Despite the current progresses of modern medicine, the resistance of malignant tumors to present medical treatments points to the necessity of developing new therapeutic approaches. In recent years, numerous studies have focused their attention on the promising use of nanomaterials, like iron oxide nanowires, zinc oxide or mesoporous silica nanoparticles, for cancer and metastasis treatment with the advantage of operating directly at the bio-molecular scale. Among them, carbon nanotubes emerged as valid candidates not only for drug delivery, but also as a valuable tool in cancer imaging and physical ablation. Nevertheless, deep investigations about carbon nanotubes’ potential bio-compatibility and cytotoxicity limits should be also critically addressed. In the present review, after introducing carbon nanotubes and their promising advantages and drawbacks for fighting cancer, we want to focus on the numerous and different ways in which they can assist to reach this goal. Specifically, we report on how they can be used not only for drug delivery purposes, but also as a powerful ally to develop effective contrast agents for tumors’ medical or photodynamic imaging, to perform direct physical ablation of metastasis, as well as gene therapy.