During the past few years, graphene has outstandingly emerged as a key nanomaterial for boosting the performance of commercial, industrial and scientific related technologies. The popularity of this novel nanomaterial in biomedical engineering is due to its excellent biological, electronic, optical and thermal properties that, as a whole, surpass the features of commonly used biomaterials and consequently open a wide range of applications so far within the reach of science fiction. In this minireview, the potential of graphene and its based materials in the expanding biomedical field is highlighted with focus on groundbreaking diagnostic, monitoring and therapeutic strategies. Some of the major challenges related to the synthesis and safety of graphene-based materials are also briefly discussed because of their critical importance in bringing this class of carbon materials closer to the clinic.