e-Repository BATAN

Advanced Search

Investigation into the Use of a Diaminodihydroxyaryl Derivative of Ethylenediaminetetraacetic Acid (DAHAEDTA) for Cu-64 PET Imaging and Radioimmunotherapy

Ramli, Martalena and Schmidt, Peter F. and Di Bartolo, Nadine and Smith, Suzanne V. (2017) Investigation into the Use of a Diaminodihydroxyaryl Derivative of Ethylenediaminetetraacetic Acid (DAHAEDTA) for Cu-64 PET Imaging and Radioimmunotherapy. Australian Journal of Chemistry, 70 (5). pp. 614-622. ISSN 1445-0038

[img] Text (A diaminodihydroxyaryl derivative of ethylenediaminetetraacetic acid (DAHA-EDTA) was synthesised in two steps and evaluated for Cu-64 radiolabelling of the B72.3 antibody.)
CH16647 - Published Version
Available under License Creative Commons Attribution Non-commercial.

Download (34kB)

Abstract

A diaminodihydroxyaryl derivative of ethylenediaminetetraacetic acid (DAHA-EDTA) was synthesised in two steps and evaluated for Cu-64 radiolabelling of the B72.3 antibody. The ligand complexes Cu-64 rapidly in a pH range 4 to 7. The Cu-64 complex of the parent species N,N′-bis(carboxymethyl)-N,N′-bis(2-hydroxyacetanilido)-1,2-diaminoethane (DHA-EDTA) shows good stability in serum at 37°C for up to 72 h. Conjugation of the Cu-64-DAHA-EDTA to the B72.3 antibody was achieved using 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) as the activating agent. The reaction conditions were optimized for protein concentration and molar ratio of Cu-64-DAHA-EDTA and EDC to antibody. The specific activity of the final [Cu-64-DAHA-EDTA]-B72.3 product was 49 MBq mg-1 at the end of synthesis. The biodistribution of [Cu-64-DAHA-EDTA]-B72.3 in LS174t tumour-bearing nude mice was monitored over a 24 h period. Maximum tumour uptake (25.8 ± 7.5 % ID g-1) was achieved at 16 h and maintained at 24 h (21.6 ± 1.8 % ID g-1). Rapid clearance of the [Cu-64-DAHA-EDTA]-B72.3 from the blood resulted in good tumour-to-blood ratios (≈ 3.3) within a shorter period (6 h) than previously reported with B72.3 whole antibody and the LS174t tumour bearing nude mouse model.

Item Type: Article
Subjects: Isotop dan Radiasi > Produksi Isotop dan Sumber Radiasi > Teknik Produksi Radiofarmaka
Divisions: Pusat Teknologi Radioisotop dan Radiofarmaka
Depositing User: USER PTRR BATAN
Date Deposited: 19 Apr 2018 03:30
Last Modified: 19 Apr 2018 03:30
URI: http://repo-nkm.batan.go.id/id/eprint/343

Actions (login required)

View Item View Item