Drug intelligence / Profile preview

itopride

Development stage
Phase 4
Lead developer
Abbott
Modality
Small Molecules
Administration
Oral
01

Overview

Itopride is a prokinetic benzamide derivative used primarily for the treatment of functional gastrointestinal disorders such as functional dyspepsia, chronic gastritis, and symptoms like gastric fullness, rapid satiation, upper abdominal pain or discomfort, anorexia, heartburn, nausea, and vomiting. It acts as both a dopamine D2 receptor antagonist and an acetylcholinesterase inhibitor. By blocking dopamine D2 receptors in the gastrointestinal tract and inhibiting acetylcholinesterase activity, itopride increases acetylcholine concentrations at neuromuscular junctions in the gut. This dual action enhances gastrointestinal motility by stimulating smooth muscle contraction via muscarinic M3 receptors and removing inhibitory dopaminergic effects on motility. Itopride does not significantly cross the blood-brain barrier due to its high polarity and is not associated with central nervous system adverse effects or QT interval prolongation. The drug is approved in several countries including Japan and Mexico but is not approved in the USA or UK[1][2][4][5][6].

Brand names
Ganaton
Other names
N-(p-(2-(Dimethylamino)ethoxy)benzyl)veratramide
02

Targets

AcetylcholinesteraseDRD2 (Dopamine D2 Receptor)

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