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Pharmaceuticals
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Advancements in Radiopharmaceutical Theranostics
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Advancements in Radiopharmaceutical Theranostics

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Radiopharmaceutical Sciences".

Deadline for manuscript submissions: 20 October 2026 | Viewed by 4418

Editors

Dr. Aiko Yamaguchi

E-Mail Website
Guest Editor
Department of Cancer Systems Imaging, University of Texas MD Anderson Cancer Center, 1881 East Rd., Houston, TX 77054, USA
Interests: antibody-drug conjugates; radiotheranostics; bioconjugation; targeted radionuclide therapy; nanobody-drug conjugates; antibody-radionuclide conjugates; radiochemistry; biorthogonal click chemistry
Special Issues, Collections and Topics in MDPI journals
Dr. Shilpa Sharma

E-Mail Website
Guest Editor
Department of Cancer Systems Imaging, University of Texas MD Anderson Cancer Center, 1881 East Rd., Houston, TX 77054, USA
Interests: radiotheranostics; radiopharmaceutical synthesis; radiometal chelation; drug discovery; fluorescence spectroscopy; fluorescence image-guided surgery
Dr. Ryan Patrick Coll

E-Mail Website
Guest Editor
Department of Cancer Systems Imaging, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA
Interests: radiotheranostics; radiochemistry; targeted radionuclide therapy; molecular imaging; radiometal chelation; bioconjugation; bioorthogonal click chemistry

Special Issue Information

Dear Colleagues,

Theranostics is a rapidly growing field in medical science, demonstrating remarkable advancements over the past decade. Radiopharmaceutical theranostics, the most clinically established application of theranostics, combines molecules possessing specificity for biological features amplified in disease-associated sites with radionuclides of varied emission profiles of medical relevance. By leveraging a targeting vector of biologically inspired design, theranostic radiopharmaceuticals can accurately deliver radioactivity to the disease location, enhancing the imaging quality and therapeutic efficacy while significantly reducing damage to healthy tissues. Furthermore, the modular nature provided by theranostics, through which the vector molecule’s chemical properties as well as the physical nature of the radionuclide’s decay scheme can be optimized based on both the disease’s nature and the patient’s specific needs, is paving the way for more personalized and efficient healthcare.

This Special Issue invites scientists and healthcare professionals to contribute their expert opinion and groundbreaking research findings on radiopharmaceutical theranostics. We welcome original research articles, reviews, and short communications that explore technical advancements in radiopharmaceutical theranostics, including, but not limited to, the use of novel targeting ligands, such as small molecules, peptides, and biologics as well as emerging radionuclides such as alpha particle emitters, including 225Ac and 211At, and the incorporation of true radiotheranostic isotope pairs, such as 64Cu/67Cu. Also of great interest are manuscripts detailing innovative discoveries in radiochemistry and imaging-derived dosimetry measurements. In addition, we welcome discussions regarding the challenges associated with the clinical translation of radiopharmaceutical theranostics.

Dr. Aiko Yamaguchi
Dr. Shilpa Sharma
Dr. Ryan Patrick Coll
Guest Editors

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-anonymized peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly 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 2900 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

  • radiopharmaceuticals
  • radiotheranostics
  • emerging radionuclides
  • radiometals
  • image-guided dosimetry
  • alpha-emitters
  • PET
  • SPECT
  • radioligand therapy
  • targeted radionuclide therapy

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Published Papers (4 papers)

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21 pages, 7419 KB  
Article
In Vitro Radiobiological Evaluation of [64Cu]CuCl2 for Theranostic Applications
by Francesca Porto, Silvia Pasquini, Chiara Contri, Martina Cappello, Giorgia Speltri, Alessandra Boschi, Licia Uccelli, Rebecca Napolitano, Lorenza Marvelli, Katia Varani, Giovanni Di Domenico, Petra Martini and Fabrizio Vincenzi
Pharmaceuticals 2026, 19(7), 1033; https://doi.org/10.3390/ph19071033 - 2 Jul 2026
Viewed by 347
Abstract
Background/Objectives: Intrinsic genetic instability and the marked heterogeneity of malignant cell populations represent significant clinical challenges in oncology, often limiting the efficacy of conventional receptor-targeted and antigen-based therapies. To overcome these limitations, [64Cu]CuCl2 has emerged as a particularly promising [...] Read more.
Background/Objectives: Intrinsic genetic instability and the marked heterogeneity of malignant cell populations represent significant clinical challenges in oncology, often limiting the efficacy of conventional receptor-targeted and antigen-based therapies. To overcome these limitations, [64Cu]CuCl2 has emerged as a particularly promising theranostic agent because it combines PET imaging (β+ emission) with therapeutic effects (β− particles and Auger electrons). In particular, Auger electrons, when delivered to the cell nucleus, induce severe DNA damage due to their high linear energy transfer and very short tissue range. This work aimed to deepen existing preclinical knowledge by providing a comprehensive in vitro analysis of the interactions of [64Cu]CuCl2 with various human cancer cell lines—specifically, the breast adenocarcinoma (MDAf-MB-231) and gastric carcinoma (NCI-N87) cell lines—and a healthy control (IMR-90 normal human fetal lung fibroblasts). Methods: We focused on evaluating cellular uptake, subcellular localization, impact on metabolic activity, and induction of apoptosis. Cell lines (MDA-MB-231, NCI-N87, IMR-90) were exposed to increasing activities of [64Cu]CuCl2 (10, 100, and 250 µCi/mL). Uptake was assessed in both nuclear and cytoplasmic compartments after 4 h. Metabolic activity and apoptosis/necrosis were evaluated at 96 and 120 h post-treatment. Results: Tumor cell lines demonstrated significantly higher [64Cu]CuCl2 uptake, particularly at the nuclear level, compared to healthy controls. A marked decrease in metabolic activity and an increase in apoptosis were observed in MDA-MB-231 and NCI-N87 cells (from 50% to 90% and 5% to 60% apoptosis, respectively). In contrast, IMR-90 cells exhibited minimal cytotoxic response (≤20%), suggesting a preferential response in the malignant cell models tested. Conclusions: [64Cu]CuCl2 induced distinct patterns of intracellular accumulation and biological response among the investigated cell models, with cancer cells displaying greater nuclear uptake and apoptotic susceptibility than non-malignant cells. These findings provide a high-resolution radiobiological baseline and microdosimetric validation, supporting the rigorous design of future, dedicated in vivo preclinical investigations to evaluate the translational potential of ionic [64Cu]CuCl2. Full article
(This article belongs to the Special Issue Advancements in Radiopharmaceutical Theranostics)
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21 pages, 8133 KB  
Article
Practical Aspects of 161Tb Production
by Marie Skálová, Tereza Janská, Matěj Štíbr, Martin Vlk, Jaroslav Šoltés, Miroslav Vinš, Sindre Hassfjell, Jiri Muller and Ján Kozempel
Pharmaceuticals 2026, 19(4), 619; https://doi.org/10.3390/ph19040619 - 14 Apr 2026
Viewed by 1088
Abstract
Background/Objectives: Terbium-161 is an interesting and promising theranostic radionuclide, thanks to its decay characteristics (T1/2 = 6.95 d, E(β)max = 593 keV, E(β)av = 154 keV, E(γ) = 74.6 keV (10.2%)). Having similar chemical properties, it is considered as [...] Read more.
Background/Objectives: Terbium-161 is an interesting and promising theranostic radionuclide, thanks to its decay characteristics (T1/2 = 6.95 d, E(β)max = 593 keV, E(β)av = 154 keV, E(γ) = 74.6 keV (10.2%)). Having similar chemical properties, it is considered as an alternative to currently used 177Lu. In addition, 161Tb emits a significant amount of conversion and Auger electrons, which contribute to the enhancement of localised therapeutic effect. The aim of this paper is to describe the preparation of 161Tb in quantity and quality relevant for preclinical and early clinical studies and to provide practical notes on the preparation. Methods: No-carrier-added 161Tb has been repeatedly prepared by neutron irradiation of highly enriched 160Gd targets (up to 98 mg of 160Gd2O3) at nuclear reactor LVR-15 (CV Řež, Czech Republic) in four different irradiation positions. The separation and purification process of 161Tb from the bulk of 160Gd target was performed by cation exchange chromatography with Dowex 50 W × 8 (H+ cycle, 200–400 mesh). Terbium-161 was obtained in 161TbCl3 form and formulated into 0.1 M HCl solution. The γ-ray spectrometry was used for radionuclide identification and radionuclidic purity and the ICP-MS method for chemical purity measurements and specific activity determination. The DOTA labelling assay was performed, as described by Gracheva et al., providing an assessment of the apparent molar activity of the preparation in terms of its competitive interaction with stable daughter nuclide 161Dy. Results: Irradiations (59.2 h to 421.52 h) of enriched 160Gd targets with mass ranging from 43.4 to 144.0 mg for 160Gd(NO3)3 and from 12.5 to 98.3 mg for 160Gd2O3 yielded 1.3–23.7 GBq of 161Tb. The separation yields of purified 161Tb varied from 85 to 99%, with the activities of 9.9–22.1 GBq and the highest achieved specific activity of the final product was 4.1 GBq/μg (of Tb). The DOTA chelator was radiolabelled with 161Tb at time points from 2 to 14 days after the end of separation (EOS). Conclusions: Based on our results, we describe practical aspects of terbium production at the laboratory scale with a particular focus on practical aspects and issues arising during the process that may surprise even experienced radiochemists, as lanthanoid separation is not always straightforward, even though it is well-known and has been extensively studied. The preparation of 161Tb in a n.c.a. form proceeds, according to the reported data, with high reproducibility and achieves significant activity levels suitable for both preclinical and clinical investigations by irradiation of highly enriched 160Gd targets in LVR-15 reactor with subsequent separation and purification of 161Tb on cation exchange resin Dowex 50 W × 8(H+). The produced [161Tb]TbCl3 is employed in subsequent experimental research and development for the labelling of preparations intended for preclinical applications. Full article
(This article belongs to the Special Issue Advancements in Radiopharmaceutical Theranostics)
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12 pages, 1419 KB  
Article
Alpha Therapy Beyond TOC and TATE—Production, Quality Control, and In-Human Results for the SSTR2 Antagonist DOTA-LM3
by Lukas Greifenstein, Marcel Martin, Sarah Stephan, Aleksandr Eismant, Carsten S. Kramer, Christian Landvogt, Corinna Mueller, Frank Rösch and Richard P. Baum
Pharmaceuticals 2026, 19(1), 172; https://doi.org/10.3390/ph19010172 - 19 Jan 2026
Cited by 1 | Viewed by 1369
Abstract
Objectives: Peptide receptor radionuclide therapy (PRRT) of neuroendocrine tumors (NETs) commonly relies on somatostatin receptor subtype 2 (SSTR2) agonists such as DOTA-TOC/TATE, which may show limited efficacy due to high hepatic uptake and therapy resistance in some patients. SSTR2 antagonists have demonstrated [...] Read more.
Objectives: Peptide receptor radionuclide therapy (PRRT) of neuroendocrine tumors (NETs) commonly relies on somatostatin receptor subtype 2 (SSTR2) agonists such as DOTA-TOC/TATE, which may show limited efficacy due to high hepatic uptake and therapy resistance in some patients. SSTR2 antagonists have demonstrated superior tumor targeting. This study aimed to establish the production and quality control of the Actinium-225-labeled SSTR2 antagonist [225Ac]Ac-DOTA-LM3 and to report in-human clinical experience with targeted alpha therapy (TAT). Methods: [225Ac]Ac-DOTA-LM3 was produced by radiolabeling DOTA-LM3 with Actinium-225 under validated conditions. Radiochemical conversion, purity, yield, and stability were assessed using radio-TLC, fractionated radio-HPLC combined with gamma spectroscopy, and in vitro serum stability testing. Clinical feasibility and therapeutic response were evaluated in a patient with metastatic neuroendocrine pancreatic neoplasm refractory to prior 177Lu-based PRRT. Results: Radiolabeling achieved reproducibly high radiochemical purity (>97%) and decay-corrected yields exceeding 80%. The radiopharmaceutical showed high in vitro stability with minimal release of free Actinium-225 over five days. Fractionated radio-HPLC enabled indirect purity assessment. In the reported patient, [225Ac]Ac-DOTA-LM3 therapy resulted in partial remission without clinically relevant hematologic, renal, or hepatic toxicity and was associated with marked clinical improvement. Conclusions: [225Ac]Ac-DOTA-LM3 can be produced with high purity and stability using clinically applicable procedures. In-human results suggest promising efficacy and safety, supporting further clinical investigation of Actinium-225-labeled SSTR2 antagonists for advanced NETs. Full article
(This article belongs to the Special Issue Advancements in Radiopharmaceutical Theranostics)
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12 pages, 256 KB  
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Radiopharmaceutical Theranostics in Primary Adrenal Malignancies: A Surgeon’s Perspective
by Styliani Laskou, George Geropoulos, Petre Adrian Radu, Catalin Pirvu, Valeriu Surlin, Christoforos Kosmidis, Kyriakos Psarras, Stelian Pantea, Victor Strambu and Konstantinos Sapalidis
Pharmaceuticals 2026, 19(5), 664; https://doi.org/10.3390/ph19050664 - 24 Apr 2026
Viewed by 692
Abstract
Radiopharmaceutical Theranostics defines the combination of molecularly targeted imaging and therapy in two consecutive phases. Targeted theranostic approaches are most established for the management of advanced prostate, thyroid and hepatocellular cancer, as well as neuroendocrine tumors (NETs). Adrenal malignancies present a complex challenge, [...] Read more.
Radiopharmaceutical Theranostics defines the combination of molecularly targeted imaging and therapy in two consecutive phases. Targeted theranostic approaches are most established for the management of advanced prostate, thyroid and hepatocellular cancer, as well as neuroendocrine tumors (NETs). Adrenal malignancies present a complex challenge, requiring highly specialized management. The two primary entities addressed by targeted radiotheranostics—pheochromocytoma/paraganglioma (PPGL) and adrenocortical cancer (ACC)—consist of fundamentally distinct molecular targets and, consequently, different radiopharmaceutical agents. While most existing literature focuses on nuclear medicine–driven perspectives, the implications of theranostic advances for surgical decision-making remain underexplored. This narrative review aims to integrate available clinical evidence with multidisciplinary practice considerations, in reshaping the role of surgery in adrenal malignancies. Full article
(This article belongs to the Special Issue Advancements in Radiopharmaceutical Theranostics)
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