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Molecules
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Applications of Radiochemistry in Healthcare
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Applications of Radiochemistry in Healthcare

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

Deadline for manuscript submissions: 30 June 2026 | Viewed by 2063

Special Issue Editor

Dr. Pierre Bohn

E-Mail Website
Guest Editor
1. AIMS, QUANTIF, University of Rouen Normandy, 76000 Rouen, France
2. Department of Nuclear Medicine, Henri Becquerel Centre, Rouen, France
Interests: radiochemistry; radiopharmacy; nuclear medicine
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Radiochemistry is a rapidly expanding discipline within the field of healthcare. Radioligand therapies have become standard treatments for metastatic prostate cancer. Radiolabeled antibodies have also been demonstrated to possess numerous benefits for therapeutic and diagnostic applications.

The advent of antibody fragments, such as nanobodies, which hold promise for applications in diagnostics, underscores the dynamism of this research domain.

The radionuclides utilized in these processes are diverse. Metal radiochemistry involves technetium, gallium, lutetium, terbium, actinium, radium, and other radionuclides, while organic radiochemistry involves carbon, fluorine, and oxygen, among other elements. Radiochemists’ broad skills offer a wide range of possibilities for improving patient care.

The objective of this Special Issue is to disseminate knowledge and advances in this field.

Dr. Pierre Bohn
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
  • radioligand therapy
  • radiolabeled antibodies
  • nanobodies
  • radionuclides

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Published Papers (2 papers)

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Research

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12 pages, 968 KB  
Article
Preclinical Theranostic Profiling of [64Cu]Cu-Acetate in Prostate Cancer
by Sadaf Ghanaatgar Kasbi, Martin Savard, Céléna Dubuc, Yves Dory, Brigitte Guérin and Fernand Gobeil
Molecules 2025, 30(19), 3957; https://doi.org/10.3390/molecules30193957 - 2 Oct 2025
Viewed by 966
Abstract
Copper plays a critical role in cancer biology, with tumor cells exhibiting abnormal copper metabolism that drives proliferation and tumor growth. A limited number of preclinical and clinical studies have reported promising theranostic potential of copper-based radionuclides, such as 64Cu, for both [...] Read more.
Copper plays a critical role in cancer biology, with tumor cells exhibiting abnormal copper metabolism that drives proliferation and tumor growth. A limited number of preclinical and clinical studies have reported promising theranostic potential of copper-based radionuclides, such as 64Cu, for both diagnostic imaging and targeted radiotherapy in diverse cancers, including prostate cancer (PCa). In this work, we evaluated the cellular uptake and antitumor efficacy of [64Cu]Cu-acetate using both cellular and animal models of PCa. Uptake assays revealed that ~70% of the administered dose (10 kBq) was internalized by PC-3 cells within 24 h, predominantly localizing to the cytoplasm, with around 9% detected in the nucleus. These results were corroborated by comparable natural Cu-acetate uptake levels (at equimolar dose) in PC-3 cells, as quantified by ICP-MS. Clonogenic assays revealed a dose-dependent reduction in survival following treatment with [64Cu]Cu-acetate (3 and 6 MBq), whereas its non-radioactive counterpart [NatCu]Cu-acetate, even at excess concentrations (10 µM), had no significant effect. Ex vivo biodistribution studies showed selective tumor accumulation/retention alongside expected hepatic uptake. Clear tumor visualization was achieved using μPET imaging with [64Cu]Cu-acetate (10 MBq iv). A single higher dose (65 MBq iv) effectively reduced tumor growth in a subcutaneous PC-3 xenograft mouse model, without systemic toxicity, as evidenced by stable body weight. Together, these results further support the theranostic potential of [64Cu]Cu in PCa. Full article
(This article belongs to the Special Issue Applications of Radiochemistry in Healthcare)
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Review

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28 pages, 1605 KB  
Review
A Scoping Review of the Challenges and Future Perspectives in the Use of Alpha-Emitters for Metastatic Ovarian Cancer
by Lu Lucy Xu, Satyendra Kumar Singh, Nelli Gaspar, Jinda Fan, Benjamin L. Viglianti and Kurt R. Zinn
Molecules 2026, 31(6), 1019; https://doi.org/10.3390/molecules31061019 - 18 Mar 2026
Viewed by 704
Abstract
Ovarian cancer (OC) is frequently diagnosed at an advanced stage and characterized by high rates of recurrence despite aggressive cytoreductive surgery and chemotherapy. Relapse is driven by microscopic residual tumors that are disseminated most often throughout the peritoneal cavity, posing significant challenges with [...] Read more.
Ovarian cancer (OC) is frequently diagnosed at an advanced stage and characterized by high rates of recurrence despite aggressive cytoreductive surgery and chemotherapy. Relapse is driven by microscopic residual tumors that are disseminated most often throughout the peritoneal cavity, posing significant challenges with conventional systemic therapy. Targeted alpha-particle therapy (TAT) combines molecular targeting with alpha-emitting radionuclides to deliver highly potent and localized cellular damage, uniquely suited for the eradication of small OC tumor clusters within the peritoneal cavity. We conducted an extensive literature search for clinical trials (clinicaltrials.gov) and pre-clinical studies (PubMed, Scopus, Google Scholar) between September 2025 and November 2025. Peer-reviewed articles published in English over the past 20 years that used OC mouse models with reported treatment data were included. Review articles without original data and clinical trials that have been terminated or withdrawn were excluded. In this review, we (1) summarize the biological and physical rationale supporting the use of TAT in OC, (2) discuss the relevant molecular and immunological anti-tumor mechanisms, and (3) critically evaluate early treatment outcomes of 19 pre-clinical and four clinical studies with respect to efficacy, safety, and feasibility. Despite the progress and promising survival outcomes, several challenges remain, including heterogeneous antigen expression, delivery and retention within the peritoneal cavity, off-target toxicity, radiation resistance, radionuclide availability, dosimetry uncertainties, and limitations in clinical trial design. We highlight future directions to overcome these barriers and the continued multidisciplinary efforts essential to translate TAT into effective clinical strategies to treat advanced stages of OC and other solid tumors resistant to conventional treatment. This work was supported with funding available to Kurt R. Zinn as the Hickman Family Endowed Chair in Oncology at Michigan State University. Full article
(This article belongs to the Special Issue Applications of Radiochemistry in Healthcare)
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