新型抗体偶联药物——维迪西妥单抗  

A novel antibody-drug conjugate:disitamab vedotin

作　　者：尹晓玉 路明 于泽芳 庞国勋[1,2] YIN Xiaoyu;LU Ming;YU Zefang;PANG Guoxun(Department of Pharmacy,Hebei General Hospital,Shijiazhuang 050051,Hebei,China;Hebei Key Laborato-ry of Clinical Pharmacy,Shijiazhuang 050051,Hebei,China;Department of Pharmacy,The Second Hospital of Hebei Medical University,Shijiazhuang 050000,Hebei,China)

机构地区：[1]河北省人民医院药学部,河北石家庄050051 [2]河北省临床药学重点实验室,河北石家庄050051 [3]河北医科大学第二医院药学部,河北石家庄050000

出　　处：《中国临床药理学与治疗学》2024年第11期1315-1320,共6页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：2022年度河北省医学科学研究课题计划(20220054);2024年度河北省医学科学研究课题计划(20241993)。

摘　　要：抗体药物偶联物(ADC)是一类新型抗肿瘤药物,其结构中的连接子将细胞毒性药物连接到单克隆抗体,并将细胞毒药物靶向释放至肿瘤细胞。维迪西妥单抗(RC48)是我国独立自主研发的新型抗体偶联药物,以肿瘤表面的HER2蛋白为靶点,兼具抗体靶向性和小分子药物杀伤性,能精准识别和杀伤肿瘤细胞。与传统的HER2靶向药物相比,维迪西妥单抗治疗窗更宽,对正常组织的毒性更小。目前,注射用维迪西妥单抗已经被国家药品监督管理局(NMPA)批准用于至少接受过2种系统化疗的HER2过表达(HER2免疫组织化学检查结果为2+或3+)局部晚期或转移性胃癌(包括胃食管结合部腺癌)的患者,以及既往接受过含铂化疗且HER2过表达即免疫组化检查结果为2+或3+的局部晚期或转移性尿路上皮癌患者。本文对维迪西妥单抗的结构特征、作用机制以及临床试验研究情况进行综述,并对该药物的临床应用前景予以展望。Antibody drug conjugates(ADCs)are a new class of anti-tumor drugs in which linkers in the structure link cytotoxic drugs to monoclonal an-tibodies and release cytotoxic drugs to tumors.Disi-tamab vedotin(RC48)is a new antibody-drug con-jugate independently developed in China.It targets the HER2 protein on the surface of tumors,it has both antibody targeting and small molecule drug killing,and can accurately recognize and kill tumor cells.Compared with traditional HER2-targeted drugs,disitamab vedotin has a wider therapeutic window and less toxicity to normal tissues.Current-ly,disitamab vedotin for injection has been ap-proved by the National Medical Products Adminis-tration(NMPA)for use in patients with HER2 over-expression(HER2 immunohistochemical results of 2+or 3+)who have locally advanced or metastatic gastric cancer(including gastroesophageal junction adenocarcinoma)and have received at least two types of systemic chemotherapy.Additionally,it is indicated for patients with locally advanced or met-astatic urothelial carcinoma who have previously undergone platinum-containing chemotherapy and exhibit HER2 overexpression,specifically 2+or 3+immunohistochemical results.In this paper,we will review the structural characteristics,mechanism of action and clinical trials of disitamab vedotin and look forward to the clinical application prospects of this drug.

关 键 词：抗体偶联靶向药物 维迪西妥单抗 人表皮生长因子受体2 

分 类 号：R969[医药卫生—药理学]