Drug intelligence / Profile preview

rebamipide + esomeprazole

Development stage
Unknown
Lead developer
Otsuka Holdings
Modality
Small Molecules
Administration
Oral
01

Overview

Rebamipide + esomeprazole is a fixed-dose combination therapy used primarily for the treatment of reflux esophagitis and for promoting healing of gastric mucosal injury, including ulcers. Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by irreversibly inhibiting the H+/K+-ATPase enzyme in gastric parietal cells, thereby reducing both basal and stimulated acid production[6]. Rebamipide is a mucosal-protective antiulcer agent that enhances gastric mucosal defense by increasing Prostaglandin E2 (PGE2) synthesis, stimulating mucin secretion, activating Cyclooxygenase 2 (COX-2) expression via ERK1/2 and p38MAPK pathways, and shifting inflammatory signaling toward anti-inflammatory responses[8]. The combination has demonstrated superior efficacy over esomeprazole monotherapy in improving symptoms of reflux esophagitis and accelerating ulcer healing after endoscopic submucosal dissection (ESD)[1][3][4][5]. Rebamipide acts as an adjunct to reduce inflammation and promote tissue repair in the gastrointestinal tract.

02

Targets

PTGS2 (Prostaglandin-Endoperoxide Synthase 2)ATP4A (Potassium–transporting ATPase alpha chain 1)mPGES-2 (Microsomal prostaglandin E synthase-2)

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