Collectively, these results demonstrate that ARV@PDSA shows superior anti‐tumor efficacy by efficiently inhibiting intracellular BRD4 and c‐Myc expression in both HeLa and B16F10 tumor‐bearing mouse models, highlighting the significance of our Nano‐PROTACs strategy to expand the therapeutic landscape for the treatment of other diseases. This evidence concerns the gene MYC and neoplasm.