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Pharmaceuticals
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Advances in Theranostic Radiopharmaceuticals
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Advances in Theranostic Radiopharmaceuticals

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

Deadline for manuscript submissions: 31 May 2026 | Viewed by 2097

Special Issue Editor

Dr. Janke Kleynhans

E-Mail Website
Guest Editor
Laboratory for Radiopharmaceutical Research, Department of Pharmaceutical and Pharmacological Sciences, KU Leuven, 3000 Leuven, Belgium
Interests: radiochemistry; radiopharmacy; generator-based radionuclides; preclinical imaging; radioanalytical procedures

Special Issue Information

Dear Colleagues,

Over the past decade, the field of theranostic radiopharmaceuticals has rapidly expanded to take centre stage in the field of precision medicine. This paradigm has been proven successful and is currently being expanded beyond traditional targets to include new mechanisms, radionuclides, and delivery systems that are being applied in the field of Nuclear Medicine for the first time.

Recent advances in radiochemistry, isotope production, and biology have enabled the translation of increasingly sophisticated radiopharmaceuticals from bench to bedside. The field of targeted alpha therapy has shown substantial growth. Established beta-minus emitters such as lutetium-177 and yttrium-90 have steadily increased, and newer dual-mechanism radionuclides such as lead-212 and terbium-161 are the newer options in the therapeutic toolbox. These novel therapies go hand-in-hand with advances on the diagnostic side, with implementation of staple radionuclides such as technetium-99m, gallium-68, and fluorine-18, but also some more exotic options being investigated. At the same time, quantitative imaging, dosimetry, and radiobiology-based modelling are refining our understanding of therapeutic efficacy and safety.

This Special Issue of Pharmaceuticals invites original research papers and comprehensive reviews that highlight innovation in the field of radiotheranostics as well as ongoing challenges. Topics of interest include (but are not limited to) novel radionuclide production methods, advances in radiolabelling methods, new target discovery, and novel radiopharmaceutical development, including in vivo evaluations, clinical translation of novel diagnostic or theranostic radiopharmaceuticals, and investigations of the radiobiology governing theranostic applications. The hope is that this issue will contain contributions that showcase the state-of-the-art and inspire and inform the next generation of radiopharmaceutical innovation.

Dr. Janke Kleynhans
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. 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

  • theranostics
  • radiopharmacy
  • targeted alpha therapy
  • preclinical imaging
  • radiobiology
  • radioisotope production
  • molecular radiotherapy
  • positron emission tomography
  • single photon emission tomography

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Published Papers (2 papers)

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16 pages, 1696 KB  
Article
Evaluation of Daughter Radionuclide Release from the 103Pd/103mRh In Vivo Generator for Targeted Auger Therapy
by Aicha Nour Laouameria, Cathryn H. S. Driver, Monika Buys, Elena Sergeevna Kurakina, Mátyás Hunyadi, Jan Rijn Zeevaart and Zoltan Szucs
Pharmaceuticals 2026, 19(1), 126; https://doi.org/10.3390/ph19010126 - 11 Jan 2026
Viewed by 697
Abstract
Background/Objectives: The 103Pd/103mRh in vivo generator represents a promising Auger electron-emitting system, in which both parent and daughter radionuclides emit predominantly Auger electrons with minimal accompanying radiation. This study investigates the release dynamics of daughter radionuclides from the 103 [...] Read more.
Background/Objectives: The 103Pd/103mRh in vivo generator represents a promising Auger electron-emitting system, in which both parent and daughter radionuclides emit predominantly Auger electrons with minimal accompanying radiation. This study investigates the release dynamics of daughter radionuclides from the 103Pd/103mRh in vivo generator and evaluates the underlying mechanisms governing bond rupture and daughter retention. Methods: Cyclotron irradiation of rhodium foils was performed in two separate batches, followed by radionuclide separation using conventional wet chemistry and a novel dry distillation technique. The purified 103Pd radionuclide was used to radiolabel DOTA-TATE, phthalocyanine-TATE, and DOTA-TOC chelators. The resulting complexes were immobilized on Strata-X and Strata-C18 solid-phase extraction columns. Scheduled elution experiments were conducted to quantify the release of the 103mRh daughter radionuclide. Results: The measured 103mRh release rates were 9.8 ± 3.0% and 9.6 ± 2.7% from Strata-X columns with DOTA-TATE and phthalocyanine-TATE, respectively, and 10.5 ± 2.7% and 12.0 ± 0.5% from Strata-X and Strata-C18 columns, respectively, with DOTA-TOC. These values are significantly lower than the ~100% release predicted based on the reported Auger electron yield of 186%. One explanation for this difference could be potential inconsistencies in decay data that may require correction; this needs further investigation. The results further demonstrated that delocalized π-electrons, introduced via phthalocyanine-based chelation, did not mitigate daughter release. Conclusions: The low observed daughter nuclide release represents a favorable characteristic for the future clinical translation of the 103Pd/103mRh Auger emitter pair. The findings support the conclusion that Auger electron cascades, rather than nuclear recoil energy, dominate bond rupture processes. Full article
(This article belongs to the Special Issue Advances in Theranostic Radiopharmaceuticals)
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18 pages, 1585 KB  
Article
Affinity- and Format-Dependent Pharmacokinetics of 89Zr-Labeled Albumin-Binding VHH Constructs
by Simon Leekens, Peter Casteels, Tom Van Bogaert, Pieter Deschaght, Veronique De Brabandere, Christopher Cawthorne, Guy Bormans and Frederik Cleeren
Pharmaceuticals 2026, 19(1), 120; https://doi.org/10.3390/ph19010120 - 9 Jan 2026
Viewed by 1008
Abstract
Background/Objectives: NANOBODY® molecules (VHHs) are attractive vectors for radiopharmaceuticals due to their small size and high target affinity, but rapid clearance and pronounced kidney retention limit their therapeutic applicability. Binding to serum albumin is a widely used strategy to prolong circulation, yet [...] Read more.
Background/Objectives: NANOBODY® molecules (VHHs) are attractive vectors for radiopharmaceuticals due to their small size and high target affinity, but rapid clearance and pronounced kidney retention limit their therapeutic applicability. Binding to serum albumin is a widely used strategy to prolong circulation, yet the respective contributions of albumin-binding affinity and molecular format remain insufficiently defined. This study aimed to systematically evaluate how affinity and valency modulate VHH pharmacokinetics. Methods: Four monovalent albumin-binding VHHs spanning nanomolar to micromolar affinities and two bivalent constructs were engineered, generated by fusing an albumin-binding VHH to an irrelevant non-binding VHH. All constructs incorporated a site-specific cysteine for DFO* conjugation, enabling uniform zirconium-89 labeling with high radiochemical purity. Pharmacokinetics were assessed in healthy mice using serial blood sampling and positron emission tomography. Blood and kidney exposure were quantified by non-compartmental analysis. Results: All albumin-binding constructs showed increased systemic exposure and reduced kidney uptake relative to a non-binding control. Nanomolar-affinity binders reached maximal exposure, and further affinity increases (KD < ~100 nM) did not improve pharmacokinetics, suggesting a threshold. The micromolar binder showed intermediate exposure but still reduced renal retention compared with control. Valency effects were affinity-dependent. They were negligible at high affinity but pronounced at low affinity, where bivalency reduced systemic exposure and increased kidney uptake toward control levels. Conclusions: Albumin binding enables tuning of VHH pharmacokinetics in an affinity-dependent manner. Above an apparent affinity threshold, pharmacokinetics become format independent, whereas below this threshold, molecular format substantially influences systemic and renal disposition. Full article
(This article belongs to the Special Issue Advances in Theranostic Radiopharmaceuticals)
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