Abstract: Cancer chemotherapy have successfully applied on oncology. During caner chemotherapy, different reactions have been observed in both the response and toxicity associted with large individual related gene variations. Individual therapy under the guidance of anti-tumor agents related genes is one of the most promising directions for clinical cancer treatment. This review introducing five genes associated with the response and toxicity of cancer chemotherapy provides an overview of the progress made in the field of genetics in cancer agents: ①DPD gene mutations and severe 5-Fu toxicity; ②EGFR gene mutations and responsiveness of NSCLC to Gefitinib and Erlotinib; ③ERCC1 polymorphisms and activity of cisplatin; ④UGT1A1 genetic variation and hydroxycamptothecine toxicity and ⑤TS gene polymorphisms and 5-FU sensitivity, to explore ways to predict response and adverse reactions and guide clinical personalized treatment of anti-tumor agents.