Malignant tumors are now one of the leading causes of death in humans. Although great progress has been made in the treatment of malignant tumors, chemotherapy remains one of the most important and commonly used means to control tumors and has a crucial position in the field of oncology treatment. The traditional way of chemotherapy drug administration is intravenous drip in oncology wards or outpatient clinics. In recent years, with the launch of new chemotherapy drugs, the types and application fields of oral chemotherapy drugs have been increasing, such as the new oral fluorouracil drugs Siroda and Tegeo for intermediate and advanced gastrointestinal tumors, the new oral tyrosine kinase inhibitor Imatinib for chronic myeloid leukemia and gastrointestinal mesenchymal stromal cell tumors, the new imidazotetrazine class oral chemotherapy agent temozolomide for newly diagnosed glioblastoma multiforme, etc. Several clinical studies have shown that oral chemotherapy drugs do have numerous advantages, including more convenient dosing, better medication compliance, better patient self-management, as well as potential improvement in quality of life, potential reduction in the number of visits and medical resources, etc. They are now increasingly favored by healthcare professionals and patients and their families, and have become a trend in oncology. Currently, there is a common misconception among healthcare professionals and patients and families that the risk of oral chemotherapy drug exposure is very low, there is almost no danger and the drug is safe to use. However, the reality is that although oral chemotherapy drugs are easier to administer, they, like intravenous dosage forms, can also bring drug exposure risks to medical personnel, patients and their families; irregularities in patients’ oral chemotherapy drugs such as improper dosing or insufficient monitoring can lead to low or high doses, serious toxic reactions or complications of diseases, and even cause death. Therefore, it is important to strengthen the safety management of oral chemotherapy drugs. The safety management of oral chemotherapy drugs involves several key areas, such as manufacturers, distributors, medical personnel, patients and caregivers. Manufacturers and distributors should provide appropriate packaging and clinically appropriate dosage forms, prominently display the cytotoxicity of the drug and precautions for administration, and provide educational materials on safety management to facilitate scientific awareness. Patients and caregivers should follow the medical staff’s instructions, keep the drugs in a safe place to avoid deterioration or misuse by children, change the dose or dosing period on their own, monitor blood and liver and kidney functions regularly during the drug administration, and monitor any adverse reactions during treatment, especially in serious cases such as fever, rash, diarrhea, etc. For adverse reactions during treatment, especially serious cases such as fever, rash, diarrhea, etc., contact medical personnel immediately for timely treatment.