Abstract： Tuberculosis is a chronic infectious disease that seriously endangers human health. At present, there are still some issues with the diagnosis of tuberculosis, the metabolism of anti-tuberculosis medications, the monitoring of adverse drug reactions, and the evaluation and assessment of therapeutic efficacy. By providing key information on the health or disease status of cells and downstream products of metabolic processes as well as particular tissues or organs, metabolomics is of great value in drug development, disease diagnosis, drug metabolism, monitoring of adverse drug reactions and therapeutic efficacy. Recent studies have shown that using urine metabolomics to explore the metabolic biomarkers of tuberculosis can help distinguish tuberculosis from latent tuberculosis infection as well as differentiate pulmonary tuberculosis from other pulmonary diseases, providing an important basis for the diagnosis of tuberculosis. Urine metabolomics is used to study the metabolism of anti-tuberculosis drugs and the mechanism of adverse reactions, providing an important tool for drug research and development as well as the monitoring of adverse reactions. In addition, urine metabolomics analysis is also important for assessing the severity of tuberculosis and its treatment outcome. This article reviewed the application of urine metabolomics in diagnosis of tuberculosis, the metabolism of anti-tuberculosis drugs, the monitoring of anti-tuberculosis drugs adverse reactions, and the assessment and judgement of therapeutic efficacy.