OICC Press Journal of Nanostructure in Chemistry 2193-8865 12 5 (October 2022) 2021 09 06 Graphene and its derivatives: understanding the main chemical and medicinal chemistry roles for biomedical applications 10.1007/s40097-021-00444-3 EN Tais Monteiro Magne Brazilian Nuclear Energy Commission, Nuclear Engineering Institute, Rio de Janeiro, 21941906, BR Thamires de Oliveira Vieira Brazilian Nuclear Energy Commission, Nuclear Engineering Institute, Rio de Janeiro, 21941906, BR Luciana Magalhães Rebelo Alencar Biophysics and Nanosystems Laboratory, Department of Physics, Federal University of Maranhão, São Luis, Maranhão, 65080805, BR Francisco Franciné Maia Junior Department of Natural Sciences, Mathematics and Statistics, Federal Rural University of the Semi-Arid, Mossoró, RN, 59625-900, BR Sara Gemini-Piperni Laboratory of Advanced Science, Universidade Unigranrio, Duque de Caxias, RJ, 25071-202, BR Samuel V. Carneiro Group of Chemistry of Advanced Materials (GQMat)-Department of Analytical Chemistry and Physic-Chemistry, Federal University of Ceará-Campus do Pici, Fortaleza, Ceará, 60451-970, BR Lillian M. U. D. Fechine Group of Chemistry of Advanced Materials (GQMat)-Department of Analytical Chemistry and Physic-Chemistry, Federal University of Ceará-Campus do Pici, Fortaleza, Ceará, 60451-970, BR Rafael M. Freire Institute of Applied Chemical Sciences, Universidad Autónoma de Chile, Santiago, 8910060, CL Kirill Golokhvast Education and Scientific Center of Nanotechnology, School of Engineering, Far Eastern Federal University, Vladivostok, RU N.I. Vavilov All-Russian Institute of Plant Genetic Resources, Saint-Petersburg, RU Pierangelo Metrangolo Laboratory of Supramolecular and Bio-Nanomaterials, Department of Chemistry, Materials, and Chemical Engineering “Giulio Natta” Politecnico Di Milano, Milano, 20131, IT Pierre B. A. Fechine Group of Chemistry of Advanced Materials (GQMat)-Department of Analytical Chemistry and Physic-Chemistry, Federal University of Ceará-Campus do Pici, Fortaleza, Ceará, 60451-970, BR Ralph Santos-Oliveira Brazilian Nuclear Energy Commission, Nuclear Engineering Institute, Rio de Janeiro, 21941906, BR Laboratory of Nanoradiopharmacy and Synthesis of Radiopharmaceuticals, Zona Oeste State University, Rio de Janeiro, 2100000, BR Journal Article 2021 09 06 Abstract Over the past few years, there has been a growing potential use of graphene and its derivatives in several biomedical areas, such as drug delivery systems, biosensors, and imaging systems, especially for having excellent optical, electronic, thermal, and mechanical properties. Therefore, nanomaterials in the graphene family have shown promising results in several areas of science. The different physicochemical properties of graphene and its derivatives guide its biocompatibility and toxicity. Hence, further studies to explain the interactions of these nanomaterials with biological systems are fundamental. This review has shown the applicability of the graphene family in several biomedical modalities, with particular attention for cancer therapy and diagnosis, as a potent theranostic. This ability is derivative from the considerable number of forms that the graphene family can assume. The graphene-based materials biodistribution profile, clearance, toxicity, and cytotoxicity, interacting with biological systems, are discussed here, focusing on its synthesis methodology, physicochemical properties, and production quality. Despite the growing increase in the bioavailability and toxicity studies of graphene and its derivatives, there is still much to be unveiled to develop safe and effective formulations. Graphic abstract