Taspoglutide is a long-acting glucagon-like peptide-1 (GLP-1) receptor agonist (EC50 value of 0.06 nM) used for the treatment of type 2 diabetes.

GLP1:（EC50）0.06 nM

Taspoglutide (R1583/BIM51077), exhibiting 93% homology with native polypeptides, is a long-acting formulation of (Aib8-35) human GLP-1 (7-36 amides) that activates the GLP-1 receptor. It demonstrates an affinity constant (1.1±0.2 nM) towards the hGLP-1 receptor, closely mirroring the natural ligand’s affinity constant of 1.5±0.3 nM, and shows similar potency in stimulating cAMP production [2].

The rate of glucose-induced insulin secretion from isolated enhanced by Taspoglutide, cultured rat islets and the perfused ZDF rat pancreas. Taspoglutide showed dose-dependent enhancement of glucose-dependent insulin release in Sprague-Dawley rats and diabetic db/db mice, thereby reducing blood glucose in the type 2 diabetic db/db mouse model[3]. Acute treatment with taspoglutide reduces glucose excursion and increased insulin response during oGTT. In chronically treated rats, glucose excursion and levels of GIP, PYY and triglycerides during oGTT on day 21 are significantly reduced[4]. Hepatic triglyceride levels are significantly reduced in livers from taspoglutide-treated. Taspoglutide does not reduce plaque area or lipid content in the aortic arch or abdominal aorta, and no significant change in aortic macrophage accumulation is detected after taspoglutide or metformin mice[5].