Ferroptosis is a new form of nonapoptotic programmed cell death characterized by iron-dependent accumulation of lipid hydroperoxides to lethal levels. An increasing number of studies have in recent years revealed close relationships between ferroptosis and nanomedicine, which has been regarded as a new strategy for developing nanomaterial-based therapeutic agents for highly effective therapy of various cancers. In this review, the molecular mechanisms and pathways for ferroptosis regulation were first presented; then, various nanomaterials that induce ferroptosis for cancer specific therapy were systematically discussed; finally, the current challenges and constructive perspectives in this field were provided.