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Targeted Radiotracers for Molecular Imaging and Therapy in Cancer

A special issue of Cancers (ISSN 2072-6694). This special issue belongs to the section "Methods and Technologies Development".

Deadline for manuscript submissions: closed (30 June 2026) | Viewed by 2183

Editors


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Guest Editor
Department of Immunology, Genetics and Pathology (IGP), Uppsala University, 751 85 Uppsala, Sweden
Interests: targeted radiotracers; molecular imaging; nuclear medicine
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Immunology, Genetics and Pathology, Uppsala University, 751 85 Uppsala, Sweden
Interests: theranostic; precision oncology; targeted radiotracer

Special Issue Information

Dear Colleagues,

Targeted radiotracers are essential tools in precision oncology, enabling the visualization and treatment of various cancers. These agents consist of radionuclides conjugated to peptides, antibodies, or small molecules that selectively bind to cancer-associated targets, including somatostatin receptors, PSMA, HER2, CXCR4, integrins, and other targets. The targeted radiotracers can be used for patient stratification for personalized therapies and assessments of response to the treatment. Molecular imaging modalities such as positron emission tomography (PET) and single-photon emission-computed tomography (SPECT) enable non-invasive, real-time visualization of tumor biology at the molecular level. Furthermore, conjugation of cytotoxic radionuclides, e.g., beta or alpha emitters, enables suppression of the tumor's growth. This Special Issue focuses on recent progress in the design, evaluation, and clinical translation of targeted radiotracers for diagnostic and therapeutic applications. Emphasis is placed on the ‘’theranostic’’ approach, where the same molecular scaffold is used for both diagnosis and targeted radionuclide therapy, as exemplified by agents such as ⁶⁸Ga-/¹⁷⁷Lu-labeled PSMA and DOTATATE. This approach improves treatment planning, dosimetry, and response monitoring. Recent advances have expanded the range of radiotracers available for clinical and preclinical use, highlighting their growing relevance in oncology. This Special Issue underscores the growing clinical relevance of targeted radiotracers and provides a comprehensive overview of current challenges and future directions in molecular imaging and therapy in cancer.

Prof. Dr. Vladimir Tolmachev
Dr. Maryam Oroujeni
Guest Editors

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Keywords

  • theranostic
  • radionuclide molecular imaging
  • targeted therapy
  • specificity
  • selectivity
  • personalized medicine
  • radiopharmaceuticals

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Published Papers (2 papers)

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13 pages, 1329 KB  
Article
Comparison of Localization Methods in Cushing Disease—Could [11C]C-Methionine PET/CT Replace MRI or BIPSS?
by Adam Daniel Durma, Marek Saracyn, Maciej Kołodziej, Grzegorz Zieliński, Piotr Zięcina, Jerzy Narloch and Grzegorz Kamiński
Cancers 2025, 17(19), 3147; https://doi.org/10.3390/cancers17193147 - 27 Sep 2025
Cited by 3 | Viewed by 1314
Abstract
Introduction: Cushing syndrome (CS) is a medical condition resulting from prolonged hypercortisolemia. The most common reason for endogenous CS is ACTH overproduction by pituitary adenoma, and then it is called Cushing disease (CD). The gold standard of CD diagnostic remains bilateral inferior [...] Read more.
Introduction: Cushing syndrome (CS) is a medical condition resulting from prolonged hypercortisolemia. The most common reason for endogenous CS is ACTH overproduction by pituitary adenoma, and then it is called Cushing disease (CD). The gold standard of CD diagnostic remains bilateral inferior petrosal sinus sampling (BIPSS); nevertheless, non-invasive diagnostic methods are being sought to provide a higher safety profile. The aim of this study was to evaluate whether [11C]C-MET PET/CT can serve as a non-invasive alternative to BIPSS and MRI in CD diagnosis. Methods: This prospective study included 21 patients with CD who underwent BIPSS, MRI of the pituitary, and [11C]C-MET PET/CT. Results: Sensitivity of BIPSS, MRI and [11C]C-MET PET/CT was 100%, 59% and 24%, respectively, while specificity was 100%, 75%, and 13%. Next, we retrospectively compared PET/CT results for patients with corticotrope pituitary adenomas (n = 18) with those for individuals with no pituitary pathology (n = 18), and the results showed significantly higher SUVmax in the study group (3.74 ± 0.90 vs. 1.87 ± 1.17; p < 0.001). In ROC curve analysis, the area under the curve (AUC) was 0.889 (p <0.001; 95% CI 0.784–0.994). For SUVmax 2.60, the calculated sensitivity and specificity were 89% and 78% respectively, and for SUVmax 3.56, sensitivity and specificity were 67% and 89%, respectively. Conclusions: [11C]C-MET PET/CT seems not to be a reliable diagnostic option in the diagnosis of pituitary corticotropic adenomas. BIPSS proved still to be the best diagnostic option for CD. Nevertheless, a higher than normal pituitary accumulation of the radiotracer may suggest the presence of increased amino acid metabolism, thus, the presence of adenoma. Full article
(This article belongs to the Special Issue Targeted Radiotracers for Molecular Imaging and Therapy in Cancer)
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17 pages, 1079 KB  
Systematic Review
Predicting Therapeutic Response to Antibody-Drug Conjugates Using Targeted PET Imaging: A Systematic Review
by David Mourath, Nour Susaeg Romdhani, Viveka Bergman, Jonathan Siikanen, Thuy A. Tran, Ali Alhuseinalkhudhur, Anna Kistner and Renske Altena
Cancers 2026, 18(15), 2514; https://doi.org/10.3390/cancers18152514 - 5 Aug 2026
Abstract
Background: Antibody-drug conjugates (ADCs) are gaining rapidly expanding clinical utility, with a growing number of approved indications across compounds that differ in target antigen, payload mechanism, and linker design. However, treatment response remains heterogeneous, and predictive biomarkers to identify patients most likely to [...] Read more.
Background: Antibody-drug conjugates (ADCs) are gaining rapidly expanding clinical utility, with a growing number of approved indications across compounds that differ in target antigen, payload mechanism, and linker design. However, treatment response remains heterogeneous, and predictive biomarkers to identify patients most likely to benefit are limited. Given that ADC efficacy depends on sufficient target antigen expression and distribution across tumor lesions, positron emission tomography (PET) imaging offers a unique opportunity to non-invasively assess whole-body target availability. We therefore conducted a systematic literature review to evaluate the relationship between PET-measured tumor antigen expression and the therapeutic response to ADCs targeting the same antigen. Method: A systematic comprehensive search of PubMed, EMBASE and Web of Science databases was conducted in accordance with Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) guidelines, using terms related to targeted PET, ADC treatment and response assessment. Article screening, eligibility assessment, and data extraction were performed independently using predefined criteria by two reviewers. Disagreements were resolved by consensus. Results: A total of 5628 records were identified. After removing duplicates, 4323 records were screened by title and abstract. Fifty-eight underwent full-text review and seven were included in the final review. Four trials investigated human epidermal growth factor receptor 2 (HER2)-targeted therapy, one Nectin-4, one mesothelin and one STEAP1. In all HER2- and Nectin-4-related trials, patients with a higher uptake on targeted PET had a higher probability of responding to targeted treatment. Included trials were generally small and had a moderate risk of bias. Conclusion: Targeted PET imaging showed potential to predict treatment response in trials evaluating clinically active agents. Additional clinical trials across a broader range of targets, along with standardized acquisition protocols and harmonized study designs, are needed to enable the integration of this technique into clinical practice and ultimately translate its benefits to patients. Full article
(This article belongs to the Special Issue Targeted Radiotracers for Molecular Imaging and Therapy in Cancer)
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