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Positron Emission Tomography

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An Automated Radiosynthesis of [68Ga]Ga-FAPI-46 for Routine Clinical Use

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Published on: May 24, 2024

Automated radiosynthesis of [⁶⁴Cu]Cu-FAPI-2286 for FAP-targeted PET imaging.

Mohd Faheem¹, Vaibhav Pandey¹, Nidhi Singh Kushwaha¹

¹Department of Nuclear Medicine, Sanjay Gandhi Postgraduate Institute of Medical Sciences, Lucknow, U.P., 226014, India.

Nuclear Medicine and Biology

|July 9, 2026

Summary

A new automated synthesis of Copper-64 FAPI-2286 ( [64Cu]Cu-FAPI-2286) offers a green and efficient method for liver fibrosis imaging. This radiotracer shows high uptake in fibrotic liver tissue, indicating its potential for non-invasive staging.

Keywords:

Liver fibrosis PET/CT Radiosynthesis [(64)Cu]Cu-FAPI-2286 logD(7.4)

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Area of Science:

Nuclear Medicine
Radiochemistry
Medical Imaging

Background:

Fibroblast Activation Protein (FAP) is a key target for imaging cancer and liver fibrosis.
Copper-64 (64Cu) offers advantages for theranostics compared to Gallium-68 (68Ga) or Lutetium-177 (177Lu).

Purpose of the Study:

To develop and characterize an automated, green synthesis of [64Cu]Cu-FAPI-2286.
To evaluate the physicochemical properties and initial clinical utility of [64Cu]Cu-FAPI-2286 for liver fibrosis imaging.

Main Methods:

Automated radiosynthesis of [64Cu]Cu-FAPI-2286 in an aqueous medium.
Physicochemical characterization including lipophilicity and stability studies.
Pilot PET/CT scan in a patient with liver fibrosis.

Main Results:

High radiochemical purity (>95%) and apparent molar activity achieved with automated synthesis.
[64Cu]Cu-FAPI-2286 demonstrated high hydrophilicity (logD7.4 = -2.38) and excellent stability in biological media.
Intense hepatic uptake observed in the patient with liver fibrosis, confirming active fibrogenesis.

Conclusions:

A robust and green automated synthesis for [64Cu]Cu-FAPI-2286 was successfully established.
The tracer's favorable properties suggest its potential as a non-invasive biomarker for liver fibrosis staging.
High hepatic uptake supports the potential for guiding future [67Cu]Cu-FAPI-2286 therapies.