Abstract: Graphene derivatives generated by modifying the surface oxygen functional groups of graphene oxide have been widely investigated in recent years. Graphene derivatives possess excellent aqueous solubility and biocompatibility similar to graphene oxide, which are important in their biomedical application. Research progress on the use of graphene derivatives in biological imaging, drug carriers and photodynamic therapy of cancer is presented. Future efforts to improve their performance in cancer therapy are also proposed, such as lowering the toxic effects introduced by chemicals used in the preparation of the graphene derivatives, expanding the drug to include genes and proteins, and coupling photodynamic therapy with imaging.