-DTPA-N-mAb with high radiochemical purity exceeding 95% and a radiochemical yield of 55%. Cell-binding assays using SFTSV-infected Vero E6 cells demonstrated that [111In]In-DTPA-N-mAb binding was detectable even without membrane permeabilization, with the binding intensity correlating with infection levels. In vivo studies using SFTSV-infected A129 mice showed high spleen accumulation of [111In]In-DTPA-N-mAb (87.5% ID/g), consistent with SFTSV tropism, compared to 12.3% ID/g in mock-infected mice. SPECT/CT imaging clearly revealed high radioactivity in these regions. Although nonspecific accumulation was noted in the liver and spleen, this issue may be mitigated through antibody modifications such as fragmentation or PEGylation. Overall, [111In]In-DTPA-N-mAb is a promising imaging agent for non-invasive visualization of SFTSV-infected sites and may aid in elucidating SFTS pathology and assessing therapeutic efficacy. Full article
(This article belongs to the Special Issue New Insights into Radiopharmaceuticals)
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Review

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25 pages, 2389 KiB  
Review
Future Prospect of Low-Molecular-Weight Prostate-Specific Membrane Antigen Radioisotopes Labeled as Theranostic Agents for Metastatic Castration-Resistant Prostate Cancer
by Ratu Ralna Ismuha, Rien Ritawidya, Isti Daruwati and Muchtaridi Muchtaridi
Molecules 2024, 29(24), 6062; https://doi.org/10.3390/molecules29246062 - 23 Dec 2024
Viewed by 1087
Abstract
Prostate cancer ranks as the fourth most common cancer among men, with approximately 1.47 million new cases reported annually. The emergence of prostate-specific membrane antigen (PSMA) as a critical biomarker has revolutionized the diagnosis and treatment of prostate cancer. Recent advancements in low-molecular-weight [...] Read more.
Prostate cancer ranks as the fourth most common cancer among men, with approximately 1.47 million new cases reported annually. The emergence of prostate-specific membrane antigen (PSMA) as a critical biomarker has revolutionized the diagnosis and treatment of prostate cancer. Recent advancements in low-molecular-weight PSMA inhibitors, with their diverse chemical structures and binding properties, have opened new avenues for research and therapeutic applications in prostate cancer management. These novel agents exhibit enhanced tumor targeting and specificity due to their small size, facilitating rapid uptake and localization at the target site while minimizing the retention in non-target tissues. The primary aim of this study is to evaluate the potential of low-molecular-weight PSMA inhibitors labeled with radioisotopes as theranostic agents for prostate cancer. This includes assessing their efficacy in targeted imaging and therapy and understanding their pharmacokinetic properties and mechanisms of action. This study is a literature review focusing on in vitro and clinical research data. The in vitro studies utilize PSMA-targeted radioligands labeled with radioisotopes to assess their binding affinity, specificity, and internalization in prostate cancer cell lines. Additionally, the clinical studies evaluate the safety, effectiveness, and biodistribution of radiolabeled PSMA ligands in patients with advanced prostate cancer. The findings indicate promising outcomes regarding the safety and efficacy of PSMA-targeted radiopharmaceuticals in clinical settings. The specific accumulation of these agents in prostate tumor lesions suggests their potential for various applications, including imaging and therapy. This research underscores the promise of radiopharmaceuticals targeting PSMA in advancing the diagnosis and treatment of prostate cancer. These agents improve diagnostic accuracy and patients’ outcomes by enhancing imaging capabilities and enabling personalized treatment strategies. Full article
(This article belongs to the Special Issue New Insights into Radiopharmaceuticals)
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