It is open for the locking thymidine kinase photosensitizer and pharmaceutical composition of cancer treatment and its use the present invention relates to the field of medicine. Locking thymidine kinase photosensitizer disclosed by the invention improves the selectivity to the photosensitizer of tumor cells and there is tolerance to get well and can achieve the maximum blood concentration in 24 hours. Locking thymidine kinase photosensitizer disclosed by the invention has a bigger conjugated system, a longer absorbing wavelength and an advantage in processing depth lump Wave-length coverage does not need many energy of one light-output equipment of consumption and LED can be used, and keeps PDT more practical and economical. Locking thymidine kinase photosensitizer disclosed by the invention can be used not only for diagnosing via the guidance of fluorescent image, also be suitble to processing prostate cancer. Pharmaceutical composition disclosed by the invention, which merges, uses a chemotherapeutics and locking thymidine kinase photosensitizer, is further improved the curative effect of PDT methods, and extension is used for the application range of lump and also has the good effects to metastatic tumo(u)r.
