Ruthenium complexes have been shown to possess remarkable chemotherapeutic-both anticancer and antimetastatic- properties. Ruthenium possesses unique attributes that have led to the development of promising anticancer and antimetastatic therapeutics, for example, RAPTA-C, KP1019 and NAMI-A. The amplified benefit that can be gained by incorporating drugs into macromolecules has only recently been investigated for ruthenium agents. The advances in macromolecular chemistries has allowed for the incorporation and examination of some of these promising moieties within macromolecular matrices. Several nano-sized delivery systems have also been developed for cancer treatment, for example, micelles, liposomes, peptide structures and hybrid moieties. The main findings of this novel body of work are presented here, highlighting the scope for further investigations. (c) 2014 Society of Chemical Industry