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通过18F正电子发射断层扫描(PET)和19F磁共振成像(MRI)监测5-氟尿嘧啶的生物分布和代谢评估:一项对比动物研究。

Assessment of the biodistribution and metabolism of 5-fluorouracil as monitored by 18F PET and 19F MRI: a comparative animal study.

作者信息

Brix G, Bellemann M E, Haberkorn U, Gerlach L, Lorenz W J

机构信息

Research Program Radiological Diagnostics and Therapy, German Cancer Research Center (DKFZ), Heidelberg, Germany.

出版信息

Nucl Med Biol. 1996 Oct;23(7):897-906. doi: 10.1016/s0969-8051(96)00122-9.

DOI:10.1016/s0969-8051(96)00122-9
PMID:8971857
Abstract

The effective clinical use of the anticancer drug 5-fluorouracil (5-FU) requires the non-invasive assessment of its transport and metabolism, particularly in the tumor and the liver, where the drug is catabolized to alpha-fluoro-beta-alanine (FBAL). In this study, the potentials and limitations of dynamic 18F PET and metabolic 19F MRI examinations for noninvasive 5-FU monitoring were investigated in ACI and Buffalo rats with transplanted MH3924A and TC5123 Morris hepatomas, respectively. Selective 5-[19F]FU and [19F]FBAL MR images were acquired 5 and 70 min after 5-FU injection using a CHESS MRI sequence. After administration of 5-[18F]FU, the kinetics of the regional 5-[18F]FU uptake were measured by dynamic PET scanning over 120 min. To allow a comparison between PET and MRI data, standardized uptake values (SUV) were computed at the same points in time. The TC5123 hepatoma showed a significantly (p < 0.002) higher mean SUV at 5 and 70 min post-5-FU injection than the MH3924A cell lines, whereas there were no significant differences between the mean SUV measured in the liver of both animal populations. In contrast to the PET data, no significant differences in the mean 5-[19F]FU and [19F]FBAL MR signal values in the tumor of both models were observed. The MR images, however, yielded the additional information that 5-FU is converted to FBAL only in the liver and not in the hepatomas.

摘要

抗癌药物5-氟尿嘧啶(5-FU)的有效临床应用需要对其转运和代谢进行非侵入性评估,尤其是在肿瘤和肝脏中,药物在这些部位会分解代谢为α-氟-β-丙氨酸(FBAL)。在本研究中,分别在移植了MH3924A和TC5123 Morris肝癌的ACI和布法罗大鼠中,研究了动态18F PET和代谢19F MRI检查用于5-FU非侵入性监测的潜力和局限性。在注射5-FU后5分钟和70分钟,使用CHESS MRI序列采集选择性5-[19F]FU和[19F]FBAL MR图像。给予5-[18F]FU后,通过动态PET扫描在120分钟内测量局部5-[18F]FU摄取的动力学。为了能够比较PET和MRI数据,在相同时间点计算标准化摄取值(SUV)。TC5123肝癌在注射5-FU后5分钟和70分钟时的平均SUV显著高于MH3924A细胞系(p < 0.002),而在两个动物群体肝脏中测量的平均SUV之间没有显著差异。与PET数据相反,在两种模型的肿瘤中,未观察到平均5-[19F]FU和[19F]FBAL MR信号值有显著差异。然而,MR图像还提供了额外信息,即5-FU仅在肝脏中转化为FBAL,而在肝癌中不会。

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