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. Here, CPQ is linked to neoplasm.