Taspoglutide is an agonist of the glucagon-like peptide 1 receptor (GLP-1R; Ki = 1.1 nM for the human receptor).1 It induces cAMP accumulation in CHO-K1 cells expressing human GLP-1R (EC50 = 0.06 nM). Taspoglutide (1 mg/animal per week) decreases blood levels of glucose and increases blood levels of insulin in an oral glucose tolerance test in Zucker diabetic obese rats. It reduces blood levels of gastric inhibitory polypeptide (GIP), plasma levels of triglycerides, and body weight in the same model.2
References:
[1]. Dong, J.Z., Shen, Y., Zhang, J., et al.Discovery and characterization of taspoglutide, a novel analogue of human glucagon-like peptide-1, engineered for sustained therapeutic activity in type 2 diabetesDiabetes Obes. Metab.13(1)19-25(2011).
[2]. Sebokova, E., Bénardeau, A., Sprecher, U., et al.Taspoglutide, a novel human once-weekly analogue of glucagon-like peptide-1, improves glucose homeostasis and body weight in the Zucker diabetic fatty ratDiabetes Obes. Metab.12(8)674-682(2010).
















