The present invention relates to the field of medicine, and discloses atargeting thymidinekinase photosensitizer and pharmaceutical composition and use for cancertreatment thereofThe targeting thymidine kinase photosensitizer disclosed by the presentinvention improves theselectivity of photosensitizers to tumor cells and has better tolerance andcan reach maximumblood concentration in 24 hours. The targeting thymidine kinasephotosensitizer disclosed bythe present invention has a bigger conjugated system, a longer absorptionwavelength and anadvantage in treating depth tumors; the wavelength area does not need toconsume much energyof a light-output device and even LEDs can be used, which render PDT morepractical andeconomical. The targeting thymidine kinase photosensitizer disclosed by thepresent inventioncan be used not only for diagnosis, but also for treating prostatic carcinomavia the guidance offluorescence imaging. The pharmaceutical composition disclosed by the presentinvention usesa combination of a chemotherapeutic agent and the targeting thymidine kinasephotosensitizer,which further improves the therapeutic effect of the PDT method, expands theapplication rangefor tumors and has good effects on metastatic tumors as well.(see above formula)