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DO3A-VS-exendin-4

Development stage: Unknown
Lead developer: Uppsala University
Modality: Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Peptides
Administration: Intravenous

Overview

DO3A-VS-exendin-4 is a radiopharmaceutical conjugate designed as a molecular imaging agent targeting the glucagon-like peptide 1 receptor (GLP-1R). It consists of the GLP-1R agonist peptide exendin-4 (specifically the Cys40-modified version) conjugated to the chelator DO3A-VS (1,4,7,10-tetraazacyclododecane-1,4,7-triacetic acid-vinylsulfone). This conjugation allows for radiolabeling with various isotopes such as Gallium-68 (68Ga) for Positron Emission Tomography (PET) imaging, as well as Copper-64 (64Cu) or Lutetium-177 (177Lu). The agent is primarily used in research settings to detect GLP-1R expression in insulinomas, monitor pancreatic beta-cell mass, and quantify transplanted human islets in the liver. It has also been utilized in clinical research to assess receptor occupancy of other incretin mimetics like tirzepatide.

Other names: [68Ga]Ga-DO3A-VS-exendin-4[64Cu]Cu-DO3A-VS-exendin-4[177Lu]Lu-DO3A-VS-exendin-4DO3A-VS-Cys40-Exendin-4DO-3A-VS-Cys40-Exendin-4DO 3A-VS-Cys40-Exendin-4

Targets

GLP1R (GLP-1R)

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