Drug intelligence / Profile preview

rebamipide

Development stage
Phase 4
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
Oral, Ophthalmic
01

Overview

Rebamipide is a small molecule gastroprotective agent primarily used for the treatment of gastric ulcers, gastritis (including acute and chronic forms), and mucosal lesions caused by nonsteroidal anti-inflammatory drugs (NSAIDs). It is also indicated for oral mucositis and has been investigated for other conditions such as keratoconjunctivitis sicca, recurrent aphthous ulcers, Behcet’s syndrome, and early gastric cancer. Rebamipide acts through multiple mechanisms: it stimulates prostaglandin generation in the gastric mucosa, increases mucus glycoprotein content, enhances blood flow to ischemic tissue via nitric oxide synthase activity, scavenges reactive oxygen species (free radicals), inhibits neutrophil adhesion molecules and inflammatory cytokines like TNF-α, downregulates 15-hydroxyprostaglandin dehydrogenase to increase protective prostaglandins (PGE2/PGI2), promotes epithelial cell migration/proliferation, and upregulates epidermal growth factor (EGF) expression to accelerate healing. These actions collectively protect the gastric lining from injury due to acid or NSAIDs and promote ulcer healing[1][4][5][6][7][8].

Brand names
Mucosta
Other names
mucotra
02

Targets

PTGER4 (Prostaglandin E2 receptor EP4 subtype)NLRP3 (Nod-like receptor family pyrin domain-containing protein 3)EGFR (Epidermal growth factor receptor)αMβ2 (Integrin αMβ2)TNFA (Tumor necrosis factor alpha (soluble))

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