ArticleEJNMMI radiopharmacy and chemistry2024
Preclinical evaluation of new GRPR-antagonists with improved metabolic stability for radiotheranostic use in oncology.
Article in EJNMMI radiopharmacy and chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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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
6 citing papers in PubMed.
- GRPR-Targeted Radionuclide Conjugates: A Molecular Evolution Perspective.Chemistry & biodiversity · 2026Review
- Preclinical Evaluation of aACS pharmacology & translational science · 2026Article
- The gastrin-releasing peptide receptor in oncology: a comprehensive review of recent advances in targeted radionuclide theranostics.Frontiers in oncology · 2026Review
- RM2 and DB15 analogues bearing [EJNMMI radiopharmacy and chemistry · 2025Article
- Targeted radioligand therapy: physics and biology, internal dosimetry and other practical aspects duringTheranostics · 2025Review
- Article
Corrections and comments
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Authors and funding
8 authors.
Funding
Abstract
backgroundThe gastrin-releasing peptide receptor (GRPR) has been extensively studied as a biomolecular target for peptide-based radiotheranostics. However, the lack of metabolic stability and the rapid clearance of peptide radioligands, including radiolabeled GRPR-antagonists, often impede clinical application. Aiming at circumventing these drawbacks, we have designed three new GRPR-antagonist radioligands using [
resultsThese radioligands were compared in a series of in vitro assays using prostate adenocarcinoma PC-3 cells and in murine models. They all displayed high and GRPR-specific uptake in PC-3 cells. Analysis of mice blood collected 5 min post-injection (pi) revealed similar or even higher metabolic stability of the new radioligands compared with [
conclusionsThese findings strongly point at AU-SAR-M1 as a promising radiotherapeutic candidate when labeled with Lu-177, or other medically appealing therapeutic radiometals, especially when combined with in situ NEP-inhibition. To this goal further investigations are currently pursued.
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Registered trials
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