Noninvasive　treatments　for　terminal　cancer　patients　constitute　a　new　trend　in　tumor　treatment.　Therefore,　phototherapy,　including　photodynamic　therapy　(PDT)　and　photothermal　therapy　(PTT),　has　attracted　considerable　interest.　Light　and　a　photosensitizer　(PS)　are　employed　in　both　treatment　methods.　For　PDT,　the　PS　generates　reactive　oxygen　species　(ROS)　when　exposed　to　light,　whereas　for　PTT,　the　PS　generates　heat.　In　this　regard,　the　systematic　design　of　new　PSs　has　become　an　active　area　of　phototherapy　research　in　an　effort　to　solve　the　problems　associated　with　conventional　PSs.　In　the　past　decade,　activatable　and　heavy-atom-free　PSs　have　become　significant　research　areas.　Therefore,　we　discuss　our　recent　contributions　to　the　PDT　and　PTT　in　this　account.　©　2022　Korean　Chemical　Society,　Seoul　&　Wiley-VCH　GmbH.