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Pharmaceutics
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Research on Radiotracers and Novel Radiopharmaceuticals for Cancer Therapy and...
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Research on Radiotracers and Novel Radiopharmaceuticals for Cancer Therapy and Diagnosis

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

Deadline for manuscript submissions: 10 August 2024 | Viewed by 3749

Special Issue Editors

Prof. Dr. Wei Lu

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Guest Editor
School of Pharmacy, Fudan University, Shanghai 201203, China
Interests: drug delivery systems; vaccine delivery; nanomedicine in cancer radiotherapy, chemotherapy and immunotherapy; theranostics
Dr. Panagiotis Kanellopoulos

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Guest Editor
Department of Medicinal Chemistry, Uppsala University, Uppsala, Sweeden
Interests: radiopharmaceuticals; radiopeptides; radiopharmacy; preclinical evaluation; theranostics
Dr. Antonio Shegani

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Guest Editor
Institute of Nuclear and Radiological Sciences and Technology, Energy & Safety, NCSR “Demokritos”, 15310 Athens, Greece
Interests: molecular imaging; radiopharmaceuticals; radiochemistry; theranostics

Special Issue Information

Dear Colleagues,

It is commonly accepted that cancer is amongst the most prominent health issues arising from the increasing life expectancy worldwide. Great progress has been made over the years concerning both the diagnosis and treatment of cancer. In the last decade, nuclear medicine has made an undeniable contribution to clinical oncology, as new radiopharmaceuticals aimed at diagnosis or therapy (theranostics) have been developed. First with the radiolabelled somatostatin analogues approved by FDA/EMA and then with the implementation of PSMA inhibitors, a new era of clinically useful radiopharmaceuticals in personalized medicine has been paved. The introduction of novel molecular targets, both on cancer cells and in the malignancy microenvironment, is providing exciting new opportunities for radiopharmaceutical development.

In the hope of reviewing these efforts, we are pleased to invite you to share your results in this Special Issue titled “Research on Radiotracers and Novel Radiopharmaceuticals for Cancer Therapy and Diagnosis”. Original articles and reviews on radiopharmaceutical development, novel approaches to improving their performance, new cancer models for preclinical evaluation and clinical translation studies are most welcome.

Prof. Dr. Wei Lu
Dr. Panagiotis Kanellopoulos
Dr. Antonio Shegani
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

  • radiopharmaceuticals
  • cancer therapy
  • preclinical evaluation
  • theranostics
  • tumour targeting
  • imaging
  • PET
  • SPECT

Published Papers (3 papers)

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Research

17 pages, 7482 KiB  
Article
Synthesis, Radiolabeling, and Biodistribution Study of a Novel DOTA-Peptide for Targeting Vascular Endothelial Growth Factor Receptors in the Molecular Imaging of Breast Cancer
by Fatemeh Ebrahimi, Nooshin Reisi Zargari, Mehdi Akhlaghi, S. Mohsen Asghari, Khosrou Abdi, Saeed Balalaie, Mahboobeh Asadi and Davood Beiki
Pharmaceutics 2024, 16(7), 899; https://doi.org/10.3390/pharmaceutics16070899 - 4 Jul 2024
Viewed by 684
Abstract
As angiogenesis plays a pivotal role in tumor progression and metastasis, leading to more cancer-related deaths, the angiogenic process can be considered as a target for diagnostic and therapeutic applications. The vascular endothelial growth factor receptor-1 (VEGR-1) and VEGFR-2 have high expression on [...] Read more.
As angiogenesis plays a pivotal role in tumor progression and metastasis, leading to more cancer-related deaths, the angiogenic process can be considered as a target for diagnostic and therapeutic applications. The vascular endothelial growth factor receptor-1 (VEGR-1) and VEGFR-2 have high expression on breast cancer cells and contribute to angiogenesis and tumor development. Thus, early diagnosis through VEGFR-1/2 detection is an excellent strategy that can significantly increase a patient’s chance of survival. In this study, the VEGFR1/2-targeting peptide VGB3 was conjugated with 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA), using 6-aminohexanoic acid (Ahx) as a spacer to prevent steric hindrance in binding. DOTA-Ahx-VGB3 was radiolabeled with Gallium-68 (68Ga) efficiently. An in vitro cell binding assay was assessed in the 4T1 cell line. The tumor-targeting potential of [68Ga]Ga-DOTA-Ahx-VGB3 was conducted for 4T1 tumor-bearing mice. Consequently, high radiochemical purity [68Ga]Ga-DOTA-Ahx-VGB3 (RCP = 98%) was prepared and stabilized in different buffer systems. Approximately 17% of the radiopeptide was internalized after 2 h incubation and receptor binding as characterized by the IC50 value being about 867 nM. The biodistribution and PET/CT studies revealed that [68Ga]Ga-DOTA-Ahx-VGB3 reached the tumor site and was excreted rapidly by the renal system. These features convey [68Ga]Ga-DOTA-Ahx-VGB3 as a suitable agent for the noninvasive visualization of VEGFR-1/2 expression. Full article
(This article belongs to the Special Issue Research on Radiotracers and Novel Radiopharmaceuticals for Cancer Therapy and Diagnosis)
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14 pages, 2998 KiB  
Article
Evaluation of Approaches for the Assessment of HER2 Expression in Breast Cancer by Radionuclide Imaging Using the Scaffold Protein [99mTc]Tc-ADAPT6
by Olga Bragina, Liubov Tashireva, Dmitriy Loos, Vladimir Chernov, Sophia Hober and Vladimir Tolmachev
Pharmaceutics 2024, 16(4), 445; https://doi.org/10.3390/pharmaceutics16040445 - 23 Mar 2024
Viewed by 1214
Abstract
Due to its small size and high affinity binding, the engineered scaffold protein ADAPT6 is a promising targeting probe for radionuclide imaging of human epidermal growth factor receptor type 2 (HER2). In a Phase I clinical trial, [99mTc]Tc-ADAPT6 demonstrated safety, tolerability [...] Read more.
Due to its small size and high affinity binding, the engineered scaffold protein ADAPT6 is a promising targeting probe for radionuclide imaging of human epidermal growth factor receptor type 2 (HER2). In a Phase I clinical trial, [99mTc]Tc-ADAPT6 demonstrated safety, tolerability and capacity to visualize HER2 expression in primary breast cancer. In this study, we aimed to select the optimal parameters for distinguishing between breast cancers with high and low expression of HER2 using [99mTc]Tc-ADAPT6 in a planned Phase II study. HER2 expression was evaluated in primary tumours and metastatic axillary lymph nodes (mALNs). SPECT/CT imaging of twenty treatment-naive breast cancer patients was performed 2 h after injection of [99mTc]Tc-ADAPT6. The imaging data were compared with the data concerning HER2 expression obtained by immunohistochemical evaluation of samples obtained by core biopsy. Maximum Standard Uptake Values (SUVmax) afforded the best performance for both primary tumours and mALNs (areas under the receiver operating characteristic curve (ROC AUC) of 1.0 and 0.97, respectively). Lesion-to-spleen ratios provided somewhat lower performance. However, the ROC AUCs were still over 0.90 for both primary tumours and mALNs. Thus, lesion-to-spleen ratios should be further evaluated to find if these could be applied to imaging using stand-alone SPECT cameras that do not permit SUV calculations. Full article
(This article belongs to the Special Issue Research on Radiotracers and Novel Radiopharmaceuticals for Cancer Therapy and Diagnosis)
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20 pages, 2079 KiB  
Article
Amide-to-Triazole Switch in Somatostatin-14-Based Radioligands: Impact on Receptor Affinity and In Vivo Stability
by Xabier Guarrochena, Panagiotis Kanellopoulos, Anna Stingeder, Lisa-Maria Rečnik, Irene V. J. Feiner, Marie Brandt, Wolfgang Kandioller, Theodosia Maina, Berthold A. Nock and Thomas L. Mindt
Pharmaceutics 2024, 16(3), 392; https://doi.org/10.3390/pharmaceutics16030392 - 13 Mar 2024
Viewed by 1228
Abstract
The use of metabolically stabilized, radiolabeled somatostatin (SST) analogs ([68Ga]Ga/[177Lu]Lu-DOTA-TATE/TOC/NOC) is well established in nuclear medicine. Despite the pivotal role of these radioligands in the diagnosis and therapy of neuroendocrine tumors (NETs), their inability to interact with all five [...] Read more.
The use of metabolically stabilized, radiolabeled somatostatin (SST) analogs ([68Ga]Ga/[177Lu]Lu-DOTA-TATE/TOC/NOC) is well established in nuclear medicine. Despite the pivotal role of these radioligands in the diagnosis and therapy of neuroendocrine tumors (NETs), their inability to interact with all five somatostatin receptors (SST1–5R) limits their clinical potential. [111In]In-AT2S is a radiolabeled DOTA-conjugate derived from the parent peptide SST-14 that exhibits high binding affinity to all SSTR subtypes, but its poor metabolic stability represents a serious disadvantage for clinical use. In order to address this issue, we have replaced strategic trans-amide bonds of [111In]In-AT2S with metabolically stable 1,4-disubstituted 1,2,3-triazole bioisosteres. From the five cyclic triazolo-peptidomimetics investigated, only [111In]In-XG1 combined a preserved nanomolar affinity for the SST1,2,3,5R subtypes in vitro and an improved stability in vivo (up to 17% of intact peptide 5 min postinjection (pi) versus 6% for [111In]In-AT2S). The involvement of neprilysin (NEP) in the metabolism of [111In]In-XG1 was confirmed by coadministration of Entresto®, a registered antihypertensive drug, in vivo releasing the selective and potent NEP-inhibitor sacubitrilat. A pilot SPECT/CT imaging study conducted in mice bearing hSST2R-positive xenografts failed to visualize the xenografts due to the pronounced kidney uptake (>200% injected activity (IA)/g at 4 h pi), likely the result of the formation of cationic metabolites. To corroborate the imaging data, the tumors and the kidneys were excised and analyzed with a γ-counter. Even if receptor-specific tumor uptake for [111In]In-XG1 could be confirmed (1.61% IA/g), further optimization is required to improve its pharmacokinetic properties for radiotracer development. Full article
(This article belongs to the Special Issue Research on Radiotracers and Novel Radiopharmaceuticals for Cancer Therapy and Diagnosis)
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