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Synthesis and biological evaluation of 99mTc(CO)3(IDA-CPT) for tumor imaging

✍ Scribed by Jianjun Wang; Tingting Niu; Jing Yang; Cunmin Tan; Xiaobei Zheng; Wangsuo Wu; Feng Dong; Hongyun Guo

Publisher
John Wiley and Sons
Year
2009
Tongue
French
Weight
89 KB
Volume
52
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

This work reports the synthesis, radiolabeling, and preliminary biodistribution results in tumor‐bearing mice of ^99m^Tc(CO)~3~(IDA‐CPT). The novel camptothecin (CPT) derivate was successfully synthesized by conjugation of iminodiacetic acid (IDA) to camptothecin via a short carbonyl‐methylene linker. Radiolabeling was performed in high yield with [^99m^Tc(CO)~3~]^+^ core to get ^99m^Tc(CO)~3~(IDA‐CPT), which was hydrophilic and stable at room temperature. Biodistribution studies in tumor‐bearing mice showed that ^99m^Tc(CO)~3~(IDA‐CPT) accumulated in the tumor with good uptake and retention. However, its clearance from normal organs was slow, resulting in poor T/NT ratios. Further modification on the linker or/and ^99m^Tc‐chelate to improve the tumor‐targeting efficacy and in vivo kinetic profiles is currently in progress. Copyright © 2009 John Wiley & Sons, Ltd.

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