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Synthesis and evaluation of a macrocyclic bifunctional chelating agent for use with bismuth radionuclides.

Authors
  • Garmestani, K
  • Yao, Z
  • Zhang, M
  • Wong, K
  • Park, C W
  • Pastan, I
  • Carrasquillo, J A
  • Brechbiel, M W
Type
Published Article
Journal
Nuclear Medicine and Biology
Publisher
Elsevier
Publication Date
May 01, 2001
Volume
28
Issue
4
Pages
409–418
Identifiers
PMID: 11395314
Source
Medline
License
Unknown

Abstract

The detailed synthesis of the bifunctional chelating agent 2-(p-isothiocyanatobenzyl)-1,4,7,10,13-pentaazacyclopentadecane-N,N',N",N"',N""-pentaacetic acid (BF_PEPA) is reported. This ligand was conjugated to monoclonal antibody B3 and the resultant immunoconjugate radiolabeled with (205,206)Bi. The in vivo stability of the radiolabeled immunoconjugate, and targeting characteristics were determined by biodistribution studies in A431 xenograft tumor-bearing mice sacrificed at 0.5, 1, 2, 4, and 24 hr. Results indicate that BF_PEPA appears to not be a suitable bifunctional chelating agent for sequestering isotopes of Bi(III) for radioimmunotherapy applications.

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