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Pharmaceuticals
Special Issues
Production, Development and Theranostic Applications of Radiopharmaceuticals for Nuclear Medicine
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Production, Development and Theranostic Applications of Radiopharmaceuticals for Nuclear Medicine

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

Deadline for manuscript submissions: closed (31 October 2025) | Viewed by 9983

Special Issue Editors

Dr. Vlad Ghizdovat

E-Mail Website
Guest Editor
Department of Biophysics and Medical Physics, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iasi, Romania
Interests: medical physics; biophysics; nuclear medicine; radiology; radiation protection
Dr. Cipriana Stefanescu

E-Mail Website
Guest Editor
Department of Biophysics and Medical Physics, “Grigore T. Popa” University of Medicine and Pharmacy, 700115 Iasi, Romania
Interests: nuclear medicine; biophysics; oncology; radiotracers
Dr. Cécile Philippe

E-Mail Website
Guest Editor
Department of Biomedical Imaging and Image-guided Therapy, Division of Nuclear Medicine, Medical University Vienna, 1090 Vienna, Austria
Interests: drug evaluation, preclinical; molecular imaging; positron-emission tomography; radioactive tracers; radiochemistry
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Theranostics is an innovative method that integrates diagnostic imaging with radionuclide treatment. There has been a significant growth in the use of theranostics in nuclear medicine clinical practice in recent years. As a result, research has been concentrated on finding new radionuclides that can attach to specific molecular targets that are commonly dysregulated in various types of cancer. The theranostic technique offers several significant benefits, such as streamlining treatments, minimizing harm to healthy tissues, enabling early diagnosis, improving predicting responses, and providing individualized patient therapy.

This Special Issue aims to discuss the current state of the art and progress in this field. Research areas may include (but are not limited to) the following: emerging theranostic molecules, recently introduced molecular targets, and production and development of new radiopharmaceuticals for theranostic applications.

Dr. Vlad Ghizdovat
Dr. Cipriana Stefanescu
Dr. Cécile Philippe
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 250 words) can be sent to the Editorial Office for assessment.

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

  • theranostic
  • radiopharmaceuticals
  • nuclear medicine
  • alpha-emitting radioisotopes
  • beta-emitting radioisotopes
  • gamma-emitting radioisotopes

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Published Papers (2 papers)

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Research

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15 pages, 4136 KB  
Article
A Novel FAPI-Based Radiopharmaceutical for SPECT Imaging of Fibrotic Interstitial Lung Disease
by Guangjie Yang, Jingnan Wang, Yu Liu, Jiyun Shi, Xueyang Zhang, Yangzhong Zhou, Qian Wang, Fan Wang and Li Huo
Pharmaceuticals 2025, 18(12), 1779; https://doi.org/10.3390/ph18121779 - 23 Nov 2025
Cited by 1 | Viewed by 1308
Abstract
Objectives: Early and noninvasive detection of fibrotic interstitial lung disease (fILD) is a critical but unmet clinical necessity. This study aimed to evaluate the feasibility of using 99mTc-HYNIC-Glu(PEG4-oncoFAPi)2 (denoted as 99mTc-H-PoFP2), a novel 99mTc-labeled [...] Read more.
Objectives: Early and noninvasive detection of fibrotic interstitial lung disease (fILD) is a critical but unmet clinical necessity. This study aimed to evaluate the feasibility of using 99mTc-HYNIC-Glu(PEG4-oncoFAPi)2 (denoted as 99mTc-H-PoFP2), a novel 99mTc-labeled radiopharmaceutical that targets fibroblast activation protein (FAP), for single-photon emission computed tomography (SPECT) imaging of pulmonary fibrosis in a mouse model and preliminary clinical studies. Methods: 99mTc-H-PoFP2 could be conveniently afforded using a kit formula with high radiochemical purity and stability. The binding specificity and affinity of 99mTc-H-PoFP2 for FAP were validated by an in vitro binding assay. The in vivo characteristics of 99mTc-H-PoFP2 were also determined. Results: 99mTc-H-PoFP2 was eliminated quickly via the urinary system, leading to low normal tissue uptake and a high target/background ratio. SPECT imaging demonstrated significantly enhanced uptake of the 99mTc-H-PoFP2 in bleomycin-induced fibrotic lung tissues, with visual effects superior to those of normal mice. Thus, a pilot clinical study of 99mTc-H-PoFP2 SPECT/CT imaging was conducted in 12 patients diagnosed with fILD. The physiological biodistribution of 99mTc-H-PoFP2 in patients was predominantly observed in the kidneys, bladder, liver, and pancreas, with relatively minor accumulation in the thyroid, salivary glands, and spleen. fILD patients exhibited elevated pulmonary 99mTc-H-PoFP2 uptake in the affected lung regions. Furthermore, the uptake of 99mTc-HPoFP2 demonstrated moderate correlations with the results of pulmonary function tests (PFTs). A higher gender–age–physiology (GAP) index was associated with elevated standardized uptake value maximum (SUVmax) and target-to-background ratio (TBR) values. Conclusions: Collectively, this study demonstrates the potential of 99mTc-HPoFP2 for SPECT imaging and assessing fILD by targeting FAP overexpressed in fibrotic lung tissues. This strategy offers new possibilities for noninvasive and precise assessment of pulmonary fibrosis. Full article
(This article belongs to the Special Issue Production, Development and Theranostic Applications of Radiopharmaceuticals for Nuclear Medicine)
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Review

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22 pages, 1010 KB  
Review
Targeted Alpha Therapy: Exploring the Clinical Insights into [225Ac]Ac-PSMA and Its Relevance Compared with [177Lu]Lu-PSMA in Advanced Prostate Cancer Management
by Wael Jalloul, Vlad Ghizdovat, Tamás Pócza, Alexandra Saviuc, Despina Jalloul, Irena Cristina Grierosu and Cipriana Stefanescu
Pharmaceuticals 2025, 18(8), 1215; https://doi.org/10.3390/ph18081215 - 18 Aug 2025
Cited by 8 | Viewed by 7790 | Correction
Abstract
Targeted alpha therapy (TAT) has recently emerged as a highly promising approach for the management of metastatic castration-resistant prostate cancer (mCRPC), especially in patients with disease progression despite standard treatments. Among alpha-emitter radiopharmaceuticals, actinium-225-labelled prostate-specific membrane antigen ([225Ac]Ac-PSMA) has shown remarkable potential due [...] Read more.
Targeted alpha therapy (TAT) has recently emerged as a highly promising approach for the management of metastatic castration-resistant prostate cancer (mCRPC), especially in patients with disease progression despite standard treatments. Among alpha-emitter radiopharmaceuticals, actinium-225-labelled prostate-specific membrane antigen ([225Ac]Ac-PSMA) has shown remarkable potential due to its high linear energy transfer (LET), short path length, and ability to induce potent, localised cytotoxic effects. This review summarises current clinical evidence regarding [225Ac]Ac-PSMA radioligand therapy (RLT), emphasising its efficacy, safety profile, and position relative to beta-emitter therapy with lutetium-177 ([177Lu]Lu-PSMA). Data from compassionate-use programs and small clinical trials demonstrate that [225Ac]Ac-PSMA produces significant biochemical and imaging responses, including > 50% declines in prostate-specific antigen (PSA) and lesion regression on [68Ga]Ga-PSMA PET/CT, even in heavily pre-treated mCRPC cohorts. Xerostomia, renal toxicity, and haematological adverse effects remain the main safety challenges, necessitating optimisation of patient selection, dosing strategies, and salivary gland protection protocols. Compared with [177Lu]Lu-PSMA, [225Ac]Ac-PSMA appears effective even in cases of beta-refractory disease, highlighting its complementary role rather than a competitive alternative. However, limited availability, high production costs, and the lack of large-scale, randomised trials hinder widespread clinical adoption. Future directions include combination protocols, improved radiopharmaceutical design, and trials evaluating its use in earlier disease stages. This review provides a comprehensive overview of the clinical aspects of [225Ac]Ac-PSMA RLT and its evolving role in advanced prostate cancer management. Full article
(This article belongs to the Special Issue Production, Development and Theranostic Applications of Radiopharmaceuticals for Nuclear Medicine)
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