[⁶⁸Ga]Ga-HBED-CC-DiAsp: A new renal function imaging agent.

Area of Science:

• Radiochemistry and Nuclear Medicine
• Medical Imaging
• Pharmacology

Background:

• ⁶⁸Ga]Ga-EDTA is a known renal imaging agent for GFR measurement.
• Development of novel agents with improved in vivo characteristics is ongoing.
• ⁶⁸Ga]Ga-HBED-CC-DiAsp was synthesized as a potential alternative renal imaging agent.

Purpose of the Study:

• To synthesize and evaluate [⁶⁸Ga]Ga-HBED-CC-DiAsp as a PET imaging agent for GFR measurement.
• To compare its characteristics with the established agent [⁶⁸Ga]Ga-EDTA.

Main Methods:

• Radiolabeling of HBED-CC-DiAsp with ⁶⁸Ga at room temperature.
• In vitro stability and plasma protein/RBC binding assays.
• In vivo biodistribution and dynamic PET/CT imaging in rodents.

Main Results:

• High radiochemical purity (>98%) achieved in a one-step kit formulation at room temperature.
• High stability (logK_GaL = 38.5) and rapid chelation compared to Ga-EDTA.
• Rapid renal-urinary clearance observed in dynamic PET/CT studies, with comparable time-to-peak and time-to-half-maximal activity to [⁶⁸Ga]Ga-EDTA.

Conclusions:

• [⁶⁸Ga]Ga-HBED-CC-DiAsp can be rapidly prepared with high yield and purity.
• In vitro and in vivo results suggest its utility as a PET imaging agent for GFR assessment.
• Its performance is comparable to [⁶⁸Ga]Ga-EDTA, indicating potential clinical applicability.