AbstractAlthough chemotherapies are successful in some cases, systemic toxicity could be simultaneously observed due to the lack of drugs selectivity to cancerous tissues, leading to the failure of the chemotherapies. Furthermore, the therapeutic effects will be significantly improved if the anticancer drugs could be delivered to cancer cells with high selectivity. In recent years, there have been many advances in the field of diagnosis and treatment of cancer as a result of the development of novel materials with noticeable and often unique properties. Nanoparticles have unique biological properties, owing to their small size and large surface area-to-volume ratio, which allow them to bind, absorb, and carry compounds such as small molecule drugs, DNA, RNA, proteins, and probes with high efficiency. In the course of the last decade, Graphene and its derivatives have attracted growing interest in medicinal and pharmaceutical sciences, and many studies have focused on the potential of Graphene and its derivatives as carriers for targeted drug delivery intended for cancer diagnosis and therapies. In the present study, we will review the characteistics and application of Graphene and its different derivatives and finally discuss the opportunities, limitations, and challenges in this encouraging field.