Pharmacogenomics has laid a critical foundation for the development of novel anti-tumor drugs and individualized precision therapy by identifying gene variants and targets related to drug response. In the development of anti-cancer drugs, the application of techniques such as genome-wide association studies and whole exome sequencing has provided important avenues for the identification of new drug targets. Genotypic stratification of patients makes the design of clinical trials of new drugs more accurate, not only shortening trial duration and reducing costs,but also improving the accuracy of clinical efficacy evaluation, thereby reducing the risk of drug development failure. Looking forward to the future, with the continuous progress of sequencing technology, pharmacogenomics based on multi-gene analysis will play an increasingly significant role in anti-tumor drug development. However, how to fully tap the potential of these technologies and strengthen the collaborative cooperation between clinical, scientific research and industry is still the core issue to be solved in the process of pharmacogenomics to help the development of anti-tumor drugs.