Chemo-photodynamic　therapy　is　a　promising　strategy　for　cancer　treatments.　However,　it　remains　a　challenge　to　develop　a　chemo-photodynamic　therapeutic　agent　with　little　side　effect,　high　tumor-targeting,　and　efficient　synergistic　effect　simultaneously.　Herein,　we　report　a　zinc(II)　phthalocyanine　(ZnPc)-doxorubicin　(DOX)　prodrug　linked　with　a　fibroblast　activation　protein　(FAP)-responsive　short　peptide　with　the　sequence　of　Thr-Ser-Gly-Pro　for　chemo-photodynamic　therapy.　In　the　conjugate,　both　photosensitizing　activity　of　ZnPc　and　cytotoxicity　of　DOX　are　inhibited　obviously.　However,　FAP-triggered　separation　of　the　photosensitizer　and　DOX　can　enhance　fluorescence　emission,　singlet　oxygen　generation,　dark-　and　photo-cytotoxicity　significantly,　and　lead　to　a　synergistic　anticancer　efficacy　against　HepG2　cells.　The　prodrug　can　also　be　specifically　and　efficiently　activated　in　tumor　tissue　of　mice.　Thus,　this　prodrug　shows　great　potential　for　clinical　application　in　chemo-photodynamic　therapy.　©　2016　Elsevier　Masson　SAS