Somatostatin is a peptide hormone secreted from the pituitary gland, pancreas, and gastrointestinal endocrine cells and regulates secretion of endocrine hormones via five G-protein-coupled receptors (SSTR1-5). Among these, SSTR5 is primarily expressed in pancreatic ß-cells and enteroendocrine cells, both of which secrete insulin and gut hormones. Somatostatin binding to SSTR5 inhibits the secretion of insulin and gut hormones, including glucagon-like peptide-1
(GLP-1) and peptide YY, which are pivotal in metabolic control.

SCO-240, identified by SCOHIA researchers and collaborators, is an orally available, selective SSTR5 antagonist and is unique owing to its dual action of elevating hormone secretions and increasing insulin sensitivity. SSTR5 antagonism effectively stimulates insulin and GLP-1 secretion, increases insulin sensitivity, and improves glycemic control in preclinical diabetic models. Considering its dual action, SCO-240 may be a novel alternative for the treatment of diabetes.

In addition, SCO-240 is effective in stimulating gallbladder motility and increasing bile flow, accounting for its therapeutic effects in animal models of gallstones and primary sclerosing cholangitis. Thus, an additional potential application of SCO-240 involves treatment of hepatobiliary diseases.

Studies developing investigational new drugs are ongoing for a Phase 1 study.

Indication

  • Diabetes
  • Gallstones
  • Primary sclerosing cholangitis
  • etc
  • Activation
  • Benefits
  • Inhibition
Somatostatin
SCO-240
SSTR5

Liver, muscle, etc

Liver, muscle, etc

Insulin resistance

Pancreas

Pancreas

Insulin secretion

Intestine

Intestine

CCK secretion

GLP-1 secretion

Gallbladder

Gallbladder

Gallbladder
motility

Bile flow

Hyperglycemia

Gallstones

Cholestasis

GLP-1 : Glucagon-like peptide 1

CCK : Cholecystokinin