Our phenotype‐based prodrug molecule proved more effective than esterase‐ and aminopeptidase‐based prodrug molecule DRP104 in drug‐resistant cell models.[17, 18, 19, 20] In addition to modulating tumor energy metabolism, NQO1‐responsive prodrug could further augment the anti‐tumor effect by enhancing the immune microenvironment and activating protective immune response. This evidence concerns the gene NQO1 and neoplasm.