Abstract: Some applications of mass spectrometry in new developing drugs investigation, including synthesis procedure, corroboration of chemical structure, quality control and drug metabolism are reviewed. The research progress of various instruments such as typical matrix-assistant laser desorption ionization time-of-flight mass spectrometry (MALDI/TOFMS), electrode spray ionization mass spectrometry (ESI-MS) and their technologies used together in biomacromolecule drugs, identification of protein, polypeptide, amino acid, DNA, RNA are summarized. Meanwhile, the broad prospects in mass spectrometry in living science are viewed.