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Background   211 At is one of the ideal nuclides for targeted radionuclide therapies (TRTs).  Meta -[ 211 At]astatobenzylguanidine ( 211 At-MABG) has been proposed for the treatment of pheochromocytoma. To effectively use these radiopharmaceuticals, dosimetry must be performed. It is important to determine the absorbed doses of free  211 At and  211 At-MABG to determine the organs that may be at risk when using TRTs. The aim of this study was to estimate human dosimetry from preclinical biodistribution of free  211 At and  211 At-MABG in various organs in normal mice.    Methods  Male C57BL/6 N mice were administered 0.13 MBq of free  211 At or 0.20 MBq of  211 At-MABG by tail-vein injection. The mice were sacrificed at 5 min, and at 1, 3, 6, and 24 h after the injection ( n  = 5 for each group). The percentage of injected activity per mass in organs and blood (%IA/g) was determined. The human absorbed doses of free  211 At and  211 At-MABG were calculated using the Organ Level INternal Dose Assessment/EXponential Modeling (OLINDA/EXM) version 2.0 and IDAC-Dose 2.1.    Results  High uptake of free  211 At was observed in the lungs, spleen, salivary glands, stomach, and thyroid. The absorbed doses of free  211 At in the thyroid and several tissues were higher than those of  211 At-MABG. The absorbed doses of  211 At-MABG in the adrenal glands, heart wall, and liver were higher than those of free  211 At.    Conclusions  The absorbed doses of  211 At-MABG in organs expressing the norepinephrine transporter were higher than those of free  211 At. In addition, the biodistribution of free  211 At was different from that of  211 At-MABG. The absorbed dose of free  211 At may help predict the organs potentially at risk during TRTs using  211 At-MABG due to deastatination.

Human dosimetry of free 211At and meta-[211At]astatobenzylguanidine (211At-MABG) estimated using preclinical biodistribution from normal mice