This review (with 239 refs.) summarizes the progress that has been made in applications of graphene-based nanomaterials (such as plain graphene, graphene oxides, doped graphene oxides, graphene quantums dots) in biosensing, imaging, drug delivery and diagnosis. Following an introduction into the field, a first large section covers the toxicity of graphene and its derivatives (with subsections on bacterial toxicity and tissue toxicity). The use of graphene-based nanomaterials in sensors is reviewed next, with subsections on electrochemical, FET-based, fluorescent, chemiluminescent and colorimetric sensors and probes. The large field of imaging is treated next, with subchapters on optical, PET-based, and magnetic resonance based methods. A concluding section summarizes the current status, addresses current challenges, and gives an outlook on potential future trends. Graphical Abstract Schematic presentation of the potential applications of graphene-based materials in life science and biomedicine, emphatically reflected in some vital areas such as DNA analysis, biological monitoring, drug delivery, in vitro labelling, in vivo imaging, tumor target, etc.