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Cancers
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Cancer Treatment: Present and Future of Radioligand Therapy
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Cancer Treatment: Present and Future of Radioligand Therapy

A special issue of Cancers (ISSN 2072-6694). This special issue belongs to the section "Cancer Therapy".

Deadline for manuscript submissions: closed (20 November 2025) | Viewed by 16975

Special Issue Editors

Dr. Egesta Lopci

E-Mail Website
Guest Editor
Nuclear Medicine Unit, Humanitas Research Hospital-IRCCS, Via Manzoni 56, 20089 Rozzano, Italy
Interests: molecular imaging; positron emission tomography; cancer imaging; immunotherapy; treatment response assessment
Special Issues, Collections and Topics in MDPI journals
Prof. Dr. Akram N. Al-Ibraheem

E-Mail Website
Guest Editor
Department of Nuclear Medicine and PET/CT, King Hussein Cancer Center (KHCC), Amman 11941, Jordan
Interests: radiotheranostics; PET/CT; molecular imaging; radioligand therapy; cancer diagnosis; nuclear medicine

Special Issue Information

Dear Colleagues,

We are excited to invite you to contribute to this Special Issue on "Cancer Treatment: Present and Future of Radioligand Therapy". Radioligand therapy (RLT) is an innovative targeted cancer treatment approach that minimizes damage to healthy organs while allowing higher therapeutic doses. Recent years have seen PSMA-based RLT become routine for prostate cancer, with promising agents like fibroblast activation protein (FAPI), C-X-C chemokine receptor type 4 (CXCR4), glucagon-like peptide-1 receptor (GLP-1R), and gastrin-releasing peptide receptor (GRPR) under investigation. This Special Issue will explore crucial RLT topics, including dosimetry, patient selection, efficacy, safety, toxicity assessment, emerging therapies, the role of molecular imaging, and the advent of artificial intelligence (AI) and machine learning applications in RLT.

We look forward to receiving your contributions.

Dr. Egesta Lopci
Prof. Dr. Akram N. Al-Ibraheem
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 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. Cancers is an international peer-reviewed open access semimonthly 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

  • radioligand therapy
  • PRLT
  • FAPI
  • PSMA
  • CXCR4
  • GRPR
  • GLP-1R
  • RLT
  • novel radiopharmaceutical
  • cancer theranostics

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Published Papers (5 papers)

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Research

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11 pages, 1001 KB  
Article
Cost Analysis of PSMA-PET in the PROSPET-BX Trial
by Egesta Lopci, Cesare Saitta, Alberto Saita, Elena Vanni, Alessandro Santandrea, Luca Disconzi, Vittorio Fasulo, Nicolò Buffi, Massimo Lazzeri and Giovanni Lughezzani
Cancers 2026, 18(5), 806; https://doi.org/10.3390/cancers18050806 - 2 Mar 2026
Viewed by 631
Abstract
Background: The PROSPET-BX trial compared [68Ga]PSMA-11 PET/CT (PSMA-PET) with multiparametric MRI (mpMRI) in parallel in men with suspicion of prostate cancer (PCa) after at least one previously negative biopsy (ClinicalTrials.gov: NCT05297162; GR-2018-12366240). In this study, we performed the cost analysis of [...] Read more.
Background: The PROSPET-BX trial compared [68Ga]PSMA-11 PET/CT (PSMA-PET) with multiparametric MRI (mpMRI) in parallel in men with suspicion of prostate cancer (PCa) after at least one previously negative biopsy (ClinicalTrials.gov: NCT05297162; GR-2018-12366240). In this study, we performed the cost analysis of the two imaging modalities with respect to the detection of clinically significant PCa (csPCa). Methods: We analyzed the data from patients enrolled in the trial who met the inclusion criteria. For the cost analysis, we identified six competing triage strategies, each defined as a binary decision rule for referral to prostate biopsy: (1) biopsy-all; (2) elevated PSA-density (PSAD; biopsy if PSAD > 0.15 ng/mL/cc; (3) mpMRI positive (PIRADS 3–5); (4) PSMA-PET positive (PRIMARY 3–5); (5) mpMRI or PSMA-PET positive; (6) PSAD and mpMRI. For each strategy, we yielded sensitivity, specificity, positive predictive value (PPV), negative predictive value (NPV), and accuracy for csPCa. Direct hospital costs were modeled from a provider perspective, incorporating testing and procedural costs. Unit costs (in EUR) were sourced from our institutional accounting records. Pairwise cost-effectiveness comparisons were performed using incremental cost-effectiveness ratio (ICER) and incremental net benefit (INB). Results: Among the six triage strategies evaluated, the “biopsy-all” approach achieved perfect sensitivity, whereas the PSAD + mpMRI pathway was the most parsimonious strategy but missed 14 csPCa cases (53.8%). The combined “mpMRI or PSMA-PET” strategy maximized detection (22 cPCa, missing only 4) at an intermediate cost (EUR 81.991 total; EUR 3.727 per csPCa). The pairwise comparison of each strategy with mpMRI alone showed for the mpMRI or PSMA-PET pathway a low ICER (~EUR 2.900/extra csPCa), with consistently positive and increasing INB across higher WTP (willingness-to-pay). Therefore, this combination provided the most favorable cost-effectiveness profile, balancing detection, efficiency, and cost. Conclusions: To the best of our knowledge, this is the first cost analysis study to compare different strategies incorporating PSMA-PET in the re-biopsy setting, demonstrating that the combined “mpMRI or PSMA-PET” pathway is the most cost-effective diagnostic pathway for csPCa detection. Full article
(This article belongs to the Special Issue Cancer Treatment: Present and Future of Radioligand Therapy)
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13 pages, 2678 KB  
Article
Digital Twins for Radiopharmaceutical Dosimetry: PBPK Modelling of [177Lu]Lu-rhPSMA-10.1 in a Preclinical mCRPC Model
by Gustavo Costa, Elham Yousefzadeh-Nowshahr, Valentina Vasic, Baiqing Sun, Luca Nagel, Alexander Wurzer, Franz Schilling, Ambros Beer, Wolfgang Weber, Susanne Kossatz and Gerhard Glatting
Cancers 2025, 17(24), 3957; https://doi.org/10.3390/cancers17243957 - 11 Dec 2025
Cited by 1 | Viewed by 990
Abstract
Background/Objectives: Accurate absorbed dose estimation is essential for optimising targeted radionuclide therapy (TRT) in metastatic castration-resistant prostate cancer, where kidney toxicity is dose-limiting. [177Lu]Lu-rhPSMA-10.1 is a novel PSMA-targeted radioligand with favourable tumour-to-kidney uptake ratios; however, inter-patient pharmacokinetic variability can lead to [...] Read more.
Background/Objectives: Accurate absorbed dose estimation is essential for optimising targeted radionuclide therapy (TRT) in metastatic castration-resistant prostate cancer, where kidney toxicity is dose-limiting. [177Lu]Lu-rhPSMA-10.1 is a novel PSMA-targeted radioligand with favourable tumour-to-kidney uptake ratios; however, inter-patient pharmacokinetic variability can lead to differences in organ and tumour absorbed doses under fixed-activity administration. Personalised dosimetry offers a means to address this variability. This work aims to create mouse PBPK model-based digital twins for [177Lu]Lu-rhPSMA-10.1 to test the model’s resistance to noise and evaluate its impact on accuracy and absorbed dose calculations. Methods: Five CB-17 SCID mice bearing LNCaP tumour xenografts received 2.6–3.1 MBq [177Lu]Lu-rhPSMA-10.1 intravenously. Biodistribution was assessed 24 h post-injection by organ weighing and gamma counting. The PBPK model, implemented in MATLAB SimBiology (R2023a), was fitted to individual biodistribution data using mouse-specific physiological parameters. Digital twins—combining the model with fitted parameters—were used to generate time–activity curves (TACs) for kidneys, tumours, and the whole body. Gaussian noise (σ = 0–0.35) was added to TACs to simulate measurement error. The model was refitted, and absorbed doses from time-integrated activities (TIAs) were compared to digital twin references. Results: The digital twin approach reproduced experimental data with physiologically plausible parameters. Absorbed dose estimates remained consistent and robust, deviating by <2.3% in kidneys and <1.0% in tumours. Conclusions: PBPK-based digital twins enable reliable, individualised dosimetry, even under substantial measurement uncertainty. Full article
(This article belongs to the Special Issue Cancer Treatment: Present and Future of Radioligand Therapy)
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Review

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30 pages, 2692 KB  
Review
Therapeutic Applications of Fibroblast Activation Protein (FAP)-Binding Radiopharmaceuticals: Review of Opportunities and Challenges
by Justine Maes, Bernard Pôlet, Janke Kleynhans, Filip Van Herpe, Karolien Goffin, Jeroen Dekervel, Philippe Nafteux, Baki Topal, Frederik Cleeren and Christophe M. Deroose
Cancers 2025, 17(24), 4019; https://doi.org/10.3390/cancers17244019 - 17 Dec 2025
Cited by 4 | Viewed by 2136
Abstract
Fibroblast activation protein (FAP)-binding radiopharmaceuticals have emerged as promising candidates for both diagnostic and therapeutic applications in oncology due to their selective targeting of cancer-associated fibroblasts (CAFs). This review evaluates the current literature on the therapeutic use of FAP-targeted radiopharmaceuticals in human studies, [...] Read more.
Fibroblast activation protein (FAP)-binding radiopharmaceuticals have emerged as promising candidates for both diagnostic and therapeutic applications in oncology due to their selective targeting of cancer-associated fibroblasts (CAFs). This review evaluates the current literature on the therapeutic use of FAP-targeted radiopharmaceuticals in human studies, with a focus on their safety, efficacy, and clinical applicability. Data on radionuclide type, clinical outcome, radiological and metabolic response and adverse events were extracted and summarized. The included studies demonstrated that lutetium-177,yttrium-90 and actinium-225 (in combination therapy) labeled FAP inhibitors exhibit high tumor uptake, with varying but mostly sufficient retention and a favorable safety profile. While mild adverse events such as fatigue, nausea and grade 1 or 2 hematotoxicity were observed, severe toxicities were rare. FAPI-based radionuclide therapies generally show high disease control rates, with promising results from tandem and combination strategies. The heterogeneity of tumor types and small sample sizes limited the generalizability of findings. FAP-targeted radioligand therapy appears to be a promising treatment option for patients with advanced cancer who have exhausted standard therapies. However, further large-scale, prospective clinical trials are necessary to determine optimal dosing strategies, long-term safety and efficacy across different tumor types. Emerging approaches, such as covalently binding FAP-targeted radiopharmaceuticals and the use of alpha-emitters such as actinium-225, lead-212 and bismuth-213, may further enhance treatment outcomes and warrant future investigation. Full article
(This article belongs to the Special Issue Cancer Treatment: Present and Future of Radioligand Therapy)
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25 pages, 800 KB  
Review
Radioligand Therapy in Cancer Management: A Global Perspective
by Gaia Ninatti, Sze Ting Lee and Andrew M. Scott
Cancers 2025, 17(21), 3412; https://doi.org/10.3390/cancers17213412 - 23 Oct 2025
Cited by 8 | Viewed by 6328
Abstract
Radioligand therapy (RLT) is a targeted treatment modality that combines a tumour-specific ligand with a therapeutic radionuclide. Once administered, the radiopharmaceutical binds selectively to cancer-associated targets, delivering cytotoxic radiation directly to tumour cells while sparing surrounding tissues. Two RLT agents, [177Lu]Lu-DOTA-TATE [...] Read more.
Radioligand therapy (RLT) is a targeted treatment modality that combines a tumour-specific ligand with a therapeutic radionuclide. Once administered, the radiopharmaceutical binds selectively to cancer-associated targets, delivering cytotoxic radiation directly to tumour cells while sparing surrounding tissues. Two RLT agents, [177Lu]Lu-DOTA-TATE (Lutathera®) and [177Lu]Lu-PSMA-617 (Pluvicto®), have received regulatory approval for the treatment of advanced gastroenteropancreatic neuroendocrine tumours and metastatic castration-resistant prostate cancer, respectively. As of July 2025, more than 400 clinical trials are registered, exploring novel molecular targets such as FAP, CAIX, and GRPR, as well as alternative radionuclides and combination regimens in both solid and haematologic malignancies. In this review, we describe the design principles and mechanisms of action of RLT, summarise clinical evidence for approved and emerging radiopharmaceuticals, and discuss current global disparities in access and availability. Finally, we outline the main clinical challenges, including fixed dosing regimens, resistance, toxicity, and variability in patient selection and response assessment. Continued research to optimise radiopharmaceutical design, together with investment in infrastructure, workforce capacity, and international collaboration, will be essential to expand access and realise the full potential of RLT as a leading treatment strategy in modern oncology. Full article
(This article belongs to the Special Issue Cancer Treatment: Present and Future of Radioligand Therapy)
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24 pages, 1200 KB  
Review
Theranostics in Hematological Malignancies: Cutting-Edge Advances in Diagnosis and Targeted Therapy
by Bojana Bogdanovic, Florent Hugonnet and Christopher Montemagno
Cancers 2025, 17(7), 1247; https://doi.org/10.3390/cancers17071247 - 7 Apr 2025
Cited by 3 | Viewed by 3663
Abstract
Hematologic malignancies, including leukemia, lymphoma, and multiple myeloma, continue to challenge clinicians with complex treatment regimens that often involve significant side effects and limited success, especially in advanced stages. Recent advancements in nuclear medicine have introduced theranostic strategies that merge diagnostic imaging with [...] Read more.
Hematologic malignancies, including leukemia, lymphoma, and multiple myeloma, continue to challenge clinicians with complex treatment regimens that often involve significant side effects and limited success, especially in advanced stages. Recent advancements in nuclear medicine have introduced theranostic strategies that merge diagnostic imaging with targeted therapeutic approaches, offering the potential for more precise and personalized treatment. A key area of progress lies in the development of alpha-emitting radiopharmaceuticals, such as 225Ac, 211At, or 212Pb, which can deliver potent radiation directly to tumor cells, sparing healthy tissue and minimizing collateral damage. In parallel with these therapeutic advancements, molecular imaging using radiolabeled agents enables better disease monitoring, assessment of treatment efficacy, and personalized management of patients with hematologic malignancies. The integration of diagnostic imaging with radiotherapy allows for a more tailored approach, where treatment can be adjusted based on real-time information about tumor progression and response. This review examines the recent strides made in both the development of radiopharmaceuticals and their applications in molecular imaging, with a focus on the potential to improve precision, reduce toxicity, and optimize patient outcomes. The synergy between targeted therapy and molecular imaging represents a transformative shift in the management of hematologic malignancies. As these technologies evolve, they are poised to redefine treatment paradigms, offering new hope for patients and potentially improving survival rates with more effective and less toxic treatment options. Full article
(This article belongs to the Special Issue Cancer Treatment: Present and Future of Radioligand Therapy)
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