ArticleCurrent radiopharmaceuticals2020
In situ Generated
Article in Current radiopharmaceuticals, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
19 citing papers in PubMed, 28 citations in OpenAlex.
- Tumor Targeting with Peptide-Drug Conjugates: Showcasing Key Progress and Hurdles.Drug design, development and therapy · 2026Review
- Lead radionuclides for theranostic applications in nuclear medicine: from atom to bedside.Theranostics · 2026Review
- Therapeutic evaluation of [European journal of nuclear medicine and molecular imaging · 2025Article
- Alpha Particle Emitter Radiolabeled Antibodies in Cancer Therapy: Current Status, Challenges, and Future Prospects.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Review
- Radionuclide-Labeled Biomaterials: A Novel Strategy for Tumor-Targeted Therapy.Biomimetics (Basel, Switzerland) · 2025Review
- Advances in PSMA-Targeted Radionuclide Therapy for Metastatic Castration-Resistant Prostate Cancer.Cancer management and research · 2025Review
- Antigen targeting and anti-tumor activity of a novel anti-CD146Scientific reports · 2024Article
- Tuning the Softness of the Pendant Arms and the Polyazamacrocyclic Backbone to Chelate theInorganic chemistry · 2024Article
- An Experimental Generator for Production of High-PurityJournal of nuclear medicine : official publication, Society of Nuclear Medicine · 2023Article
- Advances inPharmaceutics · 2022Review
- Article
- Review
- Dual targeting withFrontiers in medicine · 2022Article
- Prostate specific membrane antigen binding radiopharmaceuticals: Current data and new concepts.Frontiers in medicine · 2022Review
- Targeted alpha therapy with theFrontiers in medicine · 2022Article
- Radiolabeled PSMA Inhibitors.Cancers · 2021Review
- Evaluation of the PSMA-Binding LigandInternational journal of molecular sciences · 2021Article
- Preclinical and Clinical Status of PSMA-Targeted Alpha Therapy for Metastatic Castration-Resistant Prostate Cancer.Cancers · 2021Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
4 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundNew treatments combating bone and extraskeletal metastases are needed for patients with metastatic castration-resistant prostate cancer. The majority of metastases overexpress prostate-specific membrane antigen (PSMA), making it an ideal candidate for targeted radionuclide therapy.
objectiveThe aim of this study was to test a novel liquid 224Ra/212Pb-generator for the rapid preparation of a dual-alpha targeting solution. Here, PSMA-targeting ligands are labelled with 212Pb in the 224Ra-solution in transient equilibrium with daughter nuclides. Thus, natural bone-seeking 224Ra targeting sclerotic bone metastases and 212Pb-chelated PSMA ligands targeting PSMA-expressing tumour cells are obtained.
methodsTwo PSMA-targeting ligands, the p-SCN-Bn-TCMC-PSMA ligand (NG001), specifically developed for chelating 212Pb, and the most clinically used DOTA-based PSMA-617 were labelled with 212Pb. Radiolabelling and targeting potential were investigated in situ, in vitro (PSMA-positive C4-2 human prostate cancer cells) and in vivo (athymic mice bearing C4-2 xenografts).
resultsNG001 was rapidly labelled with 212Pb (radiochemical purity >94% at concentrations of ≥15 μg/ml) using the liquid 224Ra/212Pb-generator. The high radiochemical purity and stability of [212Pb]Pb- NG001 were demonstrated over 48 hours in the presence of ascorbic acid and albumin. Similar binding abilities of the 212Pb-labelled ligands were observed in C4-2 cells. The PSMA ligands displayed comparable tumour uptake after 2 hours, but NG001 showed a 3.5-fold lower kidney uptake than PSMA- 617. Radium-224 was not chelated and, hence, showed high uptake in bones.
conclusionA fast method for the labelling of PSMA ligands with 212Pb in the 224Ra/212Pb-solution was developed. Thus, further in vivo studies with dual tumour targeting by alpha-particles are warranted.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.