AAZTA: An Ideal Chelating Agent for the Development of 44 Sc PET Imaging Agents

Gábor Nagy; Dezső Szikra; György Trencsényi; Anikó Fekete; Ildikó Garai; Arianna M Giani; Roberto Negri; Norberto Masciocchi; Alessandro Maiocchi; Fulvio Uggeri; Imre Tóth; Silvio Aime; Giovanni B Giovenzana; Zsolt Baranyai

doi:10.1002/anie.201611207

AAZTA: An Ideal Chelating Agent for the Development of ⁴⁴ Sc PET Imaging Agents

Angew Chem Int Ed Engl. 2017 Feb 13;56(8):2118-2122. doi: 10.1002/anie.201611207. Epub 2017 Jan 18.

Authors

Gábor Nagy^{1

2}, Dezső Szikra^{1

2}, György Trencsényi^{1

2}, Anikó Fekete², Ildikó Garai¹, Arianna M Giani³, Roberto Negri³, Norberto Masciocchi⁴, Alessandro Maiocchi⁵, Fulvio Uggeri⁵, Imre Tóth⁶, Silvio Aime⁷, Giovanni B Giovenzana^{3

8}, Zsolt Baranyai^{5

6}

Affiliations

¹ Scanomed Ltd., Nagyerdei Krt. 98, 4032, Debrecen, Hungary.
² University of Debrecen, Medical Imaging Clinic, Nagyerdei krt. 98, 4032, Debrecen, Hungary.
³ Dipartimento di Scienze del Farmaco, Università del Piemonte Orientale, Largo Donegani 2/3, 28100, Novara, Italy.
⁴ Dipartimento di Scienza e Alta Tecnologia and To.Sca.Lab, Università degli Studi dell'Insubria, via Valleggio 11, 22100, Como, Italy.
⁵ Bracco Imaging spa, Bracco Research Centre, Via Ribes 5, 10010, Colleretto Giacosa (TO), Italy.
⁶ Department of Inorganic and Analytical Chemistry, University of Debrecen, 4032, Debrecen, Egyetem tér 1, Hungary.
⁷ Dipartimento di Biotecnologie Molecolari e Scienze della Salute, Centro di Imaging Molecolare e Preclinico, Università degli Studi di Torino, Via Nizza 52, 10126, Torino, Italy.
⁸ CAGE Chemicals srl, Via Bovio 6, 28100, Novara, Italy.

PMID: 28097756
DOI: 10.1002/anie.201611207

Abstract

Unprecedented fast and efficient complexation of Sc^III was demonstrated with the chelating agent AAZTA (AAZTA=1,4-bis(carboxymethyl)-6-[bis(carboxymethyl)]amino-6-methylperhydro-1,4-diazepine) under mild experimental conditions. The robustness of the ⁴⁴ Sc(AAZTA)^- chelate and conjugated biomolecules thereof is further shown by in vivo PET imaging in healthy and tumor mice models. The new results pave the way towards development of efficient Sc-based radiopharmaceuticals using the AAZTA chelator.

Keywords: PET; kinetics; radiopharmaceuticals; scandium; thermodynamics.

Publication types

Research Support, Non-U.S. Gov't