Drug intelligence / Profile preview

roxatidine

Development stage
Unknown
Lead developer
Astellas Pharma
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Roxatidine is a potent and selective histamine H2-receptor antagonist that acts as a competitive inhibitor of basal and stimulated gastric acid secretion by blocking H2 receptors on parietal cells in the stomach. This results in reduced production and secretion of gastric acid, with a dose-dependent reduction in total pepsin secretion. Roxatidine also exhibits independent mucosal protective effects. It is indicated for the treatment of peptic ulcer, gastroesophageal reflux disease (GERD), gastritis, upper gastrointestinal hemorrhage, Zollinger-Ellison syndrome, and can be used as premedication before anesthesia. After oral administration (as the prodrug roxatidine acetate), it is rapidly converted to its active form by esterases in the small intestine, plasma, and liver[1][2][5]. Roxatidine has no antiandrogenic effects or significant influence on hepatic drug-metabolizing enzymes[2][5].

Brand names
Roxit
Other names
roxatidine acetate hydrochloride
02

Targets

HRH2 (Histamine H2 Receptor)

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