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

• Published in: Angewandte Chemie International Edition Vol. 56; no. 8; pp. 2118 - 2122
• Main Authors: Nagy, Gábor, Szikra, Dezső, Trencsényi, György, Fekete, Anikó, Garai, Ildikó, Giani, Arianna M., Negri, Roberto, Masciocchi, Norberto, Maiocchi, Alessandro, Uggeri, Fulvio, Tóth, Imre, Aime, Silvio, Giovenzana, Giovanni B., Baranyai, Zsolt
• Format: Journal Article
• Language: English
• Published: Weinheim Wiley Subscription Services, Inc 13.02.2017
• Edition: International ed. in English
• Subjects: Animal models; Biomolecules; Chelating agents; Chelation; kinetics; PET; Positron emission; radiopharmaceuticals; scandium; thermodynamics; Tomography
• ISSN: 1433-7851; 1521-3773
• DOI: 10.1002/anie.201611207

Unprecedented fast and efficient complexation of ScIII 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 44Sc(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. AAZTA (1,4‐bis(carboxymethyl)‐6‐[bis(carboxymethyl)]amino‐6‐methylperhydro‐1,4‐diazepine) is a promising chelator for scandium‐based radiopharmaceuticals owing to high thermodynamic stability, kinetic inertness, and fast formation kinetics of the complexes. AAZTA allows 44Sc‐radiolabeled (bio)conjugates to be prepared under mild conditions, taking full advantage of the wide time window offered by the 44Sc isotope. (RCY=radiochemical yield).