Subcellular　organelles　are　the　cornerstones　of　cells,　and　destroying　them　will　cause　cell　dysfunction　and　even　death.　Therefore,　realizing　precise　organelle　targeting　of　photosensitizers　(PSs)　can　help　reduce　PS　dosage,　minimize　side　effects,　avoid　drug　resistance,　and　enhance　therapeutic　efficacy　in　photodynamic　therapy　(PDT).　Organelle-targeted　PSs　provide　a　new　paradigm　for　the　construction　of　the　next　generation　of　PSs　and　may　provide　implementable　strategies　for　future　precision　medicine.　In　this　Review,　the　recent　targeting　strategies　of　different　organelles　and　the　corresponding　design　principles　of　molecular　and　nanostructured　PSs　are　summarized　and　discussed.　The　current　challenges　and　opportunities　in　organelle-targeted　PDT　are　also　presented.