<p>Graphene, a sp²-hybridized carbon structure, is a two-dimensional (2D) sheet with excellent mechanical, electronic, thermal, and optical properties. Its biocompatibility and large specific surface area have drawn researchers to biomedical research. Despite its exceptional properties, graphene exhibits some degree of toxicity, primarily attributed to mechanisms such as oxidative stress, physical membrane disruption, inflammatory responses, and DNA damage, depending on its physicochemical properties like surface functionalization, size, and concentration. To address this challenge and leverage its potential in biomedicine, researchers have explored strategies to modulate its biocompatibility. These strategies involve covalent or non-covalent functionalization of graphene with moieties that enhance its biocompatibility. Examples include graphene oxide (GO) and reduced graphene oxide (rGO), which exhibit altered surface chemistries compared to pristine graphene. This review highlights various applications of graphene and graphene-based nanomaterials, such as GO, rGO, and graphene quantum dots, which have been used in biomedical science and healthcare. These applications include imaging and diagnostics, drug discovery, drug delivery systems, tissue engineering, and biosensing bioelectronic devices. Finally, an overview of the challenges and future prospects is presented.</p> Graphical Abstract <p></p>