The article is devoted to synthesis, characterisation and complex investigation of biocompatibility and cytotoxicity of graphene oxide conjugate with folic acid and cytarabine cytostatic (GO-FA-Cyt). GO was synthesised using a patented modified Hummers and Offeman's method leading to the production of GO enriched with oxygen-containing functional groups (⁓85%). Obtained nanomaterial was covalently modified with FA and non-covalently functionalised with Cyt and characterised using 13C NMR, Raman, and IR spectroscopy, XRD and DLS for aqueous dispersions. Biocompatibility and biological activity studies included investigation of haemocompatibility, antioxidant activity, genotoxicity, and cytotoxicity towards Jurkat, HL60 cell lines. The kinetic dependence of the adsorption of Cyt on the covalent GO-FA conjugate was obtained and described using various models: Brunauer, Emmett and Teller, Langmuir. Experimental data on release were fitted using zero-order, first-order and Korsmeyer–Peppas models. © 2024