[Gd(HB‐DO3A)]: Equilibrium, Dissociation Kinetic and Structural Differences in a Simple Homolog of [Gd(HP‐DO3A)] (Prohance®)

Author:

Versolatto Silvia1,Boccalon Mariangela2ORCID,Guidolin Nicol2,Travagin Fabio3ORCID,Alessio Enzo1ORCID,Aime Silvio4ORCID,Balducci Gabriele1ORCID,Giovenzana Giovanni B.3ORCID,Baranyai Zsolt2ORCID

Affiliation:

1. Dipartimento di Scienze Chimiche e Farmaceutiche Università di Trieste Piazzale Europa 1 34127 Trieste TS Italy

2. Bracco Imaging Spa CRB Trieste AREA Science Park 34149 Basovizza TS Italy

3. Dipartimento di Scienze del Farmaco Università del Piemonte Orientale Largo Donegani 2/3 Novara NO 28100 Italy

4. IRCCS SDN Research Institute Diagnostics and Nuclear SynLab Via Emanuele Gianturco, 113 80143 Napoli NA Italy

Abstract

Abstract[Gd(HP‐DO3A)] (gadoteridol) as an active compound of ProHance® is a widely employed contrast agent in clinical MRI scans in the last 30 years. Recent concerns about the long‐term retention of gadolinium‐based contrast agents (GBCAs) led to a deeper investigation of the structural features underlying the integrity of the paramagnetic metal complex. Several human and nonclinical studies have noted marked differences among the macrocyclic GBCAs, with the least retention of Gd traces and most rapid elimination consistently being reported for [Gd(HP‐DO3A)]. It was deemed of interest to assess how minor structural/electronic changes associated to the ligand structure may affect basic properties of the metal complex with several [Gd(HP‐DO3A)] analogues synthesized and characterized in the last years. We recently reported that the closest homolog of [Gd(HP‐DO3A)], i. e.: [Gd(HB‐DO3A)], in which a (±)‐2‐hydroxy‐1‐propyl pendant arm is replaced by a (±)‐2‐hydroxy‐1‐butyl moiety, showed a significantly different retention behaviour in the model interaction with collagen, despite the apparently very minor structural difference. In this paper we report a comprehensive study of the structural, thermodynamic, kinetic and relaxation properties of [Gd(HB‐DO3A)], compared to the parent [Gd(HP‐DO3A)] and to other closely related macrocyclic GBCAs to assess whether very minor structural changes can modulate the physico‐chemical properties of Gd3+ complexes.

Publisher

Wiley

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