Graphene and its derivative materials present high potential towards medical and biological applications, including drug delivery and bioimaging, due to their exceptional properties such as thermal conductivity and high specific surface area. The main focus of this work is to review the current development of graphene materials and the derivatives for biocompatible, bioimaging and drug delivery applications. Also, the synthesis methods with variation of graphene nanocomposites and the functionalisation will be further explained. For the graphene approaches, chemical vapour deposition (CVD) is the best-known technique to make high-quality graphene sheet by growth route with mass production. By considering the organic graphene nanocomposites, the biocompatibility and cytotoxic effects against graphene nanocomposites were evaluated for biomedical employments such as high quality bioimaging and effective drug delivery for cancer treatments. For example, graphene oxide incorporated with PEG and loaded with SN 38 for camptothecin analolgue as anticancer drug and revealed high cytotoxicity has an effect of 1000 times better effect than CPT in HCT-116 cells. Their drug delivery ability for both in-vivo and in-vitro applications compared to the controlled drugs such as doxorubicin (DOX) will be discussed accordingly. The graphene and its deriavatives possess some intriguing properties, which will lead to drug delivery due to strong biocompatibility and cyctotoxic effect towards biomedicine applications.