Trimetazidine is used for the treatment of angina pectoris, and works as an anti-ischemic metabolic agent. The utilization of myocardial glucose improves through the inhibition of long-chain-3-ketacyl CoA thiolase activity, reducing fatty acid oxidation and stimulating the oxidation of glucose. High rates of fatty acid oxidation can be detrimental during spells of angina due to the possibility of sodium and calcium overload in the heart, causing exacerbation of ischemic injuries and a decrease in cardiac efficiency during reperfusion.

Trimetazidine can react with monamine oxidase inhibitors, but has a high safety and tolerability profile otherwise.