Drug intelligence / Profile preview

meldonium

Development stage
Phase 4
Lead developer
Grindeks
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

Meldonium is a small molecule drug primarily used in Eastern Europe and Central Asia for the treatment of cardiovascular and metabolic conditions such as angina, heart failure, myocardial infarction, arrhythmia, atherosclerosis, and diabetes. It is also prescribed for neurological disorders and problems with cerebral circulation[1][4][8]. Meldonium acts as an anti-ischemic agent by inhibiting fatty acid oxidation through competitive inhibition of gamma-butyrobetaine hydroxylase (GBB), an enzyme involved in carnitine biosynthesis[1][6][8]. By reducing carnitine levels and blocking fatty acid metabolism—which requires high oxygen consumption—meldonium shifts cellular energy production toward glycolysis and glucose metabolism pathways that are more oxygen-efficient. This mechanism helps restore the balance between oxygen supply and demand in ischemic tissues[6]. Meldonium was developed in Latvia by Grindeks. It is not approved for use in the United States but remains widely used elsewhere under various brand names. The drug has gained notoriety due to its inclusion on the World Anti-Doping Agency’s list of banned substances because of its potential performance-enhancing effects[5].

Brand names
MildronateMildronātsQuaterine
Other names
trimethylhydrazinium propionate3-(2,2,2-trimethylhydraziniumyl)propionate
02

Targets

SLC22A5 (Organic cation/carnitine transporter 2)BBOX1 (Gamma-butyrobetaine dioxygenase)

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