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2026, 01, v.48 21-27
Development of Chemical Functional Materials for Identifying New Antitumor Drug A166
Email: lvn1314@126.com;donglinyi@tmu.edu.cn;
DOI: 10.13822/j.cnki.hxsj.2025.0199
摘要:

A166是一种靶向HER2的ADC药物,主要针对HER2阳性乳腺癌及其他HER2表达的实体瘤。用药后的临床药物检测对于临床指导用药来说至关重要,不仅可以优化给药方案,以提高疗效、减少毒副作用,还可以减少耐药情况的产生。目前临床血药浓度监测(TDM)的主要方法包括免疫分析法、色谱法(如高效液相色谱法HPLC)以及新兴的床旁检测技术(如质谱法)。但是存在对操作人员要求高、价格昂贵、设备维护、步骤繁琐等缺点。为了解决A166血液浓度监测的问题,创新性地提出了将硼酸与修饰罗丹明6G荧光素负载氧化石墨烯(HR6GGO)与硼酸亲和导向表面印迹磁性纳米颗粒(MIP-A166)相结合,用于药物A166在体内的血药浓度监测。经硼酸修饰并负载大量罗丹明6G荧光素的HR6GGO材料,可通过硼酸亲和作用选择性标记A166,实现荧光信号放大与输出。成功制备了HRBGO和MIP-A166,通过实验优化,得到的MIP-A166-HRBGO策略对A166的检测具有超高灵敏度和优越的特异性。MIP-A166则借助硼酸亲和分子印迹识别机制,对模板药物表现出特异性选择能力。MIP-A166偶联HR6GG0的夹心检测策略依托双重硼酸亲和协同作用,展现出普适性应用潜力,为临床药物监测以及指导用药提供帮助。

Abstract:

A166 is an ADC drug targeting HER2,mainly used for the treatment of HER2-positive breast cancer and other solid tumors expressing HER2.Clinical drug monitoring after administration is crucial for clinical medication guidance, as it can optimize the dosing regiments to enhance efficacy, minimize side effects, and reduce the development of drug resistance.Currently, the main methods for therapeutic drug monitoring(TDM) include immunoassay methods, chromatography methods(such as high-performance liquid chromatography HPLC),and emerging point-of-care technologies(such as mass spectrometry).However, these methods have several drawbacks, including the need for highly trained operators, high cost, equipment maintenance, and complex procedures.To address the challenge of monitoring A166 blood concentration, a novel strategy was proposed by combining boronic acid-modified rhodamine 6G-functionalized graphene oxide(HR6GGO) with a boronic acid-affinity molecularly imprinted magnetic nanoparticle(MIP-A166).The HR6GGO material, modified with borate and loaded with a large amount of rhodamine 6G fluorescent dye, can selectively label A166 through boronic acid affinity, achieving fluorescence signal amplification and output.HRBGO and MIP-A166 were successfully prepared and the MIP-A166-HRBGO strategy achieved extremely high sensitivity and excellent specificity for the detection of A166 after experimental optimization.MIP-A166 utilizes the boronic acid affinity molecular imprinting recognition mechanism, showing specific selectivity for the template drug.The sandwich detection strategy, based on the coupling of MIP-A166 with HR6GGO,relies the dual boronic acid affinity synergism, demonstrating board application potential and providing a promising tool for clinical drug monitoring and medication guidance.

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Basic Information:

DOI:10.13822/j.cnki.hxsj.2025.0199

China Classification Code:TB34;TQ460.1

Citation Information:

[1]孙梦婷,王冬,董林毅.用于识别抗肿瘤新药A166的化学功能材料的开发[J].化学试剂,2026,48(01):21-27.DOI:10.13822/j.cnki.hxsj.2025.0199.

Fund Information:

白求恩公益基金会第二期恒学精进-医学研究项目(20240602); 天津医学重点学科专科项目(TJYXZDXK-009A)

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