GPR40 is a G-protein-coupled receptor (GPCR) activated by endogenous ligands of medium-to-long chain fatty acids. GPR40 is expressed in pancreatic beta-cells and enteroendocrine cells, and it physiologically regulates the secretion of insulin, glucagon-like peptide-1 (GLP-1), and glucose-dependent insulinotropic polypeptide (GIP). The strategy to increase insulin secretion, and the activities of GLP-1 and GIP agonism, would be effective in improving diabetes and obesity in humans; hence, GPR40 seems to be highly attractive as a new class of drug for these patients.

GPR40 has three independent small-molecule binding sites. Fasiglifam, a GPR40 partial agonist, binds to one site of these pockets and markedly improves glycemic control by increasing insulin secretion in patients with type 2 diabetes.

SCO-267, identified by SCOHIA researchers and collaborators, is a GPR40 full agonist, which has a new chemical structure and binds to a site independent of the fasiglifam binding site. Contrary to GPR40 partial agonists, which increase insulin secretion only, a GPR40 full agonist such as SCO-267 is unique in that it increases the production of islet hormones and gut hormones.

In a Phase 1 study, a single dose of SCO-267 stimulated islet and gut hormones and remarkably improved glucose tolerance in diabetic patients.

In preclinical studies, SCO-267 increases the levels of GLP-1, GIP, and peptide YY, and thus, decreases body weight in obesity models. In addition to these hormones, SCO-267 increases insulin secretion and improves glucose control more effectively than GPR40 partial agonists and dipeptidyl peptidase-4 inhibitors. Furthermore, SCO-267 increases the secretion of glucagon, which has a major role in liver metabolism and function, and improves liver parameters in preclinical models with liver-dysfunctions.

Based on these observations, SCO-267 may be a new drug option for the treatment of diabetes, obesity, and non-alcoholic steatohepatitis. Moreover, a Phase 2 study is in preparation.

SCOHIA is actively seeking partnerships worldwide for the development and commercialization of SCO-267 (Contact here for partnering).


  • Diabetes
  • Obesity
  • Nonalcoholic steatohepatitis (NASH)
  • Activation
  • Benefits



Insulin secretion

Glucagon secretion






Blood glucose level

Body weight

GLP-1 : Glucagon-like peptide 1

PYY : Peptide YY

GIP : Glucose-dependent insulinotropic polypeptide