The present invention relates to the field of biomedicine, more specifically to medical applications of fusion proteins, and provides a novel tumor-targeting fusion protein drug vector for optical imaging and photodynamic therapy, wherein the sequence is represented by SEQ ID NO.1. According to the fusion protein drug vector ATF-HSA of the present invention, the natural HSA ligand binding site FA1 in the vector is utilized to load CPZ to form a ATF-HSA:CPZ complex so as to make the water solubility of the CPZ be enhanced, provide targeting selectivity for tumor cells having high uPAR expression, and make the vector can be used for optical tumor imaging and photodynamic tumor therapy in vitro and in vivo.