title: Blocking [211At]astatide accumulation in normal tissues: preliminary evaluation of seven potential compounds.
abstract: Normal tissue accumulation of 211At must be minimized during targeted radiotherapy with 211At-labeled compounds. Therefore, we investigated the ability of seven compounds to block normal organ uptake of [211At]astatide in mice: potassium iodide, sodium thiocyanate, sodium perchlorate, sodium periodate, cysteine, 2,3-dimercapto-1-propanesulfonic acid, and meso-2,3-dimercaptosuccinic acid. The monovalent anions I-, SCN-, and ClO4- reduced 211At uptake in stomach and thyroid, while thiocyanate and cysteine were the only compounds to significantly reduce activity levels in lungs and spleen. This study suggests that blocking agents may help reduce normal organ radiation doses in endoradiotherapeutic procedures with 211At-labeled radiopharmaceuticals.
authors.affiliation: Department of Radiology, Duke University Medical Center, Durham, North Carolina 27710, USA.
authors.forename: R H
authors.initials: RH
authors.lastname: Larsen
authors.forename: S
authors.initials: S
authors.lastname: Slade
authors.forename: M R
authors.initials: MR
authors.lastname: Zalutsky
mesh_terms: D000818:Animals; D000838:Anions / Q000494:pharmacology; D001246:Astatine / Q000493:pharmacokinetics* / Q000633:toxicity; D004305:Dose-Response Relationship, Drug; D004336:Drug Antagonism; D007274:Injections, Intraperitoneal; D007457:Iodine Radioisotopes / Q000493:pharmacokinetics* / Q000633:toxicity; D007928:Lethal Dose 50; D051379:Mice; D008807:Mice, Inbred BALB C; D011833:Radiation Injuries, Experimental / Q000517:prevention & control; D011878:Radiotherapy; D013438:Sulfhydryl Compounds / Q000494:pharmacology*; D014018:Tissue Distribution / Q000187:drug effects
chemical_list: D000838:Anions; D007457:Iodine Radioisotopes; D013438:Sulfhydryl Compounds; D001246:Astatine