Introduction

Pentadentate chelators able to stably complexed [Al18F]2+, thanks to their rigid structure, and to be marked with 18F very fastly at room temperature. The direct labelling at low temperature allows the diagnosis of several pathologies, thanks to the further conjugation of the chelators with sensible biomolecules, as proteins, anticorporal fragments, nanobodies, affibodies.

Technical features

Patent describes a series of pentadentate chelators able to stably complex the [Al18F]2+ ion. The presence of heterocyclic or polycyclic structures and of five donator atoms, two neutral N-amminics and three negative O-carboxylic or phenolic, allows to obtain a fast and stable complexation also at room temperature. Moreover, the labelled target demonstrated a good stability in physiological conditions and in vivo, a low 18F accumulation into the bones and a fast hepatobiliary depletion. These prerogatives allow the development of bi-functional chelators able to conjugate a wide range of specific biomolecules for the pathologies determination. The Al18F labelling technique could allow the early diagnosis of oncological diseases and/or the identification of specific pathology at the initial stage.

Possible Applications

• PET-imaging for a wide number of different pathologies in function of the biomolecule target considered;
• multimodal diagnosis or theranostics applications if coupled with probes for other imaging techniques or to therapeutic molecules/agents.

Advantages

• Fast and effective labelling with 18F also at room temperature;
• In vivo and in vitro stability of the marker;
• Wide number of applications of the bi-functional chelators with several selective biomolecules to determine pathologies detected with PET-imaging technique.