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Pharmaceutics
Special Issues
Novel Insights into Radiopharmaceutics for Cancer Therapy
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Novel Insights into Radiopharmaceutics for Cancer 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 (31 March 2022) | Viewed by 2286

Special Issue Editors

Dr. Clément Morgat

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Guest Editor
1. Department of Nuclear Medicine, University Hospital of Bordeaux, F-33000 Bordeaux, France
2. INCIA, Translational Molecular Imaging Team, University of Bordeaux, F-33000 Bordeaux, France
Interests: cancer; theranostics; PET; neuropeptides; imaging; therapy
Dr. David Kryza

E-Mail Website
Guest Editor
Laboratoire d’Automatique, de Génie des Procédés et de Génie Pharmaceutique, Université Claude Bernard Lyon 1, CNRS UMR 5007, 43 bd 11 Novembre 1918, 69622 Villeurbanne, France
Interests: cancer; theranostics; Mabs; nanoparticles;radiopharmaceuticals

Special Issue Information

Dear Colleagues,

Targeted radionuclide therapy (TRT) has reached the culmination of translational research with the pivotal NETTER and VISION trials. Patients suffering from metastatic neuroendocrine tumors and metastatic prostate cancer tumors now benefit from this new treatment modality in our departments. However, we should continue and intensify preclinical and clinical research to determine the best place of TRT throughout the various progressive stages of cancer. We should also focus our efforts on deciphering treatment resistance and recurrence mechanisms but also testing novel combinations and dose regimens for targeted radio-/immuno-/chemotherapies. Finally, the design of novel radiopharmaceuticals armed with innovative radionuclides for TRT or for pretherapeutic imaging or radiopharmaceuticals targeting novel molecular signatures of cancer cells might expand the applications of TRT to diseases not currently eligible for TRT and would increase the efficacy of TRT.

This Special Issue of Pharmaceutics welcomes articles (original research, review, and short communication) on the production and use of novel radionuclides for cancer imaging and therapy, and the design and (pre)clinical evaluation of novel radiopharmaceuticals, along with new strategies to improve the efficacy of TRT.

Dr. Clément Morgat
Dr. David Kryza
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
  • targeted radionuclide therapy
  • cancer
  • imaging
  • theranostics

Published Papers (1 paper)

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Research

16 pages, 2386 KiB  
Article
In Vitro Biological Evaluation of Aprepitant Based 177Lu-Radioconjugates
by Paweł K. Halik, Przemysław Koźmiński, Joanna Matalińska, Piotr F. J. Lipiński, Aleksandra Misicka and Ewa Gniazdowska
Pharmaceutics 2022, 14(3), 607; https://doi.org/10.3390/pharmaceutics14030607 - 10 Mar 2022
Cited by 6 | Viewed by 1829
Abstract
Currently, the search for promising NK1R-positive tumor-targeting radiopharmaceuticals based on the structure of small molecular antagonists of neurokinin-1 receptor can be observed. Following this trend, we continued our evaluation of aprepitant-based 177Lu-radioconjugates in terms of future oncological applications. For this purpose, three [...] Read more.
Currently, the search for promising NK1R-positive tumor-targeting radiopharmaceuticals based on the structure of small molecular antagonists of neurokinin-1 receptor can be observed. Following this trend, we continued our evaluation of aprepitant-based 177Lu-radioconjugates in terms of future oncological applications. For this purpose, three novel aprepitant homologues were synthesized to broaden the previously obtained derivative portfolio, functionalized with the DOTA chelator and labeled with 68Ga and 177Lu. The newly evaluated radioconjugates showed the intended significant increase in lipophilicity compared to the previous ones, while maintaining stability in the human serum. Then, in a receptor binding study to the human NK1 receptor, we compared the two series of 177Lu-radioconjugates of aprepitant with each other and with the reference Substance P derivative currently used in glioblastoma therapy, clearly indicating the high affinity and better binding capacity of the novel radioconjugates. The in vitro experimental results included in the presented study, supported by labeling optimization, radioconjugate characterization and docking modeling of new aprepitant-derived radioagents, confirm our assumptions about the usefulness of aprepitant as a NK1R targeting vector and point out the perspectives for the forthcoming first in vivo trials. Full article
(This article belongs to the Special Issue Novel Insights into Radiopharmaceutics for Cancer Therapy)
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