Graphene is a two-dimensional nanomaterial composed of carbon atoms with sp2 hybrid orbitals. Both graphene and graphene-based composite have gained broad interest among researchers because of their outstanding physiochemical, mechanical, and biological properties. Graphene production techniques are divided into top-down and bottom-up synthesis methods, of which chemical vapor deposition (CVD) is the most popular. The biomedical applications of graphene and its composite include its use in sensors, implantology, and gene and drug delivery. They can be used for tissue engineering, anticancer therapies, and as antimicrobial agents in implant application. The biocompatibility of graphene-based nanomaterials enables their use in the field of biomedicine. This article reviews the properties of graphene, the methods used to produce it, the challenges associated with its use, and the potential applications of this material in biomedicine, regenerative medicine, and drug delivery systems.