This article reviews the related literature on the reversal of multi-drug resistance in tumors by cepharanthine, and summarizes the reversal effects and mechanisms of multi-drug resistance in different tumors such as leukemia, liver cancer, ovarian cancer, breast cancer, esophageal cancer and colon cancer. Its reversal effect on multi-drug resistance of tumors is the result of a multi-channel, multi-link combination. The main mechanism is to inhibit membrane transporter function, affect enzyme transfer system, inhibit anti-apoptotic pathway activation and anti-apoptotic protein expression.