Lipidomics, a newly emerged branch of metabolomics, is aimed to systemically study the characters of lipid molecular species in organisms and their roles in regulating protein and gene expression. Lipids play diverse biological roles in organisms, including energy storage, signal transduction and apoptosis. Owning to the rapid progression of novel analytical technique, especially the application of mass spectrometry, lipid examination can be done rapidly and accurately in a high throughput manner. Many studies have demonstrated that abnormal metabolism of lipids is closely related to the development and progression of tumors. Application of lipidomics technique can reveal the changes of tumor-associated lipid and identify the abnormal metabolic pathways. Also, lipidomics has a promising future in recognition of lipid-based tumor markers, early diagnosis of tumors and the discovery of antineoplastic drug targets. In this article, we reviewed the recent progress in the above-mentioned areas.