Graphene nanomaterials have been considered as a novel class of nanomaterials that show exceptional structural, optical, thermal, electrical, and mechanical properties. As a consequence, it has been extensively studied in various fields including electronics, energy, catalysis, sensing, and biomedical fields. In the previous couple of years, a significant number of studies have been done on graphene-based nanomaterials, where it is utilized in a wide range of bioapplications that includes delivery of small molecule drugs/genes, biosensing, tissue engineering, bioimaging, and photothermal and photodynamic therapies because of its excellent aqueous processability, surface functionalizability, outstanding electrical and mechanical properties, tunable fluorescence properties, and surface-enhanced Raman scattering (SERS).Therefore, it is necessary to get detailed knowledge about it. In this review, we will highlight the various synthesis procedures of graphene family nanomaterials including graphene oxide (GO), reduced graphene oxide (rGO), and graphene quantum dots (GQDs) as well as their biomedical applications. We will also highlight the biocompatibity of graphene nanomaterials as well as its possible risk factors for bioapplications. In conclusion, we will outline the future perspective and current challenges of graphene nanomaterials for clinical applications. © Copyright 2018 American Chemical Society.