Abstract: Drug-induced nephrotoxicity remains a common cause of acute kidney injury （AKI） in hospitalized patients. Among common AKI-associated drugs, antibiotics act as a potential contributor to both structural and functional kidney injury. Antibiotic-related AKI has remained a clinical dilemma. Metabolomics has been evolved rapidly in recent years. Metabolites are end-products of the phenotypes, bridging from gene to physiological and pathological changes of human beings. Elaborating on metabolomics of antibiotics associated with AKI, this review focused upon the novel biomarkers of AKI occurrence and disturbed metabolic pathways.