68Ga-DOTA-semaglutide

68Ga-DOTA-semaglutide (also referred to as 68Ga-DOTA-SEMA) is a radiopharmaceutical diagnostic agent developed for positron emission tomography (PET) imaging of tissues expressing the glucagon-like peptide-1 receptor (GLP-1R). The agent consists of the long-acting GLP-1R agonist semaglutide—a synthetic analog of human GLP-1—conjugated to the macrocyclic chelator DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) and radiolabeled with the positron-emitting isotope Gallium-68. GLP-1R is highly expressed in pancreatic beta cells and is significantly overexpressed in insulinomas (insulin-secreting neuroendocrine tumors). By targeting these receptors, 68Ga-DOTA-semaglutide allows for the high-sensitivity detection and localization of small or occult insulinomas that may be missed by conventional imaging modalities like CT or MRI. Beyond oncology, the tracer is being investigated as a tool to non-invasively quantify functional beta-cell mass in patients with diabetes mellitus. It is currently undergoing clinical evaluation in Phase 1 and Phase 2 trials, primarily in China.

Other names

Gallium-68 DOTA-SemaglutideGallium68 DOTA-SemaglutideGallium 68 DOTA-Semaglutide68Ga-labeled DOTA-semaglutide68Ga-DOTA-SEMA-peptide