[⁶⁸Ga]DO3A-VS-Cys⁴⁰-Exendin-4, a glucagon-like peptide 1 receptor agonist, was evaluated as a potential PET tracer for the quantitation of human islets transplanted to the liver. The short-lived PET radionuclide ⁶⁸Ga, available on a regular basis from a ⁶⁸Ge/⁶⁸Ga generator, is an attractive choice. Human C-peptide was measured to evaluate human islet function post-transplantation and prior to microPET imaging. [⁶⁸Ga]DO3A-VS-Cys⁴⁰-Exendin-4 was radiosynthesized and evaluated for PET imaging of transplanted human islets in the liver of healthy NOD/SCID mice. The biodistribution of the tracer was evaluated to determine the uptake into various organs, and qPCR of liver samples was conducted to confirm engrafted islet numbers after PET imaging. Measurement of human C-peptide indicated that higher engrafted islet mass resulted in higher human C-peptide levels in post-transplantation. The microPET imaging yielded high resolution images of liver-engrafted islets and also showed significant retention in mouse livers at 8 weeks post-transplantation. Biodistribution studies in mice revealed that liver uptake of [⁶⁸Ga]DO3A-VS-Cys⁴⁰-Exendin-4 was approximately 6-fold higher in mice that received 1000 islet equivalent (IEQ) than in non-transplanted mice. qPCR analysis of insulin expression suggested that islet engraftment numbers were close to 1000 IEQ transplanted. In conclusion, human islets transplanted into the livers of mice exhibited significant uptake of [⁶⁸Ga]DO3A-VS-Cys⁴⁰-Exendin-4 compared to the livers of untreated mice; and imaging of the mice using PET showed the human islets clearly with high contrast against liver tissue, enabling accurate quantitation of islet mass. Further validation of [⁶⁸Ga]DO3A-VS-Cys⁴⁰-Exendin-4 as an islet imaging probe for future clinical application is ongoing.

#	Concept	H-Index	Publications	Citations
1	Medicine	4	4	342
2	Cell Biology	2	2	125
3	Health Sciences	1	1	136
4	Biochemistry	1	1	81
5	Cellular Physiology	1	1	88

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