The present invention relates to the field of medicine, and discloses a targeting thymidine kinase photosensitizer and pharmaceutical composition and use for cancer treatment thereof. The targeting thymidine kinase photosensitizer disclosed by the present invention improves the selectivity of photosensitizers to tumor cells and has better tolerance and can reach maximum blood concentration in 24 hours. The targeting thymidine kinase photosensitizer disclosed by the present invention has a bigger conjugated system, a longer absorption wavelength and an advantage in treating depth tumors the wavelength area does not need to consume much energy of a light-output device and even LEDs can be used, which render PDT more practical and economical. The targeting thymidine kinase photosensitizer disclosed by the present invention can be used not only for diagnosis, but also for treating prostatic carcinoma via the guidance of fluorescence imaging. The pharmaceutical composition disclosed by the present invention uses a combination of a chemotherapeutic agent and the targeting thymidine kinase photosensitizer, which further improves the therapeutic effect of the PDT method, expands the application range for tumors and has good effects on metastatic tumors as well.
