Amidst the myriad of drug delivery systems able to enhance delivery, absorption and intracellular uptake of a bioactive molecule while protecting it from deactivation, Carbon Nanotubes (CNTs) have emerged as a recent and promising option especially in cancer therapy. This is mainly due to their unique properties, which render them extremely versatile through the incorporation of several functional groups and targeting molecules at the same time, while their natural shape allows them to selectively penetrate across biological barriers in a non-invasive way. In this expert review we aim to evaluate whether this innovative material, once chemically-modified with suitable functionalizations, can be considered as a valuable system in comparison to the already existing nanodevices. This will include the estimation of the most recent advances in the field of nanotechnology, together with a cautious evaluation of potential risks and hazards associated with the extensive use of this fascinating, but still unknown, nanomaterial.