The incidence of gastric mucosal injury has been increasing rapidly because nonsteroidal anti-inflammatory drugs (NSAIDs) and antithrombotic agents are being increasingly prescribed, especially to elderly patients. Several approaches for gastric mucosa defense have been adopted for the prevention and cure of gastropathy, including gastric ulcers. Zinc l-carnosine is used for the treatment of gastric mucosal damage disease. Zinc l-carnosine (or polaprezinc) is a chelated compound that consists of l-carnosine and zinc. Zinc l-carnosine protects the mucosa against aggressive injury factors and has been found to prevent gastric mucosal injury in diverse experimental models through anti-inflammatory action, antioxidant action, growth factors, and cytoprotective factors such heat-shock proteins. Zinc l-carnosine is effective in treating Helicobacter pylori infection, NSAID-induced gastric injury, ethanol-induced gastropathy, and acetic acid-gastric damage. In conclusion, zinc l-carnosine is a valuable mucosal protective agent with multiple targets that can be used in gastric mucosal damage healing.