This review focuses on the lipid droplets (LDs)-localized chemical chromophores for photodynamic therapy. It highlights the design principles, performance, and biomedical applications of these photosensitizers (PSs). Especially, the cell death pathways induced by these tools are introduced. These targetable PSs guard our health by destroying the LDs of cancer cells, just as soldiers protect our cities from alien invasion by destroying the energy cores of alien airships (e665).