The synthesis of a drug delivery platform based on graphene was achieved through a step-by-step strategy of selective amine deprotection and functionalization. The multifunctional graphene platform, functionalized with indocyanine green, folic acid, and doxorubicin showed an enhanced anticancer activity. The remarkable targeting capacity for cancer cells in combination with the synergistic effect of drug release and photothermal properties prove the great advantage of a combined chemo- and phototherapy based on graphene against cancer, opening the doors to future therapeutic applications of this type of material.