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Pharmaceuticals
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Feature Reviews in Radiopharmaceutical Sciences: Highlights of Two-Decade Development
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Feature Reviews in Radiopharmaceutical Sciences: Highlights of Two-Decade Development

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Radiopharmaceutical Sciences".

Deadline for manuscript submissions: closed (15 September 2023) | Viewed by 15991

Special Issue Editors

Dr. Irina Velikyan

E-Mail Website
Guest Editor
Department of Surgical Science, Uppsala University, 751 85 Uppsala, Sweden
Interests: nuclear medicine; radiochemistry; positron emission tomography; molecular imaging; radiopharmaceutical sciences; cancer; diabetes; fibrosis; drug development; inflammation
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Klaus Kopka

E-Mail Website
Guest Editor
Helmholtz-Zentrum Dresden-Rossendorf (HZDR), Institute of Radiopharmaceutical Cancer Research, 01328 Dresden, Germany
Interests: radiopharmaceutical drug development; radiopharmaceutical sciences; medicinal radiochemistry; radionuclide theranostics; targeted endoradiotherapy; noninvasive molecular imaging; PET; SPECT
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Nuclear medicine with radiopharmaceutical development as a core has progressed and expanded considerably during the last two decades. Distinct areas of development and application of the radiopharmaceuticals have been outlined. This special issue is devoted to a series of review articles covering various aspects of radiopharmaceutical development and areas of their clinical applications. 

The radiopharmaceuticals are developed for the diagnosis and therapy of various diseases on the molecular level. They can be designed for targeted and pre-targeted imaging and endoradiotherapy as well as non-targeted imaging. The utilization of nuclear medicine techniques for the management of oncological, neurological, cardiological, inflammatory, diabetic, and infectious diseases has considerably expanded during the last two decades. The individualized diagnosis and therapy are becoming a standard in patient care with the most prominent example of the selection of oncological patients for peptide receptor radionuclide therapy, treatment planning and follow-up.

The development of radiopharmaceuticals is a complex process requiring identification of disease biomarkers and respective lead compounds to be modified by medicinal (radio)chemistry; production of clinically relevant radionuclides; radiolabeling of aforementioned modified lead compounds; chemical and pre-clinical evaluation of the resulting radiopharmaceuticals towards first in-human studies and prospective clinical trials. The chemical classes of the radiopharmaceuticals span from small molecules to the largest biomolecules and particles. The exploration and introduction of radionuclides not yet clinically available is also growing extensively.  

Considerable evolution in all aspects of radiopharmaceutical sciences and application has been boosted during the last two decades through marketing approval of several diagnostic, therapeutic, and theranostic radiopharmaceuticals. Therefore, the initiative to publish a special issue comprising review articles has been taken within the journal “Pharmaceuticals” wherein researchers are invited to share their abundant knowledge, expertise, experience, and ideas. The review articles are to focus and highlight the advancement achieved in:

  • Radionuclides for nuclear medicine techniques including Positron Emission Tomography (PET), Single-Photon Emission Computed Tomography (SPECT), and endoradiotherapy/molecular radiotherapy. 
  • Chemical classes of the radiopharmaceuticals spanning from small molecules via peptides and peptidomimetics to the largest biomolecules and particles. 
  • Diagnostic and therapeutic radiopharmaceuticals for the management of oncological, neurological, cardiological, inflammatory, diabetic, and infectious diseases.

Submissions to the Special Issue need to include a cover letter stating the novelty of the review article in comparison to related reviews published in the literature. A 20% discount will be applied to the Article Processing Charges (APCs).

Dr. Irina Velikyan
Prof. Dr. Klaus Kopka
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. Pharmaceuticals 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

  • nuclear medicine
  • positron emission tomography
  • single photon emission tomography
  • endoradiotherapy
  • (radionuclide)theranostics
  • personalized medicine
  • radionuclides
  • radiopharmaceuticals
  • cancer
  • diabetes
  • fibrosis
  • inflammation
  • infection
  • neurology
  • heart disease
  • drug development
  • tracers for oncological, cardiological, and neurological Nuclear Medicine
  • tracers for infection and inflammation, theranostic tracers/radiopharmaceuticals
  • emerging theranostic radionuclides and their upscaling
  • PET/CT, PET/MRI, SPECT/CT, optical imaging including fluorescent dye conjugates for image guided surgery, Can we transfer the theranostic concept to the tumor microenvironment
  • radiohalogenation methods for fluorine, bromine, iodine, astatine
  • radiometalation methods
  • emerging complexing agents for radiometalation
  • emerging theranostic biological targets
  • imaging biomarkers for non-invasive imaging
  • providing the radioindicator concept for drug development
  • tracers for distinct diseases

Published Papers (7 papers)

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31 pages, 9977 KiB  
Review
Towards the Magic Radioactive Bullet: Improving Targeted Radionuclide Therapy by Reducing the Renal Retention of Radioligands
by Kim E. de Roode, Lieke Joosten and Martin Behe
Pharmaceuticals 2024, 17(2), 256; https://doi.org/10.3390/ph17020256 - 16 Feb 2024
Cited by 1 | Viewed by 1634
Abstract
Targeted radionuclide therapy (TRT) is an emerging field and has the potential to become a major pillar in effective cancer treatment. Several pharmaceuticals are already in routine use for treating cancer, and there is still a high potential for new compounds for this [...] Read more.
Targeted radionuclide therapy (TRT) is an emerging field and has the potential to become a major pillar in effective cancer treatment. Several pharmaceuticals are already in routine use for treating cancer, and there is still a high potential for new compounds for this application. But, a major issue for many radiolabeled low-to-moderate-molecular-weight molecules is their clearance via the kidneys and their subsequent reuptake. High renal accumulation of radioactive compounds may lead to nephrotoxicity, and therefore, the kidneys are often the dose-limiting organs in TRT with these radioligands. Over the years, different strategies have been developed aiming for reduced kidney retention and enhanced therapeutic efficacy of radioligands. In this review, we will give an overview of the efforts and achievements of the used strategies, with focus on the therapeutic potential of low-to-moderate-molecular-weight molecules. Among the strategies discussed here is coadministration of compounds that compete for binding to the endocytic receptors in the proximal tubuli. In addition, the influence of altering the molecular design of radiolabeled ligands on pharmacokinetics is discussed, which includes changes in their physicochemical properties and implementation of cleavable linkers or albumin-binding moieties. Furthermore, we discuss the influence of chelator and radionuclide choice on reabsorption of radioligands by the kidneys. Full article
(This article belongs to the Special Issue Feature Reviews in Radiopharmaceutical Sciences: Highlights of Two-Decade Development)
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14 pages, 2708 KiB  
Review
Radiotracers for Imaging of Fibrosis: Advances during the Last Two Decades and Future Directions
by Olof Eriksson and Irina Velikyan
Pharmaceuticals 2023, 16(11), 1540; https://doi.org/10.3390/ph16111540 - 01 Nov 2023
Viewed by 1103
Abstract
Fibrosis accompanies various pathologies, and there is thus an unmet medical need for non-invasive, sensitive, and quantitative methods for the assessment of fibrotic processes. Currently, needle biopsy with subsequent histological analysis is routinely used for the diagnosis along with morphological imaging techniques, such [...] Read more.
Fibrosis accompanies various pathologies, and there is thus an unmet medical need for non-invasive, sensitive, and quantitative methods for the assessment of fibrotic processes. Currently, needle biopsy with subsequent histological analysis is routinely used for the diagnosis along with morphological imaging techniques, such as computed tomography (CT), magnetic resonance imaging (MRI), and ultrasound (US). However, none of these imaging techniques are sufficiently sensitive and accurate to detect minor changes in fibrosis. More importantly, they do not provide information on fibrotic activity on the molecular level, which is critical for fundamental understanding of the underlying biology and disease course. Molecular imaging technology using positron emission tomography (PET) offers the possibility of imaging not only physiological real-time activity, but also high-sensitivity and accurate quantification. This diagnostic tool is well established in oncology and has exhibited exponential development during the last two decades. However, PET diagnostics has only recently been widely applied in the area of fibrosis. This review presents the progress of development of radiopharmaceuticals for non-invasive detection of fibrotic processes, including the fibrotic scar itself, the deposition of new fibrotic components (fibrogenesis), or the degradation of existing fibrosis (fibrolysis). Full article
(This article belongs to the Special Issue Feature Reviews in Radiopharmaceutical Sciences: Highlights of Two-Decade Development)
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44 pages, 2327 KiB  
Review
Radiometals in Imaging and Therapy: Highlighting Two Decades of Research
by Shalini Sharma and Mukesh K. Pandey
Pharmaceuticals 2023, 16(10), 1460; https://doi.org/10.3390/ph16101460 - 13 Oct 2023
Cited by 4 | Viewed by 2209
Abstract
The present article highlights the important progress made in the last two decades in the fields of molecular imaging and radionuclide therapy. Advancements in radiometal-based positron emission tomography, single photon emission computerized tomography, and radionuclide therapy are illustrated in terms of their production [...] Read more.
The present article highlights the important progress made in the last two decades in the fields of molecular imaging and radionuclide therapy. Advancements in radiometal-based positron emission tomography, single photon emission computerized tomography, and radionuclide therapy are illustrated in terms of their production routes and ease of radiolabeling. Applications in clinical diagnostic and radionuclide therapy are considered, including human studies under clinical trials; their current stages of clinical translations and findings are summarized. Because the metalloid astatine is used for imaging and radionuclide therapy, it is included in this review. In regard to radionuclide therapy, both beta-minus (β−) and alpha (α)-emitting radionuclides are discussed by highlighting their production routes, targeted radiopharmaceuticals, and current clinical translation stage. Full article
(This article belongs to the Special Issue Feature Reviews in Radiopharmaceutical Sciences: Highlights of Two-Decade Development)
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33 pages, 3822 KiB  
Review
Peptide Radioligands in Cancer Theranostics: Agonists and Antagonists
by Berthold A. Nock, Panagiotis Kanellopoulos, Lieke Joosten, Rosalba Mansi and Theodosia Maina
Pharmaceuticals 2023, 16(5), 674; https://doi.org/10.3390/ph16050674 - 30 Apr 2023
Cited by 4 | Viewed by 2267
Abstract
The clinical success of radiolabeled somatostatin analogs in the diagnosis and therapy—“theranostics”—of tumors expressing the somatostatin subtype 2 receptor (SST2R) has paved the way for the development of a broader panel of peptide radioligands targeting different human tumors. This approach relies [...] Read more.
The clinical success of radiolabeled somatostatin analogs in the diagnosis and therapy—“theranostics”—of tumors expressing the somatostatin subtype 2 receptor (SST2R) has paved the way for the development of a broader panel of peptide radioligands targeting different human tumors. This approach relies on the overexpression of other receptor-targets in different cancer types. In recent years, a shift in paradigm from internalizing agonists to antagonists has occurred. Thus, SST2R-antagonist radioligands were first shown to accumulate more efficiently in tumor lesions and clear faster from the background in animal models and patients. The switch to receptor antagonists was soon adopted in the field of radiolabeled bombesin (BBN). Unlike the stable cyclic octapeptides used in the case of somatostatin, BBN-like peptides are linear, fast to biodegradable and elicit adverse effects in the body. Thus, the advent of BBN-like antagonists provided an elegant way to obtain effective and safe radiotheranostics. Likewise, the pursuit of gastrin and exendin antagonist-based radioligands is advancing with exciting new outcomes on the horizon. In the present review, we discuss these developments with a focus on clinical results, commenting on challenges and opportunities for personalized treatment of cancer patients by means of state-of-the-art antagonist-based radiopharmaceuticals. Full article
(This article belongs to the Special Issue Feature Reviews in Radiopharmaceutical Sciences: Highlights of Two-Decade Development)
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15 pages, 3918 KiB  
Review
Clearing and Masking Agents in Pretargeting Strategies
by Markus Staudt and Matthias M. Herth
Pharmaceuticals 2023, 16(4), 497; https://doi.org/10.3390/ph16040497 - 27 Mar 2023
Cited by 2 | Viewed by 1717
Abstract
‘Pretargeting’ led to increased target-to-background ratios of nanomedicines in short timeframes. However, clearing or masking agents are needed to reach the full potential of pretargeted approaches. This review gives an overview of clearing and masking agents employed in pretargeting strategies in both preclinical [...] Read more.
‘Pretargeting’ led to increased target-to-background ratios of nanomedicines in short timeframes. However, clearing or masking agents are needed to reach the full potential of pretargeted approaches. This review gives an overview of clearing and masking agents employed in pretargeting strategies in both preclinical and clinical settings and discusses how these agents work. Full article
(This article belongs to the Special Issue Feature Reviews in Radiopharmaceutical Sciences: Highlights of Two-Decade Development)
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19 pages, 3755 KiB  
Review
Computational Chemistry for the Identification of Lead Compounds for Radiotracer Development
by Chia-Ju Hsieh, Sam Giannakoulias, E. James Petersson and Robert H. Mach
Pharmaceuticals 2023, 16(2), 317; https://doi.org/10.3390/ph16020317 - 18 Feb 2023
Cited by 8 | Viewed by 3554
Abstract
The use of computer-aided drug design (CADD) for the identification of lead compounds in radiotracer development is steadily increasing. Traditional CADD methods, such as structure-based and ligand-based virtual screening and optimization, have been successfully utilized in many drug discovery programs and are highlighted [...] Read more.
The use of computer-aided drug design (CADD) for the identification of lead compounds in radiotracer development is steadily increasing. Traditional CADD methods, such as structure-based and ligand-based virtual screening and optimization, have been successfully utilized in many drug discovery programs and are highlighted throughout this review. First, we discuss the use of virtual screening for hit identification at the beginning of drug discovery programs. This is followed by an analysis of how the hits derived from virtual screening can be filtered and culled to highly probable candidates to test in in vitro assays. We then illustrate how CADD can be used to optimize the potency of experimentally validated hit compounds from virtual screening for use in positron emission tomography (PET). Finally, we conclude with a survey of the newest techniques in CADD employing machine learning (ML). Full article
(This article belongs to the Special Issue Feature Reviews in Radiopharmaceutical Sciences: Highlights of Two-Decade Development)
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Other

Jump to: Review

10 pages, 734 KiB  
Opinion
RGD Forever!—Past, Present, and Future of a 3-Letter-Code in Radiopharmacy and Life Sciences
by Johannes Notni
Pharmaceuticals 2023, 16(1), 56; https://doi.org/10.3390/ph16010056 - 30 Dec 2022
Cited by 4 | Viewed by 2127
Abstract
“RGD” is frequently pictured as a ligand for αvβ3-integrin and useful for molecular targeting of angiogenesis—which is about as simplistic as the idea that laser beams are green or red and particularly useful for arming spaceships. There is, however, much more to RGD. [...] Read more.
“RGD” is frequently pictured as a ligand for αvβ3-integrin and useful for molecular targeting of angiogenesis—which is about as simplistic as the idea that laser beams are green or red and particularly useful for arming spaceships. There is, however, much more to RGD. In particular, targeting angiogenesis is likely not the most significant stronghold of RGD-comprising constructs. RGD is the one-letter code of a very short peptide sequence, arginine-lysine-aspartate, which is recognized by eight different integrins, namely, α(IIb)β3, α5β1, α8β1, and the five dimers that αv forms with β1, β3, β5, β6, and β8. These 8 RGD receptors form an own subset among the entire class of 24 known integrins, which furthermore comprises another three distinct groups (4 collagen receptors, 4 laminin receptors, and 8 leukocyte receptors). However, the 8 RGD-recognizing integrins are far from being alike. They do not even share the same tissue prevalences and functions, but are expressed on fundamentally different cell types and fulfill the most diverse biological tasks. For example, α(IIb)β3 is found on platelets and mediates thrombus formation, whereas αvβ6- and αvβ8-integrin are expressed on epithelial cells, activate TFG-β, and thus may promote cancer progression and invasion as well as fibrosis. Recent non-clinical experiments and clinical findings suggest that the highly specific expression of αvβ6-integrin by some carcinoma types, in combination with the availability of the corresponding small-molecule ligands, may open a multitude of new and promising avenues for improved cancer diagnosis and therapy, including, but not limited to, radiopharmaceutical approaches. Full article
(This article belongs to the Special Issue Feature Reviews in Radiopharmaceutical Sciences: Highlights of Two-Decade Development)
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