Authors:

Rachael Fujimori

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Positron emission tomography (PET) is a highly sensitive and quantitative imaging modality that has been applied for noninvasive visualization of biochemical and metabolic processes in vivo. While PET has the potential to assess hepatobiliary function and transport, liver-selective PET tracers have not been successfully translated into clinical applications. Copper-64 (Cu) is a positron-emitting radionuclide that has been widely explored for PET imaging of bioactive molecules. We have developed an effective bifunctional chelator 3p-C-NE3TA that can securely and rapidly sequester "Cu under mild conditions. Herein, we report the synthesis and evaluation of a CDCA-derived chelator conjugate, 3p-C-NE3TA-chenodeoxycholic acid (CDCA), for potential applications in liver-selective PET imaging. The 3p-C-NE3TA-CDCA conjugate was efficiently radiolabeled with "Cu at room temperature. The resulting "Cu-labeled 3p-C-NE3TA-CDCA conjugate demonstrated high stability in human serum and prominent and selective hepatic uptake with favorable clearance, as evidenced by very low activity levels in blood and non-target tissues in healthy mice at 4h post-injection. Taken together, these results show that "Cu-labeled 3p-C-NE3TA-CDCA exhibits excellent radiolabeling efficiency, high in vitro and in vivo stability, and marked liver-selective biodistribution. This CDCA-derived NE3TA conjugate is a promising bile acid-based PET tracer for further optimization and comprehensive evaluation in imaging of liver diseases.

Source:

Illinois Institute of Technology

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Co-authors:

Rachael Fujimori