ArticleEuropean journal of nuclear medicine and molecular imaging2024
Mono- and multimeric PSMA-targeting small molecule-thorium-227 conjugates for optimized efficacy and biodistribution in preclinical models.
Article in European journal of nuclear medicine and molecular imaging, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 13 citations in OpenAlex.
- Bimodal Fluorescent Conjugate Based on Prostate-Specific Membrane Antigen Ligands with the Chelating Agent DOTA and SulfoCy5 Dye: Synthesis, Radiolabeling, and Biological Activity.International journal of molecular sciences · 2026Article
- Preclinical Evaluation Study ofChemical & biomedical imaging · 2026Article
- Optimizing PSMA-617-based inhibitors through charged linker modifications: Insights into structure-activity relationships.Theranostics · 2026Article
- A heterodimeric radioligand labeled with gallium-68 targeting fibroblast activation protein.EJNMMI research · 2025Article
- Determining the Multivalent Effects of d-Peptide-Based Radiotracers.Chemical & biomedical imaging · 2025Article
- An overview of the role of radionuclides in targeted cancer treatment: application of biomarkers for patient selection and developments to improve treatment efficacy.Frontiers in oncology · 2025Review
- The Pivotal Role of Preclinical Animal Models in Anti-Cancer Drug Discovery and Personalized Cancer Therapy Strategies.Pharmaceuticals (Basel, Switzerland) · 2024Review
- The importance of tyrosines in multimers of cyclic RGD nonapeptides: towards αvβ6-integrin targeted radiotherapeutics.RSC medicinal chemistry · 2024Article
- Actinium-225 targeted alpha particle therapy for prostate cancer.Theranostics · 2024Review
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Authors and funding
10 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposePSMA (prostate-specific membrane antigen) is highly expressed on prostate cancer (PrCa) cells and extensively used as a homing target for PrCa treatment. Most prominently, PSMA-targeting conjugate PSMA-617, carrying a DOTA chelator and labeled with therapeutic radionuclides like beta-emitting lutetium-177 or alpha-emitting actinium-225, has shown clinical activity in PrCa patients. We sought to develop PSMA-targeting small molecule (SMOL) conjugates that show high uptake in PSMA-expressing tumors and fast clearance, and can easily be labeled with the alpha emitter thorium-227 (half-life 18.7 days).
methodsA novel linker motif with improved competition against
resultsThe monomeric and multimeric PSMA SMOL conjugates were readily labeled with thorium-227 at room temperature and possessed high stability and good binding, internalization, and antiproliferative activity in vitro. In vivo, the monomeric, dimeric, and trimeric PSMA SMOL-TTCs showed fast clearance, potent antitumor efficacy, and high uptake and retention in prostate tumors in mice. No major uptake or retention in other organs was observed beyond kidneys. Low uptake of free thorium-227 into bone confirmed high complex stability in vivo. Salivary gland uptake remained inconclusive as mini pigs were devalidated as a relevant model and imaging controls failed in cynomolgus monkeys.
conclusionMonomeric and multimeric PSMA SMOL-TTCs show high tumor uptake and fast clearance in preclinical models and warrant further therapeutic exploration.
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