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[68Ga]DO3A-S01-GCG (also known as [68Ga]Ga-DO3A-VS-Cys40-Tuna-2 or 68Ga-Tuna-2) is a first-in-class positron emission tomography (PET) radiopharmaceutical imaging tracer that specifically targets the glucagon receptor (GCGR). Developed through a collaboration between Antaros Medical and Sanofi, the tracer consists of a potent GCGR-selective peptide agonist (S01-GCG or Tuna-2) conjugated to a DO3A/DOTA chelator and radiolabeled with gallium-68. It is designed as a target engagement biomarker to non-invasively quantify GCGR occupancy in vivo, particularly to support the clinical development of dual or triple incretin receptor agonists (such as GLP-1/GCG dual agonists) for metabolic disorders. The tracer has been evaluated in Phase I clinical studies in individuals with type 2 diabetes and obesity to assess the receptor occupancy of therapeutic candidates like SAR425899.
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