As an important component of functional genomics, gene expression profiling plays an important role in many fields such as biology, medicine and drug development. Especially with the concept of precision medicine, integrating multi-omics data including gene expression profiles for personalized medicine is a future trend. From the background of anticancer drug development, the big data analysis method based on cellular perturbation expression profiling is introduced, and its application in anticancer covenant development is summarized. The findings suggest that continuous improvement of these methods will drive the discovery of novel biomarkers that can predict drug efficacy and toxicity, thereby accelerating the drug development process and improving patient prognosis. In the future, gene expression profiling is expected to be widely used in clinical practice, changing the landscape of cancer management and ushering in a new era of individualized cancer treatment that will achieve superior efficacy with fewer side effects than ever before.