Encapsulation of the platinum(IV) prodrug mitaplatin in block copolymer nanoparticles increases drug circulation time in the blood and reduces accumulation in the kidneys, as reported by Lippard and colleagues in this issue of ACS Nano. Importantly, controlled drug release from the nanoparticles produces long-term anticancer efficacy, with the prospect of reduced side effects. We highlight the potential that such a strategy holds for the future development of metallodrugs. Metal coordination complexes offer the prospect of novel mechanisms of activity on account of their unique architectures, as well as potential activation mechanisms, including ligand substitution and metal- and ligand-centered redox properties. Nanoparticles offer exciting prospects for improving delivery, cell uptake, and targeting of metallodrugs, especially anticancer drugs, to make them more effective and safer.