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2-[18F]氟达拉滨,一种新型正电子发射断层扫描(PET)示踪剂用于淋巴瘤成像:在鼠模型中的 micro-PET 研究。

2-[18F]fludarabine, a novel positron emission tomography (PET) tracer for imaging lymphoma: a micro-PET study in murine models.

机构信息

CEA, DSV/I2BM, LDM-TEP Group, GIP Cyceron, Bd Henri Becquerel, , BP 5229, , 14074, Caen Cedex, France.

出版信息

Mol Imaging Biol. 2014 Feb;16(1):118-26. doi: 10.1007/s11307-013-0659-2.

Abstract

PURPOSE

Fludarabine has proven to be of considerable efficacy in the treatment of low-grade lymphomas. We have developed the labeling of this drug with fluorine-18 and evaluated 2-[(18)F]fludarabine as a novel positron emission tomography (PET) probe for in vivo imaging.

PROCEDURES

Preclinical studies were conducted with 2-[(18)F]fludarabine, in parallel with 2-deoxy-2-[(18)F]fluoro-D-glucose ([(18)F]FDG), in Swiss CD-1 and CB17 severely combined immunodeficient (SCID) mice, both as tumor-free control groups, and SCID mice bearing RL lymphomas.

RESULTS

In Swiss mice, micro-PET studies with 2-[(18)F]fludarabine showed a distribution restricted to the organs of excretion and the spleen, the latter being less evident in SCID animals. In lymphoma-bearing SCID mice, 2-[(18)F]fludarabine demonstrated a rapid tumor uptake over the first 20 min which subsequently plateaued and provided an improved contrast than that of [(18)F]FDG.

CONCLUSION

This radiotracer merits further evaluation to establish its clinical usefulness to image low-grade lymphoma in humans in future clinical investigations.

摘要

目的

氟达拉滨已被证明在治疗低级别淋巴瘤方面具有显著疗效。我们对该药物进行了氟-18 标记,并评估了 2-[(18)F]氟达拉滨作为一种新型正电子发射断层扫描(PET)探针用于体内成像。

方法

在瑞士 CD-1 和 CB17 严重联合免疫缺陷(SCID)小鼠中,与 2-脱氧-2-[(18)F]氟代-D-葡萄糖([(18)F]FDG)平行进行了 2-[(18)F]氟达拉滨的临床前研究,两者均作为无肿瘤对照组,以及携带 RL 淋巴瘤的 SCID 小鼠。

结果

在瑞士小鼠中,2-[(18)F]氟达拉滨的微 PET 研究显示其分布仅限于排泄器官和脾脏,而在 SCID 动物中后者则不明显。在携带淋巴瘤的 SCID 小鼠中,2-[(18)F]氟达拉滨在最初 20 分钟内快速摄取肿瘤,随后达到平台期,并提供了比 [(18)F]FDG 更好的对比度。

结论

该示踪剂值得进一步评估,以确定其在未来临床研究中用于人类低级别淋巴瘤成像的临床实用性。

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