As　a　third-generation　steroidal　aromatase　inhibitor,　exemestane　(EXE)　has　been　clinically　used　for　postmenopausal　advanced　breast　cancer　patients　whose　condition　has　progressed　after　treatment　of　tamoxifen.　However,　the　further　development　and　application　of　EXE　was　limited　due　to　its　low　solubility　and　oral　bioavailability,　inevitable　drug　resistance　and　side　effects.　Based　on　the　unique　therapeutic　advantages　of　photodynamic　therapy　(PDT),　a　novel　aromatase-targeted　photosensitizer　EX-Pc　was　synthesized　by　the　combination　of　EXE　and　the　phthalocyanine　photosensitizer.　The　compound　EX-Pc　still　maintains　the　superior　optical　properties　of　the　phthalocyanine　photosensitizer　upon　the　introduction　of　EXE　and　triethylene　glycol　chain.　Meanwhile,　the　results　of　targeted　uptake　in　vitro　and　in　vivo　indicated　that　EX-Pc　exhibited　high　selectivity　and　affinity　for　breast　cancer　cells　and　tumor　tissues,　which　have　the　overexpression　of　aromatase.　More　importantly,　the　compound　EX-Pc　exhibits　significant　photocytotoxicity　and　tumor　regression　ability　on　breast　cancer　cells　and　tumor.　In　addition,　the　compound　EX-Pc　shows　negligible　side　effects　and　high　biological　safety.　We　believe　that　this　is　a　potential　strategy　for　the　treatment　of　postmenopausal　breast　cancer.