Carrier-free 131I-meta-iodobenzylguanidine: comparison of production from meta-diazobenzylguanidine and from meta-trimethylsilylbenzylguanidine.
Journal Article (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 1994
Published In
Volume / Issue
- 15 / 4
Start / End Page
- 268 - 274
PubMed ID
- 8072739
International Standard Serial Number (ISSN)
- 0143-3636
Digital Object Identifier (DOI)
- 10.1097/00006231-199404000-00157
Language
- eng
Conference Location
- England