Targeting of the Gastric Inhibitory Polypeptide (GIP) receptor is one of several emerging strategies in anti-diabetic drug development. Antaros Medical, in collaboration with Sanofi, has developed a high affinity Positron Emission Tomography (PET) ligand, [68Ga]S02-GIP-T4, for the receptor of the incretin hormone GIP to enable the assessment of target distribution and drug target engagement. The full publication of in vitro and in vivo data is now available in the April issue of Diabetes (Drug Occupancy Assessment at the Glucose-Dependent Insulinotropic Polypeptide (GIP) Receptor by Positron Emission Tomography) demonstrating that [68Ga]S02-GIP-T4 is a novel PET biomarker for safe, non-invasive, and quantitative assessment of GIP receptor target distribution and drug occupancy.
Tailored solutions for understanding bi- and trimodal incretin agonists
Antaros Medical has extensive experience in both driving imaging science and delivering studies in diabetes, obesity, and metabolism. We have two proprietary PET tracers, [68Ga]S02-GIP-T4 targeting the GIP receptor and [68Ga]-Tuna-2 targeting the glucagon receptor. They form, together with an additional PET-tracer for the glucagon like peptide-1 (GLP1) receptor, a powerful tool set for tailoring solutions measuring receptor occupancy of both bi- and trimodal incretin agonists developed for the treatment of various metabolic disorders. This PET-tracer tool set can provide data to help set dosing and to provide evidence that the investigated drug are hitting several targets as intended – including understanding the overlapping pharmacology of activating the different incretin receptors with multi-agonist peptides. This is an important platform for moving new metabolic including anti-diabetic treatments, such as bi- and trimodal incretin agonists, forward.
For full paper in Diabetes:
Authors: Eriksson O, Velikyan I, Haack T, Bossart M, Evers A, Lorenz K, Laitinen I, Larsen PJ, Plettenburg O, Johansson L, Pierrou S, Wagner M.
To read more on the PET tracer development collaboration, please see