Photodynamic　therapy　(PDT)　as　an　emerging　therapeutic　method　has　drawn　much　attention　in　the　treatment　field　for　cancer.　Photosensitizer,　which　can　convert　photon　energy　into　cytotoxic　species　under　light　irradiation,　is　the　core　component　in　PDT.　The　design　of　photosensitizers　still　faces　problems　of　light　absorption,　targeting,　penetration　and　oxygen　dependence.　With　the　rapid　progress　of　material　science,　various　photosensitizers　have　been　developed　to　produce　cytotoxic　species　for　treatment　of　tumor　with　high　selectivity,　safety,　and　noninvasiveness.　Besides,　the　applications　of　photosensitizers　have　been　expanded　to　diverse　cancer　treatments　such　as　drug　release,　optogenetics　and　immune　checkpoint　blockade.　In　this　review,　we　summarize　the　recent　advances　of　photosensitizers　in　various　therapeutic　methods　for　cancer.　Prevailing　challenges　and　further　prospects　associated　with　photosensitizers　are　also　discussed.　©　2024　Wiley-VCH　GmbH.