CNR-Royal Society (RS) Bilateral Project

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Title: Development of hybrid phosphine-HOPO metal complexes for applications in nuclear medicine.

ICCOM Principal Investigator: Antonella Guerriero.

Project Type: International.

Duration: 01/2022 – 12/2023.

Abstract: The development of metal-based radiopharmaceuticals represents a dynamic and rapidly growing research area due to the relevant uses of these complexes for both diagnostic and therapeutic purposes. Positron emission tomography (PET) is one of the first molecular imaging modalities used clinically, and in this regard, gallium ⁶⁸Ga is a positron emitter attractive for tumor imaging. Over the past 20 years, hydroxypyridinones (HOPOs) have emerged as an important class of ligands having high affinities for “hard” metal ions such as Ga(III) and many ⁶⁸Ga³⁺ radiolabelled HOPO-based compounds have been developed giving high quality PET images. As for all drugs, biodistribution of radiopharmaceuticals is paramount and, being strictly connected to the choice of coordinating ligands, the use of hydrophilic ligands become crucial in this context. The main purpose of the two research groups involved in the project is to join their expertise on the synthesis of hydroxypyridinones and Ga-HOPO-complexes (English research group) and on the synthesis of the water soluble PTA (1,3,5-triaza-7-phopshadamantane) and CAP (1,4,7-triaza-9-phosphatricyclo[5.3.2.1]tridecane) coordination compounds (Italian research group) to develop hybrid phosphine-HOPO Ga(III)-radiolabelled complexes. The combination of bidentate hydroxypyridinone chelators and the monodentate water soluble phosphines is designed with the intent of giving to the resulting complexes the suitable properties to be used as radiopharmaceuticals for PET imaging.

Partnership: ICCOM-CNR, Institute of Pharmaceutical Science (IPS) King’s College London (KCL).

ICCOM participants: Antonella Guerriero, Luca Gonsalvi, Rossella Infantino (associate).

Financed by: Royal Society of London and CNR.

Project total budget: 26.000,00 €.

ICCOM total budget: 12.000,00 €.