CDCA-Derived NE3TA Conjugate for Liver-Selective ⁶⁴Cu PET Imaging

Area of Science:

• Nuclear medicine
• Radiopharmaceutical chemistry
• Medical imaging

Background:

• Positron emission tomography (PET) is a sensitive imaging technique for visualizing biological processes.
• Assessing liver function with PET is challenging due to the lack of liver-selective tracers.
• Copper-64 (64Cu) is a promising radionuclide for PET imaging.

Purpose of the Study:

• To develop and evaluate a novel liver-selective PET tracer for hepatobiliary imaging.
• To synthesize and characterize a Copper-64 (64Cu)-labeled bifunctional chelator conjugate with CDCA.
• To assess the stability, radiolabeling efficiency, and biodistribution of the novel tracer.

Main Methods:

• Development of a bifunctional chelator (3p-C-NE3TA) for Copper-64 (64Cu) chelation.
• Synthesis of a CDCA-derived chelator conjugate (3p-C-NE3TA-CDCA).
• Radiolabeling of the conjugate with 64Cu and evaluation of in vitro and in vivo properties in mice.

Main Results:

• Efficient radiolabeling of 3p-C-NE3TA-CDCA with 64Cu achieved at room temperature.
• The 64Cu-labeled tracer demonstrated high stability in human serum.
• Prominent and selective hepatic uptake with rapid clearance from blood and non-target tissues was observed in mice.

Conclusions:

• The 64Cu-labeled 3p-C-NE3TA-CDCA conjugate is a promising candidate for liver-selective PET imaging.
• The tracer exhibits excellent radiolabeling efficiency, stability, and biodistribution characteristics.
• This development could advance the clinical application of PET for hepatobiliary function assessment.