Automated cGMP Radiosynthesis of [18F]NOTA-ABY-030 with Aluminum Fluoride on the GE FASTlab Automated Synthesis Platform

Background Epidermal Growth Factor Receptor (EGFR) overexpression in Head and Neck Squamous Cell Carcinoma (HNSCC) is well documented and strongly correlated with aggressive phenotypes. As such EGFR is an excellent choice for molecular imaging of HNSCC as the high overexpression levels allow for a specific marker of tumors. Currently the only established EGFR radiopharmaceuticals that have been translated into human subjects are labeled versions of antibodies and antibody fragments, which all have slow pharmacokinetics and have low specificity due to high background and blood pool. [ 18 F]NOTA-ABY-030 is a promising positron emission tomography (PET) radiotracer for in vivo study of the EGFR receptor that alleviates these issues; herein we report the cGMP automated radiosynthesis for use with human subjects. Results To facilitate clinical trials a fully automated radiosynthesis procedure for [ 18 F]NOTA-ABY-030 was developed using commercially available materials on the GE HealthCare FASTlab cassette-based automated radiosynthesis system. The overall synthesis time was 20 min with a radiochemical yield of 47 ± 10% (n = 3). The radiochemical purity was greater than 90% for [ 18 F]NOTA-ABY-030 with a binding fraction of 90% ( n = 3). The protocol described herein reliably provides [ 18 F]NOTA-ABY-030 that meets all relevant release criteria for a GMP radiopharmaceutical. Conclusions A fast, reliable and efficient automated radiosynthesis was developed using a commercial cassette-based module. This will enable clinical trials work as well as simple method transfer to alternate manufacturing sites; as well as being applicable to small biologic targeting vector radiolabeling.