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Pharmaceutics
Special Issues
Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy
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Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Clinical Pharmaceutics".

Deadline for manuscript submissions: 31 August 2024 | Viewed by 2081

Special Issue Editors

Dr. Kuan Hu

E-Mail Website
Guest Editor
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
Interests: radiopharmaceuticals; peptide; PET imaging; radiotheranostics; cancer management
Dr. Volkan Tekin

E-Mail Website
Guest Editor
Department of Radiology, University of Alabama at Birmingham, Birmingham, AL, USA
Interests: cancer research; radiopharmaceuticals; cell culture; nanoparticles

Special Issue Information

Dear Colleagues,

Radiopharmaceutical therapy targets tumor- or nontumor-associated tissues to deliver a single or pair of radioactive atoms based on the location and/or the properties of the tissues. The variety of the ligands, such as protein, peptide, antibody, and nucleic acid, to be selected depending on the radioactive atom and the target tissue facilitates the targeting of many tissues, while the variety of radioactive atoms in terms of energy type, density, and the half-life ensures the destruction of the target tissues and effective treatment of many diseases with radiotherapy. Although the focus of radiopharmaceutical therapy is cancer treatment, it is known that it has a potential for use in the treatment of other diseases.

This Special Issue serves to highlight the potential of ligands and radioactive atoms to treat diseases by novel approaches or combining the current methods with a synergy of aspects. We invite authors to submit articles which focus on discovering the pathways of radiopharmaceuticals for disease therapy for this Special Issue.

Dr. Kuan Hu
Dr. Volkan Tekin
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

  • radiopharmaceutical
  • radionuclide therapy
  • radiotherapy
  • cancer treatment
  • imaging-guided therapy
  • radiotheranostics
  • nontumor diseases
  • alpha radiotherapy
  • disease treatment
  • therapy

Published Papers (2 papers)

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Research

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16 pages, 3519 KiB  
Article
GRPR-Antagonists Carrying DOTAGA-Chelator via Positively Charged Linkers: Perspectives for Prostate Cancer Theranostics
by Karim Obeid, Panagiotis Kanellopoulos, Ayman Abouzayed, Adam Mattsson, Vladimir Tolmachev, Berthold A. Nock, Theodosia Maina and Anna Orlova
Pharmaceutics 2024, 16(4), 513; https://doi.org/10.3390/pharmaceutics16040513 - 08 Apr 2024
Viewed by 588
Abstract
Gastrin-releasing peptide receptor (GRPR)-antagonists have served as motifs in the development of theranostic radioligands for prostate cancer. Our efforts have been focused on the development of radiolabeled RM26 (H-DPhe6–Gln7–Trp8–Ala9–Val10–Gly11–His12–Sta [...] Read more.
Gastrin-releasing peptide receptor (GRPR)-antagonists have served as motifs in the development of theranostic radioligands for prostate cancer. Our efforts have been focused on the development of radiolabeled RM26 (H-DPhe6–Gln7–Trp8–Ala9–Val10–Gly11–His12–Sta13–Leu14–NH2) analogs, such as [111In]In-DOTAGA-PEG2-RM26. We recently showed that its Gly11/Sar11-substituted version, [111In]In-AU-RM26-M1, resisted degradation by neprilysin (NEP) while in circulation and achieved higher tumor uptake in mice. We herein introduce the following three new AU-RM26-M1 mimics labeled with In-111, with basic residues in the linker: (i) AU-RM26-M2 (PEG2-Pip), (ii) AU-RM26-M3 (PEG2-Arg), and (iii) AU-RM26-M4 (Arg-Arg-Pip). These analogs were compared in PC-3 cells and animal models vs. AU-RM26-M1 (reference). The new analogs showed high affinity and specificity for the GRPR, exhibiting an uptake and distribution pattern in PC-3 cells typical for a radiolabeled GRPR-antagonist. They showed high stability in peripheral mice blood, except for [111In]In-AU-RM26-M3. AU-RM26-M4 achieved the highest tumor uptake and promising background clearance, followed by [111In]In-RM26-M2, showing lower background levels. These findings were confirmed for [111In]In-AU-RM26-M2 and [111In]In-AU-RM26-M4 by micro-SPECT/CT at 4 and 24 h post-injection. Hence, the type of positively charged residues in the linker of AU-RM26-M1 mimics strongly influenced biological behavior. The analogs with Pip next to DPhe6 demonstrated the best overall characteristics and warrant further investigation. Full article
(This article belongs to the Special Issue Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy)
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Review

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24 pages, 3843 KiB  
Review
Beyond Small Molecules: Antibodies and Peptides for Fibroblast Activation Protein Targeting Radiopharmaceuticals
by Xiaona Sun, Yuxuan Wu, Xingkai Wang, Xin Gao, Siqi Zhang, Zhicheng Sun, Ruping Liu and Kuan Hu
Pharmaceutics 2024, 16(3), 345; https://doi.org/10.3390/pharmaceutics16030345 - 29 Feb 2024
Viewed by 1199
Abstract
Fibroblast activation protein (FAP) is a serine protease characterized by its high expression in cancer-associated fibroblasts (CAFs) and near absence in adult normal tissues and benign lesions. This unique expression pattern positions FAP as a prospective biomarker for targeted tumor radiodiagnosis and therapy. [...] Read more.
Fibroblast activation protein (FAP) is a serine protease characterized by its high expression in cancer-associated fibroblasts (CAFs) and near absence in adult normal tissues and benign lesions. This unique expression pattern positions FAP as a prospective biomarker for targeted tumor radiodiagnosis and therapy. The advent of FAP-based radiotheranostics is anticipated to revolutionize cancer management. Among various types of FAP ligands, peptides and antibodies have shown advantages over small molecules, exemplifying prolonged tumor retention in human volunteers. Within its scope, this review summarizes the recent research progress of the FAP radiopharmaceuticals based on antibodies and peptides in tumor imaging and therapy. Additionally, it incorporates insights from recent studies, providing valuable perspectives on the clinical utility of FAP-targeted radiopharmaceuticals. Full article
(This article belongs to the Special Issue Advances in Radiopharmaceuticals for Disease Diagnoses and Therapy)
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