Developing New Cancer Nanomedicines by Repurposing Old Drugs

Abstract The high morbidity and mortality of cancer requires innovative therapeutics. Very recently, several old drugs approved by the U.S. Food and Drug Administration (FDA) or currently undergoing clinical trials, such as 2‐deoxy‐ d ‐glucose, disulfiram, artemisinin, chloroquine, metformin, and aspirin, which have been extensively applied clinically for the treatment of other diseases with reliable evidence of biosafety, have been engineered into nanosystems for enhancing cancer therapy. These old drugs can cooperate with other components of nanosystems or the ambient biological environment, to favor tumor‐specific therapeutics by nontoxicity‐to‐toxicity transition. This Minireview provides a concentrated summary of the most recent progress made in this emerging field, highlighting the “old drugs, new uses” strategy for the construction of next‐generation nanomedicines. It is expected that the clinical translation of nanomedicines can be accelerated by repurposing old drugs to elevate cancer therapeutic efficacy and specificity.