Search for Articles:
Title / Keyword
Author / Affiliation / Email
Journal
Article Type
 
 
Advanced Search
 
Section
Special Issue
Volume
Issue
Number
Page
 
9.0
5.7
Journals
Pharmaceuticals
Special Issues
Radiopharmaceuticals in Cancer Disorders: Clinical and Pharmaceutical Perspectives
share announcement

Radiopharmaceuticals in Cancer Disorders: Clinical and Pharmaceutical Perspectives

A Special Issue of Pharmaceuticals (ISSN 1424-8247) belonging to the section "Radiopharmaceutical Sciences".

Deadline for manuscript submissions: 20 January 2027 | Viewed by 7578

Editor

Dr. Marta Rusek

E-Mail Website
Guest Editor
Independent Radiopharmacy Unit, Faculty of Pharmacy, Medical University of Lublin, 20-093 Lublin, Poland
Interests: medicinal chemistry; biomarkers; radiopharmaceuticals; radiomics; anticancer activity; in vitro/in vivo
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Radiopharmaceuticals have emerged as powerful tools in both the diagnosis and treatment of cancer, offering distinct advantages through their ability to selectively target tumors at the molecular level. The expanding field of theranostics—referring to the coordinated use of diagnostic and therapeutic radiopharmaceuticals, whether in a single agent or as a matched pair of compounds—has underscored the clinical value of radiolabeled entities such as 177Lu-DOTATATE and 68Ga-PSMA in oncology. Clinicians benefit from improved imaging precision and targeted radiotherapy, while pharmaceutical scientists are essential to the development, formulation, and quality assurance of these agents to ensure safety, stability, and efficacy.

This Special Issue aims to foster interdisciplinary dialogue between clinical practice and pharmaceutical research. We hope that it will provide a platform to explore the design and synthesis of novel radiopharmaceuticals, pharmacokinetic considerations, fundamental regulatory principles relevant across jurisdictions, clinical trial outcomes, and the integration of radiopharmaceuticals into personalized cancer care.

Dr. Marta Rusek
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 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-anonymized 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
  • cancer theranostics
  • targeted radionuclide therapy
  • molecular imaging
  • pharmaceutical development

Benefits of Publishing in a Special Issue

  • Ease of navigation: Grouping papers by topic helps scholars navigate broad scope journals more efficiently.
  • Greater discoverability: Special Issues support the reach and impact of scientific research. Articles in Special Issues are more discoverable and cited more frequently.
  • Expansion of research network: Special Issues facilitate connections among authors, fostering scientific collaborations.
  • External promotion: Articles in Special Issues are often promoted through the journal's social media, increasing their visibility.
  • Reprint: MDPI Books provides the opportunity to republish successful Special Issues in book format, both online and in print.

Further information on MDPI's Special Issue policies can be found here.

Published Papers (4 papers)

Download All Papers
Order results
Result details
Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:

Research

Jump to: Review

13 pages, 2172 KB  
Article
Bridging Research and Clinical Practice: Automated [68Ga]Ga-FAPi-46 Synthesis and Quality Control for Oncological PET Imaging
by Caiubi Rodrigues de Paula Santos, Luciana Malavolta, Jorge Mejia, Leonardo Lima Fuscaldi, Lilian Yuri Itaya Yamaga and Marycel Figols de Barboza
Pharmaceuticals 2026, 19(4), 594; https://doi.org/10.3390/ph19040594 - 8 Apr 2026
Cited by 1 | Viewed by 1555
Abstract
Background/Objectives: Fibroblast activation protein (FAP) has emerged as a promising target for oncologic molecular imaging due to its high expression in cancer-associated fibroblasts and low presence in healthy tissues. Among available FAP ligands, [68Ga]Ga-FAPi-46 has shown rapid tumor accumulation, low background [...] Read more.
Background/Objectives: Fibroblast activation protein (FAP) has emerged as a promising target for oncologic molecular imaging due to its high expression in cancer-associated fibroblasts and low presence in healthy tissues. Among available FAP ligands, [68Ga]Ga-FAPi-46 has shown rapid tumor accumulation, low background uptake, and broad tumor applicability. This study reports the successful translation of [68Ga]Ga-FAPi-46 from preclinical development to routine clinical radiopharmacy practice, detailing automated synthesis, quality control performance, radiochemical stability, and the first clinical imaging results. Methods: Automated radiolabeling of FAPi-46 with gallium-68 was performed using a synthesis module. Quality control included radiochemical purity assessments by iTLC, SPE, and RP-HPLC (pH, appearance, endotoxin levels, and membrane integrity testing). Radiochemical stability was evaluated in saline (up to 6 h) and human serum (up to 90 min). In vitro characterization included the partition coefficient and serum protein binding determination. A clinical evaluation was conducted in a woman with newly diagnosed lung adenocarcinoma who underwent both [18F]FDG PET/CT and [68Ga]Ga-FAPi-46 PET/CT. Results: Automated synthesis of [68Ga]Ga-FAPi-46 achieved a high radiochemical yield (87.9 ± 1.3%) and radiochemical purity greater than 98%. All batches met release specifications for sterility, apyrogenicity, and physicochemical parameters. The radiotracer demonstrated high stability in saline and human serum, with radiochemical purity consistently above 95% at all evaluated time points. The compound showed a hydrophilic profile (LogP = −3.32 ± 0.14) and 40–60% serum protein binding. Clinically, [68Ga]Ga-FAPi-46 PET/CT provided superior lesion delineation compared to [18F]FDG, revealing additional mediastinal, supraclavicular, and brain metastases. Conclusions: [68Ga]Ga-FAPi-46 can be reliably synthesized using automated procedures under routine radiopharmacy conditions, meeting regulatory quality standards and demonstrating excellent stability. Its enhanced lesion detectability compared with [18F]FDG in the first patient case supports its potential value for oncological staging and clinical implementation. Full article
(This article belongs to the Special Issue Radiopharmaceuticals in Cancer Disorders: Clinical and Pharmaceutical Perspectives)
►▼ Show Figures

Graphical abstract

19 pages, 1403 KB  
Article
A Phase II Study of 177Lu–Lilotomab Satetraxetan, a CD37 Antibody–Radionuclide Conjugate, as Third- or Later-Line Treatment of Rituximab-Refractory Follicular B-Cell Lymphoma Patients
by Roy H. Larsen, Arne Kolstad, Alexander Fosså, Ada Repetto-Llamazares, Knut T. Smerud, Timothy Illidge and Øyvind S. Bruland
Pharmaceuticals 2026, 19(2), 250; https://doi.org/10.3390/ph19020250 - 1 Feb 2026
Viewed by 1697
Abstract
Background: CD37, an antigen highly expressed in B-cell malignancies, served as the target in the LYMRIT-37-01 Part B (PARADIGME) and Part C studies employing a single intravenous injection of the radioimmunoconjugate 177Lu–lilotomab satetraxetan (Betalutin®). Methods: Patients with follicular [...] Read more.
Background: CD37, an antigen highly expressed in B-cell malignancies, served as the target in the LYMRIT-37-01 Part B (PARADIGME) and Part C studies employing a single intravenous injection of the radioimmunoconjugate 177Lu–lilotomab satetraxetan (Betalutin®). Methods: Patients with follicular lymphoma (FL), grades I–IIIa, who had received at least two previous lines of therapy and were refractory to at least one previous regimen with rituximab or an anti-CD20 agent, were included. They were randomized to receive either a 40 mg lilotomab pretreatment and an activity dosage of 15 MBq/kg Betalutin (“40/15” regimen) or 100 mg/m2 of lilotomab and 20 MBq/kg of Betalutin (“100/20” regimen). In total, 109 patients were enrolled and received Betalutin, 72 of whom received the 40/15 regimen and 28 received the 100/20 regimen. An additional heavily pretreated “special population” of nine patients received 40/12.5 (i.e., a reduced Betalutin dosage) due to low platelets and/or a previous autologous stem cell transplant. Part C was a small expansion cohort of four patients, all receiving the 40/15 regimen, and was designed to obtain supplementary pharmacokinetic data. Results: The efficacy analysis set comprised a total of 100 patients from the PARADIGME study. The overall response rates were 38.9% and 32.1%, and the complete response rates were 20.8% and 14.3% in the 40/15 and 100/20 groups, respectively. Correspondingly, the median response durations were 8.5 months and 3.4 months in the two groups. Hence, increasing the Betalutin activity dose by using the stronger protective CD37 pre-dosing (“100/20”) did not improve the therapeutic benefit. The most common grade ≥ 3 adverse events were hematologic, including neutropenia (11.5%) and thrombocytopenia (8.0%), with nadirs occurring around weeks 5–7 and recovery by week 11. Conclusions: A single-dose administration of Betalutin had a mild toxicity profile with a clinically relevant response rate. It represents a viable treatment alternative in FL patients who are not suitable for more toxic and long-lasting treatments. Trial Registration: This trial was registered at clinicaltrials.gov under #NCT 01796171. Full article
(This article belongs to the Special Issue Radiopharmaceuticals in Cancer Disorders: Clinical and Pharmaceutical Perspectives)
►▼ Show Figures

Graphical abstract

16 pages, 1984 KB  
Article
Optimized Automated Cassette-Based Synthesis of [68Ga]Ga-DOTATOC
by Anton Amadeus Hörmann, Johannes Neumann, Samuel Nadeje, Gregor Schweighofer-Zwink, Gundula Rendl, Theresa Jung, Teresa Kiener, Ruben Lechner, Sylvia Friedl, Ursula Huber-Schönauer, Martin Wolkersdorfer, Mohsen Beheshti and Christian Pirich
Pharmaceuticals 2025, 18(9), 1274; https://doi.org/10.3390/ph18091274 - 26 Aug 2025
Viewed by 2992
Abstract
Background: [68Ga]Ga-DOTATOC is widely used in PET imaging of neuroendocrine tumors (NETs) due to its high affinity for somatostatin receptors. Given the short physical half-life of gallium-68 (~68 min), rapid, reproducible, and GMP-compliant synthesis is essential for clinical application. Methods: An [...] Read more.
Background: [68Ga]Ga-DOTATOC is widely used in PET imaging of neuroendocrine tumors (NETs) due to its high affinity for somatostatin receptors. Given the short physical half-life of gallium-68 (~68 min), rapid, reproducible, and GMP-compliant synthesis is essential for clinical application. Methods: An optimized cassette-based automated synthesis protocol was developed using a commercial cassette. Improvements included direct generator elution into the reactor without pre-purification, use of a SepPak® C18 Plus Light cartridge for purification, replacement of HEPES with 0.3 M sodium acetate buffer (final pH ~3.8), and implementation of a non-vented sterile filter enabling automated pressure-hold integrity testing. Results: Across all batches, the synthesis yielded [68Ga]Ga-DOTATOC with high radiochemical purity (> 97%) and reproducible decay-corrected radiochemical yields up to 88.3 ± 0.6%. Total synthesis time was approximately 13 min. The final product remained stable for at least 3 h post-synthesis. The use of acetate buffer eliminated the need for HEPES-specific testing, streamlining the workflow. Automated filter testing improved GMP-compliant documentation and reduced radiation exposure for personnel. Conclusions: This optimized, cassette-based synthesis protocol enables fast, high-yield, and GMP-compliant production of [68Ga]Ga-DOTATOC. It supports clinical theranostic workflows by ensuring product quality, process standardization, and regulatory compliance. Full article
(This article belongs to the Special Issue Radiopharmaceuticals in Cancer Disorders: Clinical and Pharmaceutical Perspectives)
►▼ Show Figures

Graphical abstract

Review

Jump to: Research

28 pages, 1800 KB  
Review
Chemical Scaffolds Driving Modern Anticancer Drug Discovery and Radiotheranostics: Structural Determinants, Translational Opportunities and Future Perspectives
by Marta Rusek
Pharmaceuticals 2026, 19(8), 1248; https://doi.org/10.3390/ph19081248 - 8 Aug 2026
Viewed by 635
Abstract
Cancer remains one of the leading causes of morbidity and mortality worldwide despite advances in molecular oncology and targeted therapeutics. The growing demand for precision medicine has accelerated the development of radiotheranostics, an emerging paradigm that integrates molecular imaging and targeted radionuclide therapy. [...] Read more.
Cancer remains one of the leading causes of morbidity and mortality worldwide despite advances in molecular oncology and targeted therapeutics. The growing demand for precision medicine has accelerated the development of radiotheranostics, an emerging paradigm that integrates molecular imaging and targeted radionuclide therapy. In parallel, medicinal chemistry continues to generate structurally diverse small-molecule scaffolds capable of modulating key oncogenic pathways. Increasing evidence indicates that certain chemical scaffolds possess intrinsic properties that extend beyond conventional anticancer activity and support their translation into radiotheranostic applications. This review examines major scaffold classes driving contemporary anticancer drug discovery, including thiosemicarbazones, heterocyclic compounds, metal-based agents, hybrid molecules, and multifunctional platforms. Particular attention is given to the structural features governing biological activity, target selectivity, metal coordination, and radiolabeling potential. The review further highlights the mechanistic convergence between scaffold-mediated anticancer effects and radionuclide-induced cytotoxicity, emphasizing shared pathways involving DNA damage, oxidative stress, inhibition of DNA repair, and modulation of oncogenic signaling. Based on these observations, a scaffold-centered framework for radiotheranostic development is proposed, with perspectives on hybrid molecular design, copper-based theranostic systems, and artificial intelligence-assisted ligand discovery. By integrating medicinal chemistry, molecular oncology, and nuclear medicine, this review outlines structural principles that may facilitate the rational design of next-generation precision anticancer agents and radiotheranostic platforms. Full article
(This article belongs to the Special Issue Radiopharmaceuticals in Cancer Disorders: Clinical and Pharmaceutical Perspectives)
►▼ Show Figures

Figure 1

Show export options expand_more Show export options expand_less
Select all
Export citation of selected articles as:
 
Displaying articles 1-4
Back to TopTop