The sodium pump, Na(+)/K(+)-ATPase, could be an important target for the development of anticancer drugs as it serves as a versatile signal transducer, plays a key role in cell adhesion and has abnormal expression and activity that are implicated in the development and progression of different cancers. Several publications have reported differing expression of Na(+)/K(+)-ATPase α- and β-subunits in malignant tissues compared with their normal tissue counterparts, thus offering a powerful diagnostic tool. A growing number of patent applications claim the invention or discovery of Na(+)/K(+)-ATPase inhibitors (e.g., cardiac glycosides) to be used to effectively treat certain cancers that are refractory to conventional chemotherapy or radiotherapy. The aims of this review are to provide an overview of the most significant patents that highlight Na(+)/K(+)-ATPase as a valuable target in anticancer therapy and which report on novel Na(+)/K(+)-ATPase inhibitors and ligands designed as potential anticancer agents.