用于脑肿瘤成像的[18F]1-氨基-3-氟环丁烷-1-羧酸的合成与评估

Synthesis and evaluation of [18F]1-amino-3-fluorocyclobutane-1-carboxylic acid to image brain tumors.

作者信息

Shoup T M, Olson J, Hoffman J M, Votaw J, Eshima D, Eshima L, Camp V M, Stabin M, Votaw D, Goodman M M

机构信息

Emory Center for PET, Department of Neurosurgery, Emory University, Atlanta, Georgia 30322, USA.

出版信息

J Nucl Med. 1999 Feb;40(2):331-8.

PMID:10025843

Abstract

UNLABELLED

We have developed a new tumor-avid amino acid, 1-amino-3-fluorocyclobutane-1-carboxylic acid (FACBC), labeled with 18F for nuclear medicine imaging.

METHODS

[18F]FACBC was prepared with high specific activity (no carrier added [NCA]) and was evaluated for its potential in tumor localization. A comparative study was performed for [18F]FACBC and [18F]2-fluorodeoxyglucose (FDG) in which the uptake of each agent in 9L gliosarcoma (implanted intracerebrally in Fisher 344 rats) was measured. In addition, the first human PET study of [18F]FACBC was performed on a patient with residual glioblastoma multiforme. Quantitative brain images of the patient were obtained by using a Siemens 921 47-slice PET imaging system.

RESULTS

In the rat brain, the initial level of radioactivity accumulation after injection of [18F]FACBC was low (0.11 percentage injected dose per gram [%ID/g]) at 5 min and increased slightly to 0.26 %ID/g at 60 min. The tumor uptake exhibited a maximum at 60 min (1.72 %ID/g), resulting in a tumor-to-brain ratio increase of 5.58 at 5 min to 6.61 at 60 min. In the patient, the uptake of [18F]FACBC in the tumor exhibited a maximum concentration of 146 nCi/mL at 35 min after injection. The uptake of radioactivity in the normal brain tissue was low, 21 nCi/mL at 15 min after injection, and gradually increased to 29 nCi/mL at 60 min after injection. The ratio of tumor to normal tissue was 6 at 20 min after injection. The [18F]FACBC PET scan showed intense uptake in the left frontal region of the brain.

CONCLUSION

The amino acid FACBC can be radiofluorinated for clinical use. [18F]FACBC is a potential PET tracer for tumor imaging.

摘要

未标注

我们研发了一种新的肿瘤亲和性氨基酸，即1-氨基-3-氟环丁烷-1-羧酸（FACBC），并用18F进行标记用于核医学成像。

方法

制备了具有高比活度（无载体添加[NCA]）的[18F]FACBC，并评估其在肿瘤定位方面的潜力。对[18F]FACBC和[18F]2-氟脱氧葡萄糖（FDG）进行了一项对比研究，测量了这两种试剂在9L胶质肉瘤（植入Fisher 344大鼠脑内）中的摄取情况。此外，对一名多形性胶质母细胞瘤残留患者进行了首例[18F]FACBC人体PET研究。使用西门子921 47层PET成像系统获取了该患者的定量脑图像。

结果

在大鼠脑中，注射[18F]FACBC后5分钟时放射性积聚的初始水平较低（每克注射剂量的0.11%[％ID/g]），60分钟时略有增加至0.26％ID/g。肿瘤摄取在60分钟时达到最大值（1.72％ID/g），导致肿瘤与脑的比值从5分钟时的5.58增加到60分钟时的6.61。在患者中，注射后35分钟时肿瘤中[18F]FACBC的摄取达到最大浓度146 nCi/mL。正常脑组织中的放射性摄取较低，注射后15分钟时为21 nCi/mL，注射后60分钟时逐渐增加至29 nCi/mL。注射后20分钟时肿瘤与正常组织的比值为6。[18F]FACBC PET扫描显示大脑左额叶区域有强烈摄取。