⁹⁰Y-DOTA-Nimotuzumab: Synthesis of a Promising β- Radiopharmaceutical.

IF 1.5 4区医学 Q3 PHARMACOLOGY & PHARMACY

Current radiopharmaceuticals Pub Date : 2022-01-01 DOI:10.2174/1874471013999210104220031

Teresa Scotognella, Daria Maccora, Isabella Bruno, Marco Chinol, Massimo Castagnola, Francesco Collamati, Carlo Mancini-Terraciano, Silvio Morganti, Valerio Bocci, Elena Solfaroli Camillocci, Dante Rotili, Antonella Cartoni, Ilaria Fratoddi, Federica Marini, Iole Venditti, Riccardo Faccini, Alessandro Giordano

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引用次数: 1

Abstract

Background: Nimotuzumab is a humanized anti-epidermal growth factor receptor (EGFR) monoclonal antibody, nowadays used for tumour immunochemotherapy. This study aimed to label the conjugate DOTA-nimotuzumab with yttrium-90, in order to provide a β- emitting radioimmunoconjugate (⁹⁰Y-DOTA-nimotuzumab) potentially useful to assess the feasibility of a new radio-guided surgery approach.

Methods: The synthesis of 90Y-DOTA-nimotuzumab was performed in two days. Nimotuzumab was conjugated with a 50-fold excess of DOTA and then labelled with 90Y3+. The ⁹⁰Y-DOTA-nimotuzumab preparation was optimized considering several parameters such as pH, temperature and reaction volume. Moreover, the ⁹⁰Y-DOTA-nimotuzumab stability was evaluated in human plasma.

Results: The radioimmunoconjugate ⁹⁰Y-DOTA-nimotuzumab was obtained with a radiochemical purity greater than 96%, and showed a good stability at 20°C as well as at 37°C in human plasma.

Conclusions: The optimized conditions for a mild and easy preparation of ⁹⁰Y-DOTA-nimotuzumab joined to a promising stability under physiological conditions suggest to propose this radioimmunoconjugate as a potential diagnostic radiopharmaceutical for β- radio-guided surgery.

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90Y-DOTA-Nimotuzumab:一种有前途的β-放射性药物的合成。

背景:尼莫单抗是一种人源抗表皮生长因子受体(EGFR)单克隆抗体，目前用于肿瘤免疫化疗。本研究旨在用钇-90标记DOTA-nimotuzumab偶联物，以提供一种β-放射免疫偶联物(90Y-DOTA-nimotuzumab)，可能有助于评估一种新的放射引导手术方法的可行性。方法:90y - dota -尼莫单抗在2天内合成。尼莫妥珠单抗与50倍过量的DOTA偶联，然后用90Y3+标记。考虑pH、温度、反应体积等参数对90Y-DOTA-nimotuzumab制剂进行了优化。此外，90Y-DOTA-nimotuzumab在人血浆中的稳定性进行了评估。结果:获得放射免疫偶联物90Y-DOTA-nimotuzumab，放射化学纯度大于96%，在20℃和37℃的人血浆中均表现出良好的稳定性。结论:90Y-DOTA-nimotuzumab的制备工艺温和易行，且在生理条件下具有良好的稳定性，表明该放射免疫偶联物有望成为β-放射引导手术的潜在诊断放射性药物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Current radiopharmaceuticals PHARMACOLOGY & PHARMACY-

CiteScore

3.20

自引率

4.30%

发文量