BACKGROUND AND OBJECTIVE: Acute coronary syndrome (ACS) is a common cardiovascular disease in clinical practice. It is caused mainly by vulnerable plaque rupture (PR) or surface plaque erosion (PE) caused by serious thrombotic events, and eventually leads to myocardial blood supply insufficiency or necrosis. The disease has high morbidity and mortality rates. In this study, we review the literature on biomarkers of ACS metabolites and modification of disease by altering related metabolic pathways through drugs, aiming to provide clarity on potential biomarkers of disease identified to date. METHODS: PubMed was used for literature review. From January 1, 2014 to December 3, 2024, English articles on clinical trials, randomized controlled trials of metabolomics studies in ACS were included. KEY CONTENT AND FINDINGS: In this review, we discuss the advantages and disadvantages of three techniques currently used for metabolomic analysis. In addition, the recent decade of metabolomic approaches to the discovery of potential diagnostic and prognostic biomarkers for ACS is reviewed. It was found that the metabolites changed in patients with ACS were mostly amino acids, lipids and carbohydrates. Tryptophan and glutamine can be used as potential diagnostic biomarkers. Mannitol and ceramide can be used as prognostic biomarkers. Drugs can improve disease by affecting changes in metabolites in the body. CONCLUSIONS: ACS studies based on metabolomics have demonstrated great potential for identifying disease-related metabolomic features in the discovery of potential biomarkers for diagnosis and prognosis and mechanisms of drug therapy.