Photodynamic Therapy (PDT) is a new method developed from last century to treat series of malignant tumor,superficial or intracavitary benign lesion by injection of photosensitiser systemic or local application,then a special wave-length light is used to treat the lesion.As an influential factor,Photosensitiser plays an important role in PDT.This article summarized the mechanism of PDT,characteristic and photochemistry of photosensitizer,focus on the uptake,distribution and effect in PDT of photosensitiser.