Abstract: Objective To study the biodistribution of ¹⁸⁸Re-octreotide in nude mice which bear-ing human H460 non-small-cell lung cancer and to establish the laying foundation of targeting therapy.Methods ¹⁸⁸Re-octreotide was injected through tail vein of 16 nude mice, those nude mice were killed and the tumors and major organs were taken out from those mice at 2h, 4h, 24h and 48h after injection, then the radioactivity count of those organs and tumors were measured. Other two nude mouse were injected the same dosage ¹⁸⁸Re-octreotide too, SPECT scanning and using regoin of interest technique for semi-quantitative analysis of main organs and tumors'uptake at 2h, 4h, 24h and 48h after injection.Results It was found that the labeling efficiency of ¹⁸⁸Re-octreotide was (95.3±1.8)%. ¹⁸⁸Re-octreotide was major distributed in tumors, lives, small bowels, large bowels and kidneys in nude mice. The largest uptake of tumors is 9.8%ID/g at 4h after injection and the largest tumor/muscle ratios in the SPECT study in those nude mice is 7.1 at 24h after injection.Conclusion The results indicated that ¹⁸⁸Re-octreotide can be located to those tumors which high expressed somatostatin receptor. The tumor/muscle ratios in nude mice is so high that expect to be used for targeting therapy of human H460 non-small-cell lung cancer.