Cancer stands out as the primary cause of mortality globally. The variety of cancer-causing cells and their ability to adapt to the normal cellular milieu substantially complicates the treatment of cancer. Traditional cancer treatments encounter numerous constraints, including considerable side effects, insufficient efficacy and poor selectivity. This highlights the persistent demand for precise and efficient anticancer drug delivery vehicles capable of transporting therapeutic drugs specifically to targeted locations within the body. Through a comprehensive analysis of various drug delivery vehicles, multiple challenges have been identified. Nevertheless, years of in-vitro and in-vivo research, along with insights from experts around the globe, have spurred the evolution of nanotechnology-based cancer therapeutics. Among these advancements, nanocomposites derived from carbon allotropes and biopolymers have garnered significant interest owing to their non-toxic characteristics, substantial surface area for drug interaction and exemplary biocompatibility. In particular, nanocomposites composed of graphene oxide (GO) and chitosan (CS) have emerged as a significant area of focus in cancer research. By scrutinizing the findings of a plethora of research published over the past ten years, this comprehensive review delves into the recent advancements that have materialized in the field of cancer research utilizing chitosan-functionalized graphene oxide (CS/GO) nanocomposites as drug delivery vehicles. This review explores the various types of CS/GO nanovehicles, their preparation methods and modifications including functionalization with metals, polymers and biomolecules. We have also provided an in-depth analysis of the drug loading efficiency, its analytical evaluation and the key factors influencing it. Significant attention is directed towards understanding various drug release mechanisms, with a particular focus on pH-triggered stimuli-controlled release and the mathematical models employed to characterize drug release dynamics. Additionally, we have assessed the cytotoxicity and biocompatibility of CS/GO nanovehicles, which are critical considerations for guaranteeing safe and effective therapeutic outcomes. We assert that our review will serve as a strategic paradigm for researchers, offering an overview of the current landscape, addressing opportunities and challenges ahead and ultimately delineating sustainable prospective research goals focused on the drug delivery applications of CS/GO nanocomposites.