Carrier-free 131I-meta-iodobenzylguanidine: comparison of production from meta-diazobenzylguanidine and from meta-trimethylsilylbenzylguanidine.

Published

Journal Article

Meta-iodobenzylguanidine (MIBG) is a drug which is selectively accumulated by the uptake-1 process in adrenergic tissues. When labelled with 131I, it may be used for the targetted radiotherapy of tumours such as phaeochromocytoma and neuroblastoma. This paper describes the preparation of carrier-free 131I-MIBG by radioiodination of meta-diazobenzylguanidine, and compares this process with one involving iododesilylation of meta-trimethylsilylbenzylguanidine. Both processes result in the formation of carrier-free 131I-MIBG whose specific activity at greater than 3 x 10(16) Bq mol-1 is at least 100 times higher than that of commercially available 131I-MIBG for therapeutic use. The therapeutic use of 131I-MIBG with a higher than usual specific activity is predicted to result in a greater target-to-nontarget ratio, and therefore enhanced efficacy because of an increased therapeutic index. As the radiochemical yield of the process involving the metadiazobenzylguanidine intermediate is only 13%, compared with 98% for the iododesilylation reaction, the latter is the preferred synthetic route.

Full Text

Duke Authors

Cited Authors

  • Mairs, RJ; Gaze, MN; Watson, DG; Skellern, GG; Constable, P; McKellar, K; Owens, J; Vaidyanathan, G; Zalutsky, MR

Published Date

  • April 1, 1994

Published In

Volume / Issue

  • 15 / 4

Start / End Page

  • 268 - 274

PubMed ID

  • 8072739

Pubmed Central ID

  • 8072739

International Standard Serial Number (ISSN)

  • 0143-3636

Language

  • eng

Conference Location

  • England