Radiopharmaceuticals in Cancer Disorders: Clinical and Pharmaceutical Perspectives

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

Deadline for manuscript submissions: 31 January 2026 | Viewed by 545

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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
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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

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Keywords

  • radiopharmaceuticals
  • cancer theranostics
  • targeted radionuclide therapy
  • molecular imaging
  • pharmaceutical development

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Published Papers (1 paper)

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Research

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 414
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
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