GASTROPROTECTIVE PROPERTIES OF EBROTIDINE - A REVIEW

Ebrotidine ethyl]amino]methylene]-4-bromo-benzenesulfonamide, CAS 1009 81-43-9, FI-3542) is a new antiulcer drug which combines the propertie s of an H-2-receptor antagonist with those of a cytoprotective agent. The cytoprotective properties of ebrotidine are not dependent upon end ogenous prostaglandin generation, but stem from the ability of the dru g to induce mucosal responses manifested in the enhanced physicochemic al characteristics of mucus gel. These include the increase in mucus g el dimension, viscosity, hydrophobicity and hydrogen ion retardation c apacity. Improvements in mucus gel protective qualities with ebrotidin e are directly related to the ability of the drug to enhance the synth esis and secretion of sulfo- and sialomucins and phospholipids of gast ric mucus and to promote mucin macromolecular assembly. An equally imp ortant property of ebrotidine in promotion of ulcer healing is its cap ability to enhance the gastric mucosal expression of integrin receptor s for the interaction with proteins of the extracellular matrix such a s laminin. Furthermore, the accelerated ulcer healing with ebrotidine is reflected in a marked increase in the mucosal expression of EGF and PDGF receptors. The drug has also been shown to modulate the processe s associated with cell cycle progression during ulcer healing, and is known to protect the gastric epithelial integrity from calcium imbalan ce. Thus, ebrotidine, unlike other H-2-blockers, has a unique ability to promote the event essential for mucosal repair and the maintenance of mucosal integrity. These features make ebrotidine a drug of great p otential in the treatment of ulcer disease.