This perspective provides novel insights on the LACTB’s metabolic role in cancer progression and clinical prognosis for developing LACTB-targeted cancer therapies or neoadjuvant therapeutic interventions, e.g., to combine the LACTB-targeted strategy with the developing drug delivery systems, such as the transferrin/α-tocopherol modified poly(amidoamine) dendrimers to improve tumor targeting [58] or transferrin and octaarginine modified dual-functional liposomes to enhance intracellular delivery [59]. The gene discussed is LACTB; the disease is cancer.