The Fe-N co-doped TiO2nanocomposites were synthesized by a sol-gel method and characterized by scanning electron microscope (SEM), transmission electron microscope (TEM), X-ray diffraction (XRD), ultraviolet-visible absorption spectroscopy (UV-vis) and X-ray photoelectron spectroscopy (XPS). Then the photocatalytic inactivation of Fe-N-doped TiO2on leukemia tumors was investigated by using Cell Counting Kit-8 (CCK-8) assay. Additionally, the ultrastructural morphology and apoptotic percentage of treated cells were also studied. The experimental results showed that the growth of leukemic HL60 cells was significantly inhibited in groups treated with TiO2nanoparticles and the photocatalytic activity of Fe-N-TiO2was significantly higher than that of Fe-TiO2and N-TiO2, indicating that the photocatalytic efficiency could be effectively enhanced by the modification of Fe-N. Furthermore, when 2 wt% Fe-N-TiO2nanocomposites at a final concentration of 200 μg/mL were used, the inactivation efficiency of 78.5% was achieved after 30-minute light therapy.