以人类表皮生长因子受体为靶点的乳腺癌抗体偶联药物研究进展  

Advances in Antibody-drug Conjugate Targeting Human Epidermal Growth Factor Receptor for Breast Cancer

作　　者：杨绍时[1] 柴慈曼 王宏[1] YANG Shaoshi;CHAI Ciman;WANG Hong(Department of Thyroid and Breast Surgery,the Second Hospital of Tianjin Medical Universiry,Tianjin 300211,China)

机构地区：[1]天津医科大学第二医院甲状腺乳腺外科,天津300211

出　　处：《医学综述》2023年第14期2788-2793,共6页Medical Recapitulate

摘　　要：近年来,乳腺癌分子靶向药物研发取得了飞速发展,其中乳腺癌抗体偶联药物(ADC)是非常有前途的新型靶向治疗药物,以人类表皮生长因子受体为靶点的多种ADC(恩美曲妥珠单抗、曲妥珠单抗-德卢替康)已经获批上市,还有些处于临床试验后期(Trastuzumab Duocarmazine、维迪西妥单抗等)。另外,也有一些新型的ADC仍处于研究初级阶段,甚至因为严重的副作用终止了研究。由于细胞内作用机制和乳腺肿瘤细胞抗原表达量限制,ADC脱靶引起的副作用以及耐药性的存在阻碍了其进一步发展。为了增强细胞毒性药物疗效,新型ADC应在提高细胞毒性药物递送效率、减少脱靶效应等方面进行改良。In recent years,the development of molecular targeted drugs for breast cancer has developed rapidly.Among them,antibody-drug conjugate(ADC)for breast cancer are very promising new targeted therapeutic drugs.A variety of ADC targeting human epidermal growth factor receptor(Trastuzumab Emtansine,Trastuzumab Deruxtecan)have been approved for marketing,and some are in the late stage of clinical trials(Trastuzumab Duocarmazine,Disitamab Vedotin,etc.).In addition,some new ADC are still in the initial stage of research,and even terminated because of serious adverse effects.Due to the limitation of intracellular mechanism and antigen expression of breast tumor cells,the side effects and drug resistance caused by off-target of ADC hinder its development.In order to enhance the efficacy of cytotoxic drugs,new ADC should be improved in improving the delivery efficiency of cytotoxic drugs and reducing the off-target effect.

关 键 词：乳腺癌 人类表皮生长因子受体 抗体偶联药物 靶向治疗 

分 类 号：R737.9[医药卫生—肿瘤]