Gastrin
Overview
Gastrin is an endogenous peptide hormone secreted by G-cells in the gastric antrum and duodenum, existing primarily as gastrin-17 and gastrin-34. It binds to the CCK-2 receptor on parietal and enterochromaffin-like cells, stimulating gastric acid secretion and promoting gastric mucosal growth. Therapeutic applications have focused on gastrin analogs for diagnostic purposes and investigation of gastrin immunotherapy for gastrin-dependent tumors. Dysregulation of gastrin secretion occurs in conditions such as Zollinger-Ellison syndrome and atrophic gastritis.
Key Research Findings
Pentagastrin, a synthetic gastrin analog, was historically used for diagnostic gastric acid secretion testing but has been largely replaced by other methods. Gastrin immunotherapy approaches targeting gastrin or the CCK-2 receptor have been explored in preclinical models of gastric and pancreatic cancers with limited clinical translation. No gastrin-based peptide therapeutic is currently in active clinical development for gastrointestinal indications.
Subcutaneous injection, Intravenous
Research Phase
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Octreotide (Sandostatin)
FDA ApprovedA synthetic octapeptide analog of somatostatin with a substantially longer half-life (90 minutes IV, 6 hours subcutaneous vs. 2 minutes for native somatostatin). Octreotide binds somatostatin receptors (primarily SSTR2 and SSTR5) to inhibit the secretion of GH, glucagon, insulin, gastrin, secretin, VIP, and other GI hormones. It reduces splanchnic blood flow, GI motility, and exocrine pancreatic secretion.
Lanreotide (Somatuline Depot)
FDA ApprovedA synthetic octapeptide analog of somatostatin with high affinity for SSTR2 and moderate affinity for SSTR5 receptors. Lanreotide is formulated as a supersaturated solution that forms a drug depot at the injection site, providing sustained release over 4 weeks. It inhibits GH secretion, GI hormone release, and has direct antiproliferative effects on neuroendocrine tumor cells through cell cycle arrest and apoptosis induction.
Pasireotide (Signifor)
FDA ApprovedA multireceptor-targeted somatostatin analog with high binding affinity for SSTR1, SSTR2, SSTR3, and SSTR5, particularly notable for its 40-fold greater affinity for SSTR5 compared to octreotide. This receptor profile makes pasireotide uniquely effective in Cushing's disease, where corticotroph adenomas predominantly express SSTR5. Pasireotide suppresses ACTH secretion from pituitary corticotroph tumors, reducing cortisol production.
Plecanatide (Trulance)
FDA ApprovedA synthetic 16-amino acid peptide structurally related to uroguanylin, an endogenous intestinal peptide that regulates fluid and electrolyte homeostasis in the GI tract. Plecanatide activates guanylate cyclase-C (GC-C) receptors on intestinal epithelial cells in a pH-dependent manner, preferentially in the proximal small intestine where pH is slightly acidic. GC-C activation increases intracellular and extracellular cGMP, stimulating chloride and bicarbonate secretion while reducing visceral pain signaling.