Advances in the Development and Application of Targeted Radiopharmaceuticals for Cancer Management, 2nd Edition

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 August 2023) | Viewed by 7941

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Guest Editor
Department of Radiology & Nuclear Medicine, Erasmus University Medical Center, Rotterdam, The Netherlands
Interests: breast cancer; prostate cancer; nuclear imaging and therapy; targeted therapy; molecular and cell biology; cancer diagnostics
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Special Issue Information

Dear Colleagues,

In the past decades, the development and application of targeted radiopharmaceuticals for the imaging and treatment of cancer have been an emerging area of research, not only in the field of nuclear medicine but also in that of cancer research in general. In the late 1980s–early 1990s, the first successful preclinical and clinical studies were performed with a targeted radiopharmaceutical. Following this success, a broad range of targeted radiopharmaceuticals directed against different cancer types have been developed. Over time, many research breakthroughs occurred, which led to the improvement of targeted radiopharmaceuticals and their application. As a result of these breakthroughs, a radiopharmaceutical was recently EMA- and FDA-approved for the treatment of neuroendocrine tumours. Despite the major advances in the development of radiopharmaceuticals that have been made over the years, there is still room for improvement. This Special Issue of Pharmaceutics will focus on novel advances in the development of radiopharmaceuticals for cancer imaging and therapy. This includes, but is not limited to, studies on the production and use of novel radionuclides, the development and application of new radiotracers, and the application of advanced strategies to improve radiopharmaceuticals’ pharmacokinetics. Short communications, original research papers, and reviews are welcome.

Dr. Simone U. Dalm
Guest Editor

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Keywords

  • radiopharmaceuticals
  • theranostics
  • imaging
  • treatment
  • radionuclides
  • cancer
  • radiochemistry
  • dosimetry
  • in vitro and in vivo studies
  • clinical studies
  • molecular biology
  • safety
  • toxicity

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Published Papers (2 papers)

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Review

26 pages, 2661 KiB  
Review
DNA Damage by Radiopharmaceuticals and Mechanisms of Cellular Repair
by Yousef Khazaei Monfared, Pedram Heidari, Samuel J. Klempner, Umar Mahmood, Aparna R. Parikh, Theodore S. Hong, Matthew R. Strickland and Shadi A. Esfahani
Pharmaceutics 2023, 15(12), 2761; https://doi.org/10.3390/pharmaceutics15122761 - 12 Dec 2023
Cited by 5 | Viewed by 2734
Abstract
DNA is an organic molecule that is highly vulnerable to chemical alterations and breaks caused by both internal and external factors. Cells possess complex and advanced mechanisms, including DNA repair, damage tolerance, cell cycle checkpoints, and cell death pathways, which together minimize the [...] Read more.
DNA is an organic molecule that is highly vulnerable to chemical alterations and breaks caused by both internal and external factors. Cells possess complex and advanced mechanisms, including DNA repair, damage tolerance, cell cycle checkpoints, and cell death pathways, which together minimize the potentially harmful effects of DNA damage. However, in cancer cells, the normal DNA damage tolerance and response processes are disrupted or deregulated. This results in increased mutagenesis and genomic instability within the cancer cells, a known driver of cancer progression and therapeutic resistance. On the other hand, the inherent instability of the genome in rapidly dividing cancer cells can be exploited as a tool to kill by imposing DNA damage with radiopharmaceuticals. As the field of targeted radiopharmaceutical therapy (RPT) is rapidly growing in oncology, it is crucial to have a deep understanding of the impact of systemic radiation delivery by radiopharmaceuticals on the DNA of tumors and healthy tissues. The distribution and activation of DNA damage and repair pathways caused by RPT can be different based on the characteristics of the radioisotope and molecular target. Here we provide a comprehensive discussion of the biological effects of RPTs, with the main focus on the role of varying radioisotopes in inducing direct and indirect DNA damage and activating DNA repair pathways. Full article
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22 pages, 2832 KiB  
Review
Safety and Therapeutic Optimization of Lutetium-177 Based Radiopharmaceuticals
by Typhanie Ladrière, Julie Faudemer, Elise Levigoureux, Damien Peyronnet, Cédric Desmonts and Jonathan Vigne
Pharmaceutics 2023, 15(4), 1240; https://doi.org/10.3390/pharmaceutics15041240 - 13 Apr 2023
Cited by 5 | Viewed by 4853
Abstract
Peptide receptor radionuclide therapy (PRRT) using Lutetium-177 (177Lu) based radiopharmaceuticals has emerged as a therapeutic area in the field of nuclear medicine and oncology, allowing for personalized medicine. Since the first market authorization in 2018 of [¹⁷⁷Lu]Lu-DOTATATE (Lutathera®) targeting somatostatin receptor [...] Read more.
Peptide receptor radionuclide therapy (PRRT) using Lutetium-177 (177Lu) based radiopharmaceuticals has emerged as a therapeutic area in the field of nuclear medicine and oncology, allowing for personalized medicine. Since the first market authorization in 2018 of [¹⁷⁷Lu]Lu-DOTATATE (Lutathera®) targeting somatostatin receptor type 2 in the treatment of gastroenteropancreatic neuroendocrine tumors, intensive research has led to transfer innovative 177Lu containing pharmaceuticals to the clinic. Recently, a second market authorization in the field was obtained for [¹⁷⁷Lu]Lu-PSMA-617 (Pluvicto®) in the treatment of prostate cancer. The efficacy of 177Lu radiopharmaceuticals are now quite well-reported and data on the safety and management of patients are needed. This review will focus on several clinically tested and reported tailored approaches to enhance the risk–benefit trade-off of radioligand therapy. The aim is to help clinicians and nuclear medicine staff set up safe and optimized procedures using the approved 177Lu based radiopharmaceuticals. Full article
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