Abstract: With the development of metabonomics and modern instrumental analysis and bioinformatics, pharmaco-metabonomics has been rapidly put into the diagnosis and treatment of tumor, with a particularly important role in the evaluation and prediction of efficacy, toxicity and resistance of anti-tumor drugs, indivisualized medication and detection of tumor markers. This paper reviews the concept and methodologies of pharmaco-metabonomics, as well as the latest research advances of pharmaco-metabonomics in the diagnosis and freatment of tumors.