Preparation and Preliminary Clinical Application of[18F]AlF-NOTA-TATE
68Ga-DOTA-TATE has been successfully applied in the diagnosis of clinical neuroendocrine tumors,but its short half-life limits its widespread use.This study aimed to develop[18F]AlF-NOTA-TATE to meet the clinical demands of patients with neuroendocrine tumors(NETs)for diagnosis and treatment evaluation.A new column chromatography purification method for[18F]AlF-NOTA-TATE was developed and automated synthesis was performed using a clinical single-vessel multi-functional fluorine synthesis module.The lipophilicity,in vitro stability,and pharmacokinetics of[18F]AlF-NOTA-TATE were studied,and biodistribution experiments and PET/CT imaging of nude mice with NCI-H69(SSTR2 positive expression)small cell lung cancer were conducted,followed by preliminary clinical evaluation on three patients with neuroendocrine tumors.The new column chromatography purification method for[18F]AlF-NOTA-TATE was simple,which was synthesized in a short time with higher than 95%of radiochemical purity and,less than 3%of.ethanol content.Pharmacokinetic and biodistribution experiments in BALB/c mice showed rapid blood clearance of the drug and renal metabolism.PET/CT imaging of tumor-bearing mice showed specific uptake of the radiotracer in SSTR-positive tumors.Preliminary clinical application showed that[18F]AlF-NOTA-TATE is well targeted in patients with long retention time and can provide better image quality.The column chromatography method for the preparation of[18F]AlF-NOTA-TATE was simple and had high radiochemical purity.Preliminary clinical results suggested that[18F]AlF-NOTA-TATE has further value for clinical research.
[18F]AlF-NOTA-TATEcolumn color layer purificationneuroendocrine tumorsclinical application