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

被引：41

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

页码：497 / 505

页数：9

共 20 条

[1] The addition of DTPA to [177Lu-DOTA0,Tyr3]octreotate prior to administration reduces rat skeleton uptake of radioactivity [J].