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[177Lu]Lu-AMBA的合成、稳定化及制剂研究，一种用于胃泌素释放肽受体阳性肿瘤的全身放射治疗剂

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

作者信息

Chen Jianqing, Linder Karen E, Cagnolini Aldo, Metcalfe Edmund, Raju Natarajan, Tweedle Michael F, Swenson Rolf E

机构信息

Bracco Research USA Inc., 305 College Road East, Princeton, NJ 08540, USA.

出版信息

Appl Radiat Isot. 2008 Apr;66(4):497-505. doi: 10.1016/j.apradiso.2007.11.007. Epub 2007 Nov 19.

DOI:10.1016/j.apradiso.2007.11.007
PMID:18178448
Abstract

A robust formulation was developed for [(177)Lu]Lu-AMBA ((177)Lu-DO3A-CH(2)CO-G-[4-aminobenzoyl]-QWAVGHLM-NH(2)), 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.

摘要

针对[(177)Lu]Lu - AMBA（(177)Lu - DO3A - CH(2)CO - G - [4 - 氨基苯甲酰基] - QWAVGHLM - NH(2)）开发了一种稳健的制剂，[(177)Lu]Lu - AMBA是一种对胃泌素释放肽（GRP）受体具有高亲和力的类蛙皮素激动剂。在标记优化过程中，评估了几种放射性稳定剂的效果；硒代蛋氨酸和抗坏血酸的组合显示出优于其他测试的放射性稳定剂。所得的双瓶制剂在室温下至少2天保持>90%的放射化学纯度（RCP）。这种稳定化方法对于诊断和治疗应用中其他含蛋氨酸的肽放射性药物应该是有用的。

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