The object of expression proteomics is to define and quantify all proteins within a cell or subcellular organelle under normal，diseased or drug-treated conditions． In the recent years，expression proteomics plays a role in the research and development of anti-cancer drugs． Herein，we referred and summarized the relevant literature，and introduced the expression proteomics used for the research and development of anti-cancer drugs，including discovery of new targets，clarification of action mechanisms of drugs，clinical diagnosis，and the realization of drug development concept based on the network pharmacology． Although expression proteomics itself still has some flaws，it has a broad prospect of application and will greatly promote the research and development of innovative anti-cancer drugs．