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Radiolabeled Compounds for Theranostic Applications in Oncology

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Oncology".

Deadline for manuscript submissions: 20 January 2026 | Viewed by 735

Special Issue Editor


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Guest Editor
1. Nuclear Medicine Department, Institut Régional du Cancer de Montpellier (ICM), University of Montpellier, 34298 Montpellier, France
2. IBMM, University Montpellier, CNRS, ENSCM, 34293 Montpellier, France
Interests: radiochemistry; medicinal chemistry; drug discovery; pharmacomodulation; radiolabeling; PET Imaging; targeted radionuclide therapy; hospital pharmacy; pharmacy technology; peptide receptor radionuclide therapy; gallium-68; lutetium-177

Special Issue Information

Dear Colleagues,

The design and evaluation of novel radiopharmaceutical candidates is an extremely dynamic and rapidly growing field, as evidenced by the increasing interest of certain pharmaceutical companies in this type of diagnostic and therapeutic tool. Indeed, the latest generation of vector molecules for nuclear medicine applications is designed to be ideally suited for use in either medical imaging or targeted radionuclide therapy, depending on the physical properties of the radioelement they carry. Given the wide range of molecular targets that can be exploited in oncology for this type of theranostic approach, preclinical research on innovative radioactive vectors is also highly active.

In this context, the editorial team of the International Journal of Molecular Sciences is developing a Special Issue titled “Radiolabeled Compounds for Theranostic Applications in Oncology”. This Special Issue will focus on all aspects of the conception, characterization, and evaluation of radiolabeled compounds for the diagnosis and treatment of cancer diseases. The application of new radiochemistry and methodologies for the development of radiolabeled probes for molecular targeting is also a key part of this topic. Submissions—both original research papers and reviews—related to the areas mentioned above are cordially invited.

Dr. Cyril Fersing
Guest Editor

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Keywords

  • radiopharmaceuticals
  • theranostic
  • cancer therapy
  • targeted radionuclide therapy
  • molecular imaging
  • positron emission tomography
  • single-photon emission tomography
  • radiolabeling

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Published Papers (1 paper)

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Research

22 pages, 3555 KB  
Article
Tailored Reaction Conditions and Automated Radiolabeling of [177Lu]Lu-PSMA-ALB-56 in a 68Ga Setting: The Critical Impact of Antioxidant Concentrations
by Johanne Vanney, Léa Rubira, Jade Torchio and Cyril Fersing
Int. J. Mol. Sci. 2025, 26(19), 9642; https://doi.org/10.3390/ijms26199642 - 2 Oct 2025
Viewed by 463
Abstract
The growing use of experimental radiopharmaceuticals for targeted radionuclide therapy (TRT) highlights the need for robust “in house” radiolabeling protocols. Among these, PSMA-ALB-56 is a PSMA ligand incorporating an albumin-binding moiety to enhance pharmacokinetics, which showed promise for prostate cancer treatment. This study [...] Read more.
The growing use of experimental radiopharmaceuticals for targeted radionuclide therapy (TRT) highlights the need for robust “in house” radiolabeling protocols. Among these, PSMA-ALB-56 is a PSMA ligand incorporating an albumin-binding moiety to enhance pharmacokinetics, which showed promise for prostate cancer treatment. This study investigated manual radiolabeling conditions of this vector molecule with lutetium-177 and developed a corresponding automated synthesis protocol. Manual experiments on low activities explored buffer systems and antioxidants, identifying sodium acetate buffer and L-methionine as optimal, achieving radiochemical purities above 97% with excellent stability over 48 h. However, when these conditions were transposed directly to an automated process on a GAIA® module with activities > 2 GBq, radiochemical purity dropped below 70% due to significant radiolysis. This result emphasized that conditions optimized at low activities are not directly transferable to high-activity automated production, and highlighted the crucial role of antioxidant concentration. An optimized automated method was subsequently developed, integrating a solid-phase extraction purification step, higher antioxidant levels during radiolabeling and formulation, and a larger final product volume. These changes led to radiochemical purities above 98.9% and excellent product stability over 120 h for 3 test batches. The presence of high concentrations of methionine and ascorbic acid was essential to protect against radiolysis. This work underscores the importance of adjusting radiolabeling strategies during process scale-up and confirmed that antioxidant concentration is essential for successful 177Lu radiolabeling. The optimized automated method developed here for [177Lu]Lu-PSMA-ALB-56 may also be adapted to other radiopharmaceuticals in development for TRT. Full article
(This article belongs to the Special Issue Radiolabeled Compounds for Theranostic Applications in Oncology)
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