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Pharmaceutics
Special Issues
Promising Radiopharmaceuticals in Oncological Therapy
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Promising Radiopharmaceuticals in Oncological Therapy

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Drug Targeting and Design".

Deadline for manuscript submissions: closed (29 February 2024) | Viewed by 4543

Special Issue Editors

Dr. György Trencsényi

E-Mail Website
Guest Editor
Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, H-4032 Debrecen, Hungary
Interests: experimental oncology; in vivo tumor models; molecular imaging with SPECT/PET radiotarcers; translationsal research
Special Issues, Collections and Topics in MDPI journals
Dr. Képes Zita

E-Mail Website
Guest Editor
Division of Nuclear Medicine and Translational Imaging, Department of Medical Imaging, Faculty of Medicine, University of Debrecen, Nagyerdei St. 98, 4032 Debrecen, Hungary
Interests: experimental oncology (in vitro and in vivo); preclinical tumor models; glucose transport and glucose metabolism in tumor cells; development and biological application of PET (positron emission tomography) radiopharmaceuticals; functional imaging with PET technique

Special Issue Information

Dear Colleagues,

Targeted radionuclide therapy (TAT), which involves applying tumor-specific biomolecules capable of selective radioisotope delivery to neoplastic sites, is a field that has been exhaustively investigated in current oncological research. The establishment of α- or β-emitting therapeutic radiopharmaceuticals seems alluring due to their inherent ability to reach substantial radioactive concentration and related radiotoxicity directly at the intended site without significant collateral damage to nearby healthy tissues and organs.

Using preclinical tumor models, nuclear medical imaging modalities, including SPECT or PET, provide a unique opportunity to explore the therapeutic gains of de novo constructed radiotracers in real-time, on a molecular level, and even in a quantitative way. In addition, the replacement of the therapeutic isotope with its diagnostic sister allows for the use of theranostic agents that enable a multi-tasking approach to targeted drug delivery and in vivo molecular imaging.

Since therapeutic radiopharmaceuticals have already shown promising results in a cluster of malignant diseases at both the preclinical and clinical level, we expect to see more radioprobes designed for therapeutic or theranostic purposes in the foreseeable future.

This Pharmaceutics Special Issue, entitled “Promising Radiopharmaceuticals in Oncological Therapy”, will collate  manuscripts that present the recent preclinical advances regarding therapeutic radiopharmaceuticals or theranostic agents designed for targeted cancer therapy, as well as those present future perspectives on these topics. Submissions of original research articles and reviews that aim to uncover open questions regarding targeted radionuclide therapy are also welcome. Research areas may include (but are not limited to) the following: novel molecular targets for cancer treatment, radiolabeled anti-angiogenesis molecules, radiopharmaceutical development, innovative radiopharmaceuticals, therapeutic radioisotopes, radiosynthesis, dosimetry, the mechanism of action of therapeutic radiotracers, and the application and design of theranostics. 

We look forward to receiving your contributions.

Dr. György Trencsényi
Dr. Zita Képes
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 100 words) can be sent to the Editorial Office for announcement on this website.

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. Pharmaceutics 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

  • targeted radiotherapy
  • radioisotopes
  • tumor-specific molecular targets
  • tumor-selective radiopharmaceuticals
  • preclinical level
  • positron emission tomography (PET)
  • single-photon emission computed tomography (SPECT)
  • theranostics
  • in vivo tumor models
  • translational research

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Published Papers (2 papers)

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Research

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13 pages, 1541 KiB  
Article
Synthesis of Novel, Dual-Targeting 68Ga-NODAGA-LacN-E[c(RGDfK)]2 Glycopeptide as a PET Imaging Agent for Cancer Diagnosis
by Barbara Gyuricza, Judit P. Szabó, Viktória Arató, Dániel Szücs, Adrienn Vágner, Dezső Szikra and Anikó Fekete
Pharmaceutics 2021, 13(6), 796; https://doi.org/10.3390/pharmaceutics13060796 - 26 May 2021
Cited by 6 | Viewed by 2718
Abstract
Radiolabeled peptides possessing an Arg-Gly-Asp (RGD) motif are widely used radiopharmaceuticals for PET imaging of tumor angiogenesis due to their high affinity and selectivity to αvβ3 integrin. This receptor is overexpressed in tumor and tumor endothelial cells in the case [...] Read more.
Radiolabeled peptides possessing an Arg-Gly-Asp (RGD) motif are widely used radiopharmaceuticals for PET imaging of tumor angiogenesis due to their high affinity and selectivity to αvβ3 integrin. This receptor is overexpressed in tumor and tumor endothelial cells in the case of numerous cancer cell lines, therefore, it is an excellent biomarker for cancer diagnosis. The galectin-3 protein is also highly expressed in tumor cells and N-acetyllactosamine is a well-established ligand of this receptor. We have developed a synthetic method to prepare a lactosamine-containing radiotracer, namely 68Ga-NODAGA-LacN-E[c(RGDfK)]2, for cancer diagnosis. First, a lactosamine derivative with azido-propyl aglycone was synthetized. Then, NODAGA-NHS was attached to the amino group of this lactosamine derivative. The obtained compound was conjugated to an E[c(RGDfK)]2 peptide with a strain-promoted click reaction. We have accomplished the radiolabeling of the synthetized NODAGA-LacN-E[c(RGDfK)]2 precursor with a positron-emitting 68Ga isotope (radiochemical yield of >95%). The purification of the labeled compound with solid-phase extraction resulted in a radiochemical purity of >99%. Subsequently, the octanol–water partition coefficient (log P) of the labeled complex was determined to be −2.58. In addition, the in vitro stability of 68Ga-NODAGA-LacN-E[c(RGDfK)]2 was investigated and it was found that it was stable under the examined conditions. Full article
(This article belongs to the Special Issue Promising Radiopharmaceuticals in Oncological Therapy)
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Review

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29 pages, 3024 KiB  
Review
Zirconium 89 and Copper 64 for ImmunoPET: From Antibody Bioconjugation and Radiolabeling to Molecular Imaging
by Laure Badier and Isabelle Quelven
Pharmaceutics 2024, 16(7), 882; https://doi.org/10.3390/pharmaceutics16070882 - 30 Jun 2024
Viewed by 1355
Abstract
Immunotherapy has transformed cancer treatment. Nevertheless, given the heterogeneity of clinical efficacy, the multiplicity of treatment options available and the possibility of serious adverse effects, selecting the most effective treatment has become the greatest challenge. Molecular imaging offers an attractive way for this [...] Read more.
Immunotherapy has transformed cancer treatment. Nevertheless, given the heterogeneity of clinical efficacy, the multiplicity of treatment options available and the possibility of serious adverse effects, selecting the most effective treatment has become the greatest challenge. Molecular imaging offers an attractive way for this purpose. ImmunoPET provides specific imaging with positron emission tomography (PET) using monoclonal antibodies (mAb) or its fragments as vector. By combining the high targeting specificity of mAb and the sensitivity of PET technique, immunoPET could noninvasively and dynamically reveal tumor antigens expression and provide theranostic tools of several types of malignancies. Because of their slow kinetics, mAbs require radioelements defined by a consistent half-life. Zirconium 89 (89Zr) and Copper 64 (64Cu) are radiometals with half-lives suitable for mAb labeling. Radiolabeling with a radiometal requires the prior use of a bifunctional chelate agent (BFCA) to functionalize mAb for radiometal chelation, in a second step. There are a number of BFCA available and much research is focused on antibody functionalization techniques or on developing the optimum chelating agent depending the selected radiometal. In this manuscript, we present a critical account of radiochemical techniques with radionuclides 89Zr and 64Cu and their applications in preclinical and clinical immuno-PET imaging. Full article
(This article belongs to the Special Issue Promising Radiopharmaceuticals in Oncological Therapy)
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