A platinum (Pt)-based agent belonging to the phosphaplatin family comprised of Pt complexed to a pyrophosphate ligand, with potential antineoplastic activity. Although the exact mechanisms through which imifoplatin exerts its effect have yet to be fully elucidated, this agent, upon intravenous administration, binds to certain transmembrane proteins and activates several genes involved in tumor suppression and apoptosis. This leads to the activation of various signal transduction pathways, induces S/G2 phase cell cycle, and causes tumor cell apoptosis. In addition, imifoplatin may inhibit angiogenesis. Unlike conventional Pt-based chemotherapeutics, imifoplatin does not bind to DNA and is able to overcome drug resistance, which occurs with conventional Pt-based chemotherapeutics; it also has a more favorable side effect profile and is more stable in plasma.