| 郝 月,卫静文,宋正波.抗体-细胞毒偶联药物在实体瘤治疗中的耐药机制[J].肿瘤学杂志,2022,28(5):396-401. |
| 抗体-细胞毒偶联药物在实体瘤治疗中的耐药机制 |
| Mechanism of Drug Resistance of Antibody-drug Conjugates in Treatment of Solid Tumor |
| 投稿时间：2022-01-19 |
| DOI：10.11735/j.issn.1671-170X.2022.05.B010 |
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| 中文关键词: 抗体-细胞毒偶联药物 耐药机制 人表皮生长因子受体2 实体肿瘤 |
| 英文关键词:antibody-drug conjugates resistance mechanism human epidermal growth factor receptor 2 solid tumor |
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| 摘要点击次数: 733 |
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| 中文摘要: |
| 摘 要：新一代的由抗体及细胞毒性成分连接而成的抗体-细胞毒偶联药物在抗肿瘤治疗领域实现新突破，因其具备特异性地结合到抗原表面及内化于肿瘤细胞内产生强大杀伤作用的特点得到广泛关注。目前，针对人表皮生长因子受体2（HER2）阳性患者的Trastuzumab emtansine和Trastuzumab deruxtecan已初显成效。随后，针对各种不同靶向基因的偶联药物也在不断探索中。但由于肿瘤抗原水平的表达、药物内吞迁移的抑制、溶酶体功能障碍、药物外排泵以及靶点突变等引发了相关的耐药。全文对抗体-细胞毒偶联药物的耐药机制进行综述。 |
| 英文摘要: |
| Abstract： The new generation of antibody-drug conjugates has achieved breakthroughs in anti-tumor therapy，which exerts killing effects on tumor through specific binding to the cell surface and drug internalization in tumor cells. Currently，Trastuzumab emtansine and Trastuzumab deruxtecan have shown initial success in treatment of patients with human epidermal growth factor receptor 2(HER2) positive cancer. New antibody-drugs conjugates targeting to various genes are also being explored. However，the expression level of tumor antigen，inhibition of drug endocytosis migration，lysosomal dysfunction，drug efflux pump，and target mutation may lead to drug resistance. The drug resistance mechanism of antibody-drug conjugates is reviewed in this article. |
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