A kit method for the high level synthesis of [211At]MABG.

Journal Article (Journal Article)

meta-[(211)At]Astatobenzylguanidine ([(211)At]MABG), an analogue of meta-iodobenzylguanidine (MIBG) labeled with the alpha-emitter (211)At, targets the norepinephrine transporter. Because MABG has been shown to have excellent characteristics in preclinical studies, it has been considered to be a promising targeted radiotherapeutic for the treatment of tumors such as micrometastatic neuroblastoma that overexpress the norepinephrine transporter. To facilitate clinical evaluation of this agent, a convenient method for the high level synthesis of [(211)At]MABG that is adaptable for kit formulation has been developed. A tin precursor anchored to a solid-support was treated with a methanolic solution of (211)At in the presence of a mixture of H(2)O(2)/HOAc as the oxidant; [(211)At]MABG was isolated by simple solid-phase extraction. By using C-18 solid-phase extraction, the radiochemical yield from 25 batches was 63+/-13%; however, loss of radioactivity during evaporation of the methanolic solution was a problem. This difficulty was avoided by use of a cation exchange resin cartridge for isolation of [(211)At]MABG, which resulted in radiochemical yields of 63+/-9% in a shorter duration of synthesis. The radiochemical purity was more than 90% and no chemical impurity has been detected. The final doses were sterile and apyrogenic. These results demonstrate that [(211)At]MABG can be prepared via a kit method at radioactivity levels anticipated for initiation of clinical studies.

Full Text

Duke Authors

Cited Authors

  • Vaidyanathan, G; Affleck, DJ; Alston, KL; Zhao, X-G; Hens, M; Hunter, DH; Babich, J; Zalutsky, MR

Published Date

  • May 15, 2007

Published In

Volume / Issue

  • 15 / 10

Start / End Page

  • 3430 - 3436

PubMed ID

  • 17387017

Pubmed Central ID

  • PMC1885228

International Standard Serial Number (ISSN)

  • 0968-0896

Digital Object Identifier (DOI)

  • 10.1016/j.bmc.2007.03.016


  • eng

Conference Location

  • England