Nanobiotechnology has huge potential in the field of regenerative medicine. One of the main drivers has been the development of novel nanomaterials. One developing class of materials is graphene and its derivatives recognized for their novel properties present on the nanoscale. In particular, graphene and graphene-based nanomaterials have been shown to have excellent electrical, mechanical, optical and thermal properties. Due to these unique properties coupled with the ability to tune their biocompatibility, these nanomaterials have been propelled for various applications. Most recently, these two-dimensional nanomaterials have been widely recognized for their utility in biomedical research. In this review, a brief overview of the strategies to synthesize graphene and its derivatives are discussed. Next, the biocompatibility profile of these nanomaterials as a precursor to their biomedical application is reviewed. Finally, recent applications of graphene-based nanomaterials in various biomedical fields including tissue engineering, drug and gene delivery, biosensing and bioimaging as well as other biorelated studies are highlighted.