177Lu-labeled cyclic polyaminophosphonates as potential agents for bone pain palliation

被引：64

作者：

Das, T

Chakraborty, S

Unni, PR

Banerjee, S

Samuel, G

Sarma, HD

Venkatesh, M

Pillai, MRA ^{[1
]}

机构：

[1] Bhabha Atom Res Ctr, Radiopharmaceut Div, Bombay 400085, Maharashtra, India

[2] Bhabha Atom Res Ctr, Div Radiat Biol, Bombay 400085, Maharashtra, India

来源：

APPLIED RADIATION AND ISOTOPES | 2002年 / 57卷 / 02期

关键词：

bone pain palliation; therapeutic radionuclide; Lu-177; cyclic phosphonates; bone agents;

D O I：

10.1016/S0969-8043(02)00104-5

中图分类号：

O61 [无机化学];

学科分类号：

070301 [无机化学]; 081704 [应用化学];

摘要：

Lu-177 (T-1/2 = 6.71 d, E-beta(max) = 497 keV) has radionuclidic properties suitable for use in palliative therapy of bone pain due to metastasis. Lu-177 was produced in high-specific activity (3-4 TBq/g) and excellent radionuclidic purity (100%) by thermal neutron bombardment of natural Lu target. Two cyclic tetraaminomethylene phosphonate ligands, namely DOTMP and CTMP were synthesized and radiolabeled with Lu-177. The Lu-177-DOTMP complex was formed with very high yield (>99%) and showed excellent stability (up to 40 d at room temperature). Biodistribution of Lu-177-DOTMP was carried out in Wistar rats and the complex showed significant bone uptake (4.23%/g in femur and 5.23% in tibia at 3 h p. i.), rapid clearance from blood (no activity at 3 h p. i.) and minimum uptake in soft tissues. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：177 / 184

页数：8

共 22 条

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