Drug intelligence / Profile preview

somatostatin

Development stage
Phase 4
Lead developer
Novartis
Modality
Peptides, Recombinant Proteins and Enzymes
Administration
Intravenous
01

Overview

Somatostatin is a natural peptide hormone produced by the hypothalamus and other tissues such as the pancreas and gastrointestinal tract. It acts as a universal inhibitor of endocrine and exocrine secretion throughout the body. Somatostatin inhibits the release of several hormones including growth hormone (GH), thyroid-stimulating hormone (TSH), insulin, glucagon, gastrin, secretin, motilin, cholecystokinin (CCK), vasoactive intestinal peptide (VIP), gastric inhibitory polypeptide (GIP), prolactin (PRL), neurotensin, pancreatic polypeptide (PP) and others[1][2][5][8]. It also suppresses exocrine secretions from salivary glands and gastrointestinal mucosa as well as enzymes from the pancreas[8]. Somatostatin reduces blood flow in the splanchnic circulation and decreases gastric acid secretion by direct inhibition of parietal cells[6]. Its mechanism involves binding to five subtypes of Gi-protein-coupled somatostatin receptors (SSTR1-5). Activation of these receptors leads to inhibition of adenylyl cyclase activity, reduced cyclic AMP levels, decreased calcium influx via voltage-gated channels, activation of phosphotyrosine phosphatase pathways and modulation of MAP kinase signaling—resulting in broad suppression of cellular secretion[1]. Clinically it is used for acute bleeding from esophageal varices or GI ulcers; prevention or treatment of pancreatic complications after surgery; restriction of upper GI/pancreatic/biliary secretions; management or diagnosis in certain neuroendocrine tumors; and sometimes for acromegaly or pituitary adenomas when analogs are not available[1][2].

Brand names
Stilamin
Other names
growth hormone-inhibiting hormoneGHIHSRIFSST
02

Targets

SSTR5 (Somatostatin receptor 5)SSTR3 (Somatostatin receptor 3)SSTR1 (Somatostatin Receptor Type 1)SSTR2 (Somatostatin receptor type 2)SSTR4 (Somatostatin receptor 4)

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