Optimization and scale-up of [⁶⁸Ga]Ga-FAPI-46 production on a Modular-Lab PharmTracer platform for clinical...

Area of Science:

• Nuclear medicine
• Radiopharmaceutical chemistry

Background:

• The fibroblast activation protein (FAP) targeting radiotracer [68Ga]Ga-FAPI-46 is increasingly used in PET/CT for cancer diagnostics.
• Routine production of high activities of [68Ga]Ga-FAPI-46 is needed to meet clinical demand.

Purpose of the Study:

• To optimize and scale-up an automated method for [68Ga]Ga-FAPI-46 production.
• To ensure convenient and routine production of high-activity [68Ga]Ga-FAPI-46 using a PharmTracer module and two GalliaPharm generators.

Main Methods:

• Optimization of labeling conditions including precursor amount, ascorbic acid concentration, buffer pH, and heating parameters.
• Utilized a PharmTracer automated synthesis module with two GalliaPharm generators.
• Evaluated 43 routine syntheses to assess yield, purity, and quality control parameters.

Main Results:

• Optimal labeling achieved with 40 μg precursor, 3 mg ascorbic acid, 0.4 M sodium acetate buffer (pH 4.5), and 15 min heating at 95°C.
• Vitamin C was added as a stabilizer for product quality up to 3 hours post-synthesis.
• Achieved a decay-corrected yield of 91.1 ± 3.4% and radiochemical purity of 99.8 ± 0.3% across 43 syntheses.

Conclusions:

• An efficient and robust automated method for [68Ga]Ga-FAPI-46 production was successfully developed.
• The method provides multiple doses, effectively addressing the clinical need for this radiopharmaceutical.
• The developed process ensures high quality and reliable supply for cancer diagnostics.