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20th Anniversary of Pharmaceuticals—Advances in Radiopharmaceutical Sciences and Nuclear...
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20th Anniversary of Pharmaceuticals—Advances in Radiopharmaceutical Sciences and Nuclear Medicine

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

Deadline for manuscript submissions: 25 February 2025 | Viewed by 5193

Special Issue Editor

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

Special Issue Information

Dear Colleagues,

It is our great delight and honor to celebrate the 20th Anniversary of Pharmaceuticals with a Special Issue from the section of Radiopharmaceutical Sciences, and to invite the researchers to contribute a manuscript of original research, review, or short communication. The articles from this section of "Radiopharmaceutical Sciences" will be compiled into a dedicated book.

This Special Issue entitled “Advances in radiopharmaceutical sciences and nuclear medicine” aims to cover success stories of established radiopharmaceuticals, development of novel radiopharmaceuticals, latest advances in nuclear medicine, frontier developments, and visions for the future achievements.

The development of radiopharmaceuticals considers the design, synthesis and radiolabeling of the associated agents, their biological and preclinical evaluation, and finally clinical application. Contributions may concern targeted, pre-targeted, and non-targeted radiopharmaceuticals ranging from small molecules via peptides, peptidomimetics and antibodies and derivatives to particles for their use in gamma scintigraphy, including single photon emission tomography (SPECT), positron emission tomography (PET) and endo radiotherapy. The field of diagnostic imaging and (radio)pharmaceutical therapy guided by diagnostic imaging is of strong interest. Manuscripts on the related topics of physics, dosimetry, radiopharmacy, and hybrid imaging will also be accepted. Another area of interest is the implementation of computational chemistry for radiopharmaceutical development and machine learning for image analysis. Please refer to the keyword list below for additional details.

Dr. Irina Velikyan
Guest Editor

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

  • radiopharmaceuticals, agents and probes
  • radionuclides
  • imaging biomarkers
  • biological/preclinical evaluation
  • first in-human clinical studies
  • SPECT, PET/CT and PET/MRI
  • labeling chemistry
  • medicinal radiochemistry, (pre)clinical radiopharmacology, and radiopharmacy including GMP-compliant production
  • radiopharmaceutical drug development
  • radio theranostics
  • hybrid imaging
  • organic molecules, high-molecular weight biomolecules and nano- and microparticles
  • artificial intelligence and machine learning in image analysis
  • computational chemistry in radiopharmaceutical development

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Published Papers (4 papers)

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Research

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16 pages, 4037 KiB  
Article
Enhancing Effects of Olaparib by Alpha- and Beta-Emitting Radionuclides, X-Rays, and Ultraviolet A Light in Combination with Ortho-IodoHoechst in a Prostate Cancer Cell Model
by Andrea C. Luna Mass, Roswitha Runge, Kerstin Wetzig, Lisa Huebinger, Claudia Brogsitter and Joerg Kotzerke
Pharmaceuticals 2024, 17(11), 1450; https://doi.org/10.3390/ph17111450 - 30 Oct 2024
Viewed by 682
Abstract
Background: New therapeutic strategies for metastatic castration-resistant prostate cancer (mCRPC) have been developed in the past to achieve the best response rates. Most recently, the use of combination therapies has been explored to optimize patient outcomes. Poly(ADP-ribose) polymerase inhibitors (PARPi) may help to [...] Read more.
Background: New therapeutic strategies for metastatic castration-resistant prostate cancer (mCRPC) have been developed in the past to achieve the best response rates. Most recently, the use of combination therapies has been explored to optimize patient outcomes. Poly(ADP-ribose) polymerase inhibitors (PARPi) may help to treat mCRPC more effectively. Objectives: This study aimed to determine whether the combination of a PARPi with different radiation qualities results in different levels of radiosensitization of PC-3 cells. Methods: The radiosensitizing potential of Olaparib in combination with 177Lu, 223Ra, X-rays and photodynamic therapy (PDT) using the UVA light-activated photosensitizer ortho-iodoHoechst33258 (oIH) was evaluated by determining the clonogenic survival, DNA damage and cell cycle analysis. Results: Here, we show that this combination strategy differentially sensitized PC-3 cells to different radiation qualities. The combination of 177Lu with Olaparib increased the numbers of persistent double-strand breaks (DSBs) by a factor of 3.3 and cell death in PC-3 cells. Overall, the β-emitter 177Lu indicated a higher radiosensitization efficacy compared to 223Ra, with X-rays corresponding to dose modification factors (DMF) of 1.77, 1.17 and 1.16 respectively. Even in the case of the α-emitter 223Ra, the effects were much less pronounced than for 177Lu. PARPi also showed a slight potentiation of the cytotoxic effects both in co-treatment with X-rays and with PDT. Conclusions: The results of our study indicate a potential role for Olaparib in further optimizing the PSMA radioligand therapy (PRLT) outcomes. However, further evaluation of the combination of PARPi with PRLT is needed to gain more insights into improving the benefit to patients suffering from mCRPC. Full article
(This article belongs to the Special Issue 20th Anniversary of Pharmaceuticals—Advances in Radiopharmaceutical Sciences and Nuclear Medicine)
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11 pages, 4342 KiB  
Article
Efficacy of Selective Internal Radiation Therapy for Hepatocellular Carcinoma Post-Incomplete Response to Chemoembolization
by Salma Binzaqr, Frederic Debordeaux, Jean-Frédéric Blanc, Panteleimon Papadopoulos, Elif Hindie, Bruno Lapouyade and Jean-Baptiste Pinaquy
Pharmaceuticals 2023, 16(12), 1676; https://doi.org/10.3390/ph16121676 - 1 Dec 2023
Cited by 1 | Viewed by 1787
Abstract
Hepatocellular carcinoma (HCC) is one of the most common neoplasms worldwide and the third most common cause of cancer-related death. Several liver-targeted intra-arterial therapies are available for unresectable HCC, including selective internal radiation therapy (SIRT) and trans-arterial chemoembolization (TACE). Those two are the [...] Read more.
Hepatocellular carcinoma (HCC) is one of the most common neoplasms worldwide and the third most common cause of cancer-related death. Several liver-targeted intra-arterial therapies are available for unresectable HCC, including selective internal radiation therapy (SIRT) and trans-arterial chemoembolization (TACE). Those two are the most used treatment modalities in localized non-operable HCC. TACE is the treatment option for patients with stage B, according to the BCLC staging system. In contrast, SIRT does not have an official role in the treatment algorithm, but recent studies showed promising outcomes in patients treated with SIRT. Although TACE is globally a safe procedure, it might provoke several vascular complications such as spasms, inflammatory constriction, and, in severe cases, occlusion, dissection, or collateralization. Hence, it is acclaimed that those complications could restrain the targeted response of the radio-embolization when we use it as second-line therapy post TACE. In this study, we will assess the efficacity of SIRT using Yttrium 90 Microspheres post incomplete or failure response to TACE. In our retrospective study, we had 23 patients who met the inclusion criteria. Furthermore, those patients have been followed radiologically and biologically. Then, we evaluated the therapeutic effect according to the mRECIST criteria, in addition to the personalized dose analysis. We found 8 patients were treated with TheraSphere®, with a median tumor absorbed dose of 445 Gy, while 15 received SIR-Spheres® treatment with a mean tumor dose of 268 Gy. After radiological analysis, 56.5% of the patients had a complete response, and 17.3% showed partial response, whereas 13% had stable disease and 13% had progressive disease. For patients treated with SIRT after an incomplete response or failure to TACE, we found an objective response rate of 73.8%. Despite the known vascular complications of TACE, SIRT can give a favorable response. Full article
(This article belongs to the Special Issue 20th Anniversary of Pharmaceuticals—Advances in Radiopharmaceutical Sciences and Nuclear Medicine)
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Review

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26 pages, 4608 KiB  
Review
Experiences from Clinical Research and Routine Use of Florbetaben Amyloid PET—A Decade of Post-Authorization Insights
by Aleksandar Jovalekic, Santiago Bullich, Núria Roé-Vellvé, Guilherme Domingues Kolinger, Lorelei R. Howard, Floriana Elsholz, Mariana Lagos-Quintana, Beatriz Blanco-Rodriguez, Esther Pérez-Martínez, Rossella Gismondi, Audrey Perrotin, Marianne Chapleau, Richard Keegan, Andre Mueller, Andrew W. Stephens and Norman Koglin
Pharmaceuticals 2024, 17(12), 1648; https://doi.org/10.3390/ph17121648 - 7 Dec 2024
Viewed by 538
Abstract
Florbetaben (FBB) is a radiopharmaceutical approved by the FDA and EMA in 2014 for the positron emission tomography (PET) imaging of brain amyloid deposition in patients with cognitive impairment who are being evaluated for Alzheimer’s disease (AD) or other causes of cognitive decline. [...] Read more.
Florbetaben (FBB) is a radiopharmaceutical approved by the FDA and EMA in 2014 for the positron emission tomography (PET) imaging of brain amyloid deposition in patients with cognitive impairment who are being evaluated for Alzheimer’s disease (AD) or other causes of cognitive decline. Initially, the clinical adoption of FBB PET faced significant barriers, including reimbursement challenges and uncertainties regarding its integration into diagnostic clinical practice. This review examines the progress made in overcoming these obstacles and describes the concurrent evolution of the diagnostic landscape. Advances in quantification methods have further strengthened the traditional visual assessment approach. Over the past decade, compelling evidence has emerged, demonstrating that amyloid PET has a strong impact on AD diagnosis, management, and outcomes across diverse clinical scenarios, even in the absence of amyloid-targeted therapies. Amyloid PET imaging has become essential in clinical trials and the application of new AD therapeutics, particularly for confirming eligibility criteria (i.e., the presence of amyloid plaques) and monitoring biological responses to amyloid-lowering therapies. Since its approval, FBB PET has transitioned from a purely diagnostic tool aimed primarily at excluding amyloid pathology to a critical component in AD drug development, and today, it is essential in the diagnostic workup and therapy management of approved AD treatments. Full article
(This article belongs to the Special Issue 20th Anniversary of Pharmaceuticals—Advances in Radiopharmaceutical Sciences and Nuclear Medicine)
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15 pages, 1045 KiB  
Review
Mechanistic Sequence of Histone Deacetylase Inhibitors and Radiation Treatment: An Overview
by Elsie Neo Seane, Shankari Nair, Charlot Vandevoorde and Anna Joubert
Pharmaceuticals 2024, 17(5), 602; https://doi.org/10.3390/ph17050602 - 8 May 2024
Viewed by 1328
Abstract
Histone deacetylases inhibitors (HDACis) have shown promising therapeutic outcomes in haematological malignancies such as leukaemia, multiple myeloma, and lymphoma, with disappointing results in solid tumours when used as monotherapy. As a result, combination therapies either with radiation or other deoxyribonucleic acid (DNA) damaging [...] Read more.
Histone deacetylases inhibitors (HDACis) have shown promising therapeutic outcomes in haematological malignancies such as leukaemia, multiple myeloma, and lymphoma, with disappointing results in solid tumours when used as monotherapy. As a result, combination therapies either with radiation or other deoxyribonucleic acid (DNA) damaging agents have been suggested as ideal strategy to improve their efficacy in solid tumours. Numerous in vitro and in vivo studies have demonstrated that HDACis can sensitise malignant cells to both electromagnetic and particle types of radiation by inhibiting DNA damage repair. Although the radiosensitising ability of HDACis has been reported as early as the 1990s, the mechanisms of radiosensitisation are yet to be fully understood. This review brings forth the various protocols used to sequence the administration of radiation and HDACi treatments in the different studies. The possible contribution of these various protocols to the ambiguity that surrounds the mechanisms of radiosensitisation is also highlighted. Full article
(This article belongs to the Special Issue 20th Anniversary of Pharmaceuticals—Advances in Radiopharmaceutical Sciences and Nuclear Medicine)
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