Because of great diversity of chemical and physical properties and wide ranges of concentrations of different metabolites in metabolome samples, metabolome analysis is a challenging task. Compromises in coverage, quantification accuracy and sample throughput are often used to provide a sufficient amount of metabolomic information for a biological or clinical application. Chemical derivatization of metabolites offers an opportunity to improve the overall analytical performance of liquid chromatography mass spectrometry (LC-MS)-based metabolomics. This review highlights recent progresses (since 2016) in the field of chemical derivatization LC-MS for both targeted and untargeted metabolome analysis. Due to increased recognition of the benefits of derivatization in LC-MS metabolome analysis, many research groups have been involved in advancing this active research field. Due to space limitation, we selected a few examples of recently reported derivatization methods and applications to showcase the advantages of chemical derivatization, compared to conventional label-free methods. •Metabolome analysis is not easy due to chemical/physical diversity of metabolites.•Derivatization can improve metabolite separation, detection and identification.•Labeling reagents targeting different chemical groups have been reported.•Performance of reagents for targeted and untargeted metabolomics varies greatly.•Improved performance often outweighs the inconvenience of doing derivatization.