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[68Ga]Ga-DO3A-VS-Cys40-exendin-4
- Development stage
- Unknown
- Modality
- Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptide-Drug Conjugates → Peptide Conjugates → Peptides
- Administration
- Intravenous
01
Overview
[68Ga]Ga-DO3A-VS-Cys40-exendin-4 is a radiolabeled peptide-based imaging agent designed for positron emission tomography (PET) targeting the glucagon-like peptide 1 receptor (GLP-1R), which is overexpressed in insulinomas and pancreatic beta cells. It consists of an exendin-4 backbone—a potent full agonist of GLP-1R—conjugated with the chelator DO3A-VS at the Cys^40 residue, allowing for effective ^68Ga labeling for PET imaging. The agent leverages the high affinity of exendin-4 for GLP-1R to visualize insulinoma lesions with high sensitivity. This probe has shown promising results in preclinical animal models and preliminary human cases for the detection of insulinomas and for imaging transplanted islets. The development of analogous compounds labeled with therapeutic radionuclides, such as ^177Lu, is also underway for theranostic purposes[1][3][5].
- Other names
- [68Ga]DO3A-VS-Cys40-exendin-4[68Ga]-DO3A-VS-Cys40-exendin-4
02
Targets
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