Synthesis, stabilization and formulation of [177Lu]Lu-AMBA, a systemic radio therapeutic agent for Gastrin Releasing Peptide receptor positive tumors

被引：39
|
作者：
Chen, Jianqing [1 ]
Linder, Karen E. [1 ]
Cagnolini, Aldo [1 ]
Metcalfe, Edmund [1 ]
Raju, Natarajan [1 ]
Tweedle, Michael F. [1 ]
Swenson, Rolf E. [1 ]
机构：
[1] Bracco Res USA Inc, Princeton, NJ 08540 USA
来源：
APPLIED RADIATION AND ISOTOPES | 2008年 / 66卷 / 04期
关键词：
Lu-177-AMBA; bombesin; gastrin releasing peptide; targeted radiotherapy; radiolysis protection;
D O I：
10.1016/j.apradiso.2007.11.007
中图分类号：
O61 [无机化学];
学科分类号：
070301 ; 081704 ;
摘要：
A robust formulation was developed for [Lu-177]Lu-AMBA (Lu-177-DO3A-CH2CO-G-[4-aminobenzoyl]-QWAVGHLM-NH2), a Bombesin-like agonist with high affinity for Gastrin Releasing Peptide (GRP) receptors. During optimization of labeling, the effect of several radiostabilizers was evaluated; a combination of selenomethionine and ascorbic acid showed superiority over other tested radiostabilizers. The resulting two-vial formulation maintains a radiochemical purity (RCP) of >90% for at least 2 days at room temperature. The method of stabilization should be useful for other methionine-containing peptide radiopharmaceuticals in diagnostic and therapeutic applications. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：497 / 505
页数：9
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