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首页> 外文期刊>Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine >Comparative studies of 177Lu-EDTMP and 177Lu-DOTMP as potential agents for palliative radiotherapy of bone metastasis.
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Comparative studies of 177Lu-EDTMP and 177Lu-DOTMP as potential agents for palliative radiotherapy of bone metastasis.

机译：177Lu-EDTMP和177Lu-DOTMP作为姑息性骨转移放疗药物的比较研究。

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摘要

(177)Lu is presently considered as an excellent radionuclide for developing bone pain palliation agents owing to its suitable nuclear decay characteristics [T(1/2)=6.73d, E(beta)((max))=497keV, E(gamma)=113keV (6.4%) and 208keV (11%)] and large-scale production feasibility with adequate specific activity using moderate flux research reactors. Multidentate polyaminophosphonic acids have already been proven as the carrier molecule of choice for radiolanthanides and similar +3 metal ions in designing agents for palliative radiotherapy of bone pain due to skeletal metastases. The present paper describes a comparison between (177)Lu complexes of two potential polyaminophosphonic acid ligands, namely Ethylenediaminetetramethylene phosphonic acid (EDTMP) and 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetramethylene phosphonic acid (DOTMP) with respect to their radiochemical and in-vivo biological characteristics. Although both the agents have exhibited promising features, the study reveals that (177)Lu-EDTMP hasmarginally higher skeletal accumulation in comparison to that of (177)Lu-DOTMP, while the latter has slightly faster blood clearance along with lower retention in liver and kidneys in animal models.
机译：（177）Lu由于具有适当的核衰变特征[T（1/2）= 6.73d，Eβ（（max））= 497keV，E（γ），目前被认为是开发骨痛缓解剂的优良放射性核素。 ）= 113keV（6.4％）和208keV（11％）]，并且使用中等通量研究反应堆，具有足够的比活，可以大规模生产。多齿聚氨基膦酸已被证明是用于放射性镧系元​​素和类似的+3金属离子的选择载体，是设计用于骨转移性骨痛姑息放疗的设计剂。本文描述了两种潜在的聚氨基膦酸配体（乙二胺四亚甲基膦酸（EDTMP）和1,4,7,10-四氮杂环十二烷-1,4,7,10-四亚甲基膦酸（DOTMP）的（177）Lu配合物之间的比较）的放射化学和体内生物学特性。尽管两种药物均显示出令人鼓舞的功能，但研究表明（177）Lu-EDTMP与（177）Lu-DOTMP相比具有较高的骨骼蓄积，而后者的血液清除速度稍快，在肝脏和肝脏的滞留性较低。动物模型中的肾脏。

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