212Bi-DOTMP：一种用于靶向放疗的发射α粒子的亲骨性制剂。

212Bi-DOTMP: an alpha particle emitting bone-seeking agent for targeted radiotherapy.

作者信息

Hassfjell S P, Bruland O S, Hoff P

机构信息

Department of Chemistry, University of Oslo, Norway.

出版信息

Nucl Med Biol. 1997 Apr;24(3):231-7. doi: 10.1016/s0969-8051(97)00059-0.

DOI:10.1016/s0969-8051(97)00059-0

PMID:9228657

Abstract

The synthesis and in vivo stability of the bone-seeking alpha-particle emitting compounds 212Bi-DOTMP and 212Pb/212Bi-DOTMP are described. 212Bi-DOTMP, injected i.v. into Balb/c mice, showed prominent bone localization and a rapid clearance from blood and other organs. Femur/blood ratios increased from 13 at 15 min up to 490 at 2.0 h postinjection. Enhanced uptake of 212Bi-DOTMP was demonstrated in regions with high bone turnover. A comparison between 212Bi-DOTMP and [153Sm]Sm-EDTMP showed essentially no differences in biodistribution. 212Pb/212Bi-DOTMP followed a similar biodistribution, except for slightly elevated levels of 212Bi in the kidneys. The present study has shown 212Bi-DOTMP to be an in vivo stable bone-seeking radiopharmaceutical with promising biological properties for the treatment of sclerotic metastases and osteoblastic osteosarcoma.

摘要

本文描述了亲骨性发射α粒子的化合物212Bi-DOTMP和212Pb/212Bi-DOTMP的合成及其体内稳定性。静脉注射到Balb/c小鼠体内的212Bi-DOTMP显示出显著的骨定位以及从血液和其他器官的快速清除。注射后15分钟时股骨/血液比值为13，至2.0小时时增至490。在骨转换率高的区域显示出212Bi-DOTMP摄取增加。212Bi-DOTMP与[153Sm]Sm-EDTMP之间的生物分布基本没有差异。212Pb/212Bi-DOTMP遵循类似的生物分布，只是肾脏中212Bi的水平略有升高。本研究表明，212Bi-DOTMP是一种体内稳定的亲骨性放射性药物，对治疗硬化性转移瘤和成骨性骨肉瘤具有良好的生物学特性。