Herein,　we　developed　a　dual-activated　prodrug,　BTC,　that　contains　three　functional　components:　a　glutathione　(GSH)-responsive　BODIPY-based　photosensitizer　with　a　photoinduced　electron　transfer　(PET)　effect　between　BODIPY　and　the　2,4-dinitrobenzenesulfonate　(DNBS)　group,　and　an　ROS-responsive　thioketal　linker　connecting　BODIPY　and　the　chemotherapeutic　agent　camptothecin　(CPT).　Interestingly,　CPT　displayed　low　toxicity　because　the　active　site　of　CPT　was　modified　by　the　BODIPY-based　macrocycle.　Additionally,　BTC　was　encapsulated　with　the　amphiphilic　polymer　DSPE-mPEG(2000)　to　improve　drug　solubility　and　tumor　selectivity.　The　resulting　nano-prodrug　passively　targeted　tumor　cells　through　enhanced　permeability　and　retention　(EPR)　effects,　and　then　the　photosensitizing　ability　of　the　BODIPY　dye　was　restored　by　removing　the　DNBS　group　with　the　high　concentration　of　GSH　in　tumor　cells.　Light-triggered　ROS　from　activated　BODIPY　can　not　only　induce　apoptosis　or　necrosis　of　tumor　cells　but　also　sever　the　thioketal　linker　to　release　CPT,　achieving　the　combination　treatment　of　selective　photodynamic　therapy　and　chemotherapy.　The　antitumor　activity　of　the　prodrug　has　been　demonstrated　in　mouse　mammary　carcinoma　4T1　and　human　breast　cancer　MCF-7　cell　lines　and　4T1　tumor-bearing　mice.