The purpose of this study was to examine the radiolabeling and biodistribution of 188Re(V)-DMSA as a therapeutic cancer radiopharmaceutical. We made a DMSA kit(NaHC03 1.5 mg, meso-2,3-dimercaptosuccinic acid 1.0 mg L(+)-ascorbic acid 0.7mg, SnCl2·2H2O 0.34 mg, pH 2.9) for labeling with 188Re. In this kit, 188ReO4- 5 mCi/2 ml added and boiled at 100℃ for 3 hr in water bath. The final pH adjusted to 7.5 with 7% NaHCO3 solution. We checked the labelling efficacy with TLC- SG(n-butanol : acetic acid:H2O = 3 : 2 : 3) and examined the stability both in room temperature and in serum at 37℃. Biodistribution(l, 3, 13, 24, 48 hr) of 188Re(V)-DMSA compound was evaluated in Sarcoma 180 tumor-bearing mice. Each labeling efficiency and stability at room temperature for 48 hours was over 98% and 95%, respectely. The stability in serum were 82%(6 hr) and 85%(48 hr). Tumor uptake of 188Re(V)-DMSA in Sarcoma 180- bearing mice were 0.66±0.15%(1 hr), 0.51±0.10%(3 hr), 0.19±0..05%(24 hr) and 0.13±0.02% (48 hr). These result are consistent with those of 99mTc(V)-DMSA which were reported previously In conclusion, 188Re(V)-DMSA may be a useful therapeutic radiopharmaceutical for treating some cancers and metastatic bone lesion.