Graphene oxide has been widely used in various fields due to its special physical and chemical properties.It is often used as a carrier of antitumor drugs in the treatment of cancer.The surface structure can be purposefully modified to better exert its drug-loading and drug-releasing effects according to its rich surface modification sites.Aiming to provide a theoretical basis for further development of its application in antitumor，this article reviews some of the domestic and foreign research on its structural transformation and its use as a carrier of anticancer drugs.