Graphene- and graphene oxide-based nanomaterials have gained broad interests in research because of their unique physical, chemical, and mechanical properties. The 2D allotropic structure allows it to be used in various biological fields. The biomedical applications of graphene and its composite include its use in gene and small molecular drug delivery. It is further used for bio functionalization of protein, in anticancer therapy, as an antimicrobial agent for bone and teeth implantation. The biocompatibility of the newly synthesized nanomaterials allows its substantial use in medicine and biology.