O-(2-[^(18)F]氟代乙基)-L-酪氨酸的合成及临床实验

Synthesis and Preliminary Studies of O-(2-[^(18)F] fluoroethyl)-L-tyrosine as a Positron Emission Tomography Imaging Agent

目的氨基酸类显像剂O-(2-犤18F犦氟代乙基)-L-酪氨酸(18F-FET)用于脑肿瘤显像的诊断价值。方法通过两步反应合成18F-FET并配成注射液,进行小鼠异常毒性实验、细菌和细菌内毒素检查实验,并对脑瘤患者进行与2-犤18F犦氟代脱氧葡萄糖(18F-FDG)的对比显像。结果18F-FET注射液放化纯度大于95%,室温下放置6h稳定;注射液细菌及细菌内毒素符合中国药典标准;正常脑组织中18F-FET摄取明显低于肿瘤组织,肿瘤组织摄取高于18F-FDG,且显像清晰。结论18F-FET制备简便,体外稳定,毒性小,用于人体非常安全;非肿瘤组织摄取低,获得的图像清晰且优于18F-FDG,是一个较好的脑肿瘤显像剂。

Objective To develop a 18 F-labeled amino acid,O-(2-18 F fluoroethyl)-L-tyrosine( 18 F-FET),as a posi-tron emission tomography(PET)tracer for imaging cerebral tumors.Methods 18 F-FET was synthesized.Preclinical studies including sterility,endotoxin,and toxicity tests were performed.Two brain tumor cases were studied using 18 F-FET and compared with 18 F-FDG.Results Radiochemical purity of 18 F-FET was over95%which remained stable for6hours.The 18 F-FET injection was sterile and its endotoxin content accorded with the standards of Chinese Pharmacopoeia.The uptake of 18 F-FET in the normal brain tissues was significantly lower than that of the tumor,and the images of the brain tumor were clearer than those of 18 F-FDG.Conclusion 18 F-FET can accumulate in the tumor tissues to give high quality images.It suggests that 18 F-FET may be a safe and effective tracer for brain tumor imaging.