| 治疗非小细胞肺癌脑转新药:Zorifertinib |
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| 引用本文： | 郭婷婷,朱双圆,李明,谭绍英.治疗非小细胞肺癌脑转新药:Zorifertinib[J].广州化学,2021(2):1-5,59. |
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| 作者姓名： | 郭婷婷 朱双圆 李明 谭绍英 |
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| 作者单位： | 上海工程技术大学化学化工学院;中国医药工业研究总院上海医药工业研究院创新药物与制药工艺国家重点实验室 |
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| 基金项目： | 国家自然科学基金(31702070);上海市青年科技启明星计划(18QB1404000);上海市自然科学基金(19ZR1437900)。 |
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| 摘 要： | 新药Zorifertinib是阿斯利康公司针对非小细胞肺癌(NSCLC)脑转研发的一种表皮生长因子酪氨酸激酶抑制剂(EGFR-TKI),对EGFR 19外显子缺失和EGFR 21外显子L858R突变有高选择性和高抑制性,相较于其他EGFR-TKIs的突出优势是具有优秀的血脑屏障渗透性。临床研究表明Zorifertinib可以在脑内达到等同血浆的药物浓度,有效抑制脑内肿瘤生长,减少脑内肿瘤面积,并且预防脑内肿瘤形成。本文将对该新药的作用机制、研发历程、药代动力学、临床研究和安全性进行综述,为广大研究者以及今后的临床应用提供参考。
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| 关 键 词： | Zorifertinib 表皮生长因子酪氨酸激酶抑制剂 血脑屏障 肺癌脑转 |
An Effective New Drug in Treatment of Non-small Cell Lung Cancer with Brain Metastases(BM)and Leptomeningeal Metastases(LM):Zorifertinib |
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| GUO Ting-ting,ZHU Shuang-yuan,LI Ming,TAN Shao-ying.An Effective New Drug in Treatment of Non-small Cell Lung Cancer with Brain Metastases(BM)and Leptomeningeal Metastases(LM):Zorifertinib[J].Guangzhou Chemistry,2021(2):1-5,59. |
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| Authors: | GUO Ting-ting ZHU Shuang-yuan LI Ming TAN Shao-ying |
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| Institution: | (College of Chemistry and Chemical Engineering,Shanghai University of Engineering Science,Shanghai 201620,China;State Key Lab of New Drug and Pharmaceutical Process,Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry,Shanghai 201203,China) |
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| Abstract: | Zorifertinib is a new drug developed by AstraZeneca for brain metastases(BM)or leptomeningeal metastases(LM)of non-small cell lung cancer(NSCLC).It is an oral small molecule epidermal growth factor tyrosine kinase inhibitor(EGFR-TKI)which has high selectivity and high inhibition to EGFR 19 exon deletion and EGFR 21 exon L858R mutation.Compared with other EGFR TKIs,Zorifertinib has excellent blood-brain barrier permeability.Clinical trials have confirmed that Zorifertinib can reach the drug concentration similar to plasma in brain so that can effectively inhibit the growth of brain tumor,reduce the area of brain tumor,and prevent the formation of brain tumor.In this paper,the mechanism of action,research and development,pharmacokinetics,clinical research and safety of the new drug will be reviewed to provide reference for researchers and clinical application in the future. |
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| Keywords: | Zorifertinib epidermal growth factor tyrosine kinase inhibitor blood-brain barrier(BBB) lung cancer with brain metastases(BM)or leptomeningeal metastases(LM) |
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