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[111In]In-DOTAGA-PEG2-(Sar11)RM26
- Development stage
- Preclinical
- Lead developer
- National Centre for Scientific Research 'Demokritos'
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Gamma Emitters → Radiopharmaceuticals, Peptides
- Administration
- Intravenous
01
Overview
[111In]In-DOTAGA-PEG2-(Sar11)RM26 (also known as [111In]In-AU-RM26-M1) is a preclinical-stage radiolabeled peptide antagonist targeting the gastrin-releasing peptide receptor (GRPR). Developed by researchers at Uppsala University and the National Centre of Scientific Research 'Demokritos', the compound is designed for the diagnostic imaging of GRPR-expressing tumors, such as prostate cancer, using single-photon emission computed tomography (SPECT). It is a modified version of the GRPR antagonist RM26, where the glycine residue at position 11 is replaced with sarcosine (Sar11). This structural modification significantly enhances the metabolic stability of the peptide against degradation by the cell-surface metalloendopeptidase neprilysin (NEP) in vivo, leading to improved tumor uptake and high-contrast imaging.
- Other names
- DOTAGA-PEG2-(Sar11)RM26DOTAGA-PEG2-[Sar11]RM26[111In]In-DOTAGA-PEG2-[Sar11]RM26
02
Targets
GRPR (Gastrin-releasing peptide receptor)
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