With recent advances in nanotechnology, nanoparticles (NPs) have emerged as powerful platforms in cancer therapy, offering enhanced drug delivery capabilities with improved targeting specificity and reduced systemic toxicity.[30] Engineered NPs serve as multifunctional carriers, capable of increasing drug bioavailability; while, minimizing adverse effects.[31] Among them, self‐assembled M2pep‐Cs NPs/Plerixafor NPs represent a next‐generation nanomedicine system designed to specifically inhibit the CXCL12–CXCR4 signaling pathway and reprogram TAMs to potentiate the anti‐tumor immune response. The gene discussed is CXCR4; the disease is neoplasm.