Lidocaine, as an amide anesthetic, has been widely used in clinical anesthesia and treatment of arrhythmia. Studies have shown that lidocaine exhibited anti‑inflammatory, anti‑bacterial and analgesic effects. Meanwhile, lidocaine exhibited significant anti‑tumor activities against a variety of tumor cells，and can inhibit the development of many cancers，such as breast cancer, lung cancer, liver cancer, gastric cancer, colorectal cancer, cervical cancer, and ovarian cancer. This review summarizes the anti‑tumor mechanisms of lidocaine, including induction of tumor cell apoptosis, inhibition of tumor cell migration, invasion and proliferation, synergistic sensitization of chemotherapy drugs and sensitization hyperthermia, so as to provide useful reference for further study.