The use of carbon nanotubes (CNTs) as polyvalent tools for cancer treatment is progressing at a very fast pace. The most promising approach is the targeted delivery of drugs, designed to selectively direct the therapeutic treatment towards the tumours. CNTs may offer several advantages to overcome one of the main limitations of most existing anticancer therapies, namely the lack of selectivity. Herein, an account of the existing literature on CNT-based nanomedicine for cancer treatment is given. The most significant results obtained so far in the field of drug delivery are presented for many anticancer chemotherapeutics (doxorubicin, methotrexate, taxanes, platinum analogues, camptothecine and gemcitabine), but also for immunotherapeutics and nucleic acids. Moreover, the alternative anticancer therapies based on thermal ablation and radiotherapy are discussed. The attention throughout the review is focused on the different targeting strategies proposed so far, mainly based on antibodies, but also on other specifically recognised molecules or on the application of an external magnetic field.