Phase I Study of 68Ga-NOTA-HL for PET/CT Imaging of Hepatic Asialoglycoprotein Receptors in Healthy Volunteers.

This study investigated the safety, biodistribution, and dosimetry of ⁶⁸Ga-hexavalent lactoside (⁶⁸Ga-NOTA-HL), a PET tracer targeting asialoglycoprotein receptors (ASGPRs) on hepatocytes. ASGPRs, key for glycoprotein homeostasis, serve as a valuable biomarker of liver function. ⁶⁸Ga-NOTA-HL demonstrated excellent safety in 12 healthy volunteers with no adverse events. Biodistribution studies revealed high liver uptake with minimal uptake in other organs, consistent with ASGPR targeting. The effective dose was 0.0289 mSv/MBq, indicating low radiation exposure. These findings suggest ⁶⁸Ga-NOTA-HL PET/CT holds significant promise as a safe and effective imaging technique for assessing liver function. The high liver specificity and extremely low background activity provide a strong foundation for further clinical investigations into its potential for evaluating liver function in various clinical settings, including the assessment of liver reserve in patients with liver diseases.