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New Advances in Radiopharmaceutical Sciences, 2nd Edition

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

Deadline for manuscript submissions: 31 May 2026 | Viewed by 687

Special Issue Editor


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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
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Special Issue Information

Dear Colleagues,

The development of radiopharmaceuticals—from their conception to their use in patients—is a highly interdisciplinary process. It brings together the fields of chemistry, biology, medicine, physics, and engineering. Preclinical and clinical studies of new radiopharmaceuticals, whether based on antibodies, peptides, or small molecules, require expertise in identifying new molecular targets and applying them in nuclear medicine for imaging and therapy. These applications cover a wide range of conditions, including neurodegenerative diseases, heart and metabolic disorders, cancers, and immune-related illnesses.

The evaluation process involves laboratory (in vitro) and animal/human (in vivo) studies to understand how radiopharmaceuticals bind to targets, how they are distributed in the body, and how they are metabolized. Dosimetry is also involved, measuring the radiation dose delivered to tissues. Advances in research techniques and clinical studies have significantly expanded the potential of radiopharmaceuticals. Examples include imaging that helps to categorize patients according to their suitability for specific treatments, as well as the increasing use of radiopharmaceuticals as 'theranostic' tools—agents that can diagnose and treat disease, thereby supporting personalized medicine.

At the core of radiopharmaceutical design lies radiochemistry—the process of selecting the right radionuclide based on its chemical and physical properties, as well as developing methods to effectively attach it to the targeting molecule. This process involves considering how the compound will behave in the body, as well as how it can be effectively produced and purified. Ultimately, these choices enable the standardized, automated production of pharmaceutical-grade radiopharmaceuticals.

The fundamental aspect of radiopharmaceutical design is the selection of appropriate radiochemistry. This involves identifying a radionuclide based on its chemical and physical characteristics and determining suitable labeling strategies and precursors that take into account the chemistry and pharmacokinetics of the target vector, as well as its production and purification processes. Collectively, these considerations enable the optimized and automated synthesis of pharmaceutical-grade radiopharmaceuticals.

We welcome contributions of all types, including short communications, full research articles, and reviews that highlight recent progress and future directions in the field of radiopharmaceuticals.

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 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

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

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Published Papers (1 paper)

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Research

13 pages, 4475 KB  
Article
Comparative In Vitro and In Vivo Evaluation of Anti-CCR8 Full-Sized IgG and Its Fab Fragments in Murine Colorectal Cancer Models
by Tongshuo Hu, Rubin Jiao, Kevin J. H. Allen, Connor Frank, Mackenzie E. Malo and Ekaterina Dadachova
Molecules 2025, 30(22), 4445; https://doi.org/10.3390/molecules30224445 - 18 Nov 2025
Viewed by 484
Abstract
CCR8 chemokine receptor is a selective marker of tumor-infiltrating regulatory T cells (ti-Tregs) which interfere with the efficacy of checkpoint inhibitor immunotherapy (ICI) in many types of cancer. Eliminating CCR8+ ti-Tregs dramatically improves the results of subsequent ICI. We have recently reported using [...] Read more.
CCR8 chemokine receptor is a selective marker of tumor-infiltrating regulatory T cells (ti-Tregs) which interfere with the efficacy of checkpoint inhibitor immunotherapy (ICI) in many types of cancer. Eliminating CCR8+ ti-Tregs dramatically improves the results of subsequent ICI. We have recently reported using 225Actinium-labeled anti-CCR8 IgG for killing CCR8+ ti-Tregs in murine colorectal tumors which synergized with subsequent anti-CTLA4 ICI. Here, we aimed to compare the in vivo behavior of anti-CCR8 full-sized IgG and its Fab fragments to select the best antibody format for the pre-clinical development of this combination modality. Anti-CCR8 Fab fragments were generated by papain digest of the whole IgG. The whole IgG and Fab were conjugated to bifunctional chelating agent DOTA and labeled with 111Indium (111In). MC8 and CT6 murine colorectal tumor-bearing C57Bl6 and Balb/c mice, respectively, were administered 111In-DOTA-IgG or 111In-DOTA-Fab and imaged with microSPECT/CT at 2–72 h post-injection. A biodistribution was performed after the last imaging time point. Both 111In-DOTA-IgG and 111In-DOTA-Fab demonstrated high tumor uptake in both MC38 and CT26 tumors, with 111In-DOTA-IgG uptake being significantly higher from the 24 h time point and onwards. 111In-DOTA-Fab also exhibited pronounced kidney uptake which persisted even at 72 h. The kidney clearance and retention of 111In-DOTA-Fab might represent a problem during therapy employing 225Actimium or other long-lived therapeutic radionuclides by potentially causing a dose-limiting kidney toxicity. This imaging/biodistribution evaluation not only determined that full-size anti-CCR8 IgG is the optimal antibody format for pre-clinical development but also informed on the timing of immunotherapy administration in future radioimmunotherapy and immunotherapy combination studies. Full article
(This article belongs to the Special Issue New Advances in Radiopharmaceutical Sciences, 2nd Edition)
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