靶向HER3的在研抗体偶联药物——U3-1402

HER3-targeting antibody-drug conjugate——U3-1402

人表皮生长因子受体酪氨酸激酶抑制剂(epidermal growth factor receptor tyrosine kinase inhibitors,EGFR-TKI)是治疗非小细胞肺癌(non-small cell lung cancer,NSCLC)患者的一线治疗药物,但患者在治疗过程中易出现耐药现象。目前,对EGFR-TKI耐药的NSCLC患者尚无有效的治疗手段。U3-1402是由日本第一三共公司开发的靶向人表皮生长因子受体3(human epithelial growth factor receptor 3,HER3)的抗体偶联药物,临床研究表明其对各种EGFR耐药及耐药机制不明的NSCLC患者均有治疗效果,疾病控制率达100%。该药有望为EGFR-TKI耐药NSCLC患者带来新的治疗方案。本文就U3-1402的基本信息、作用机制、临床前研究和临床试验情况作一概述。

Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKI) are first-line drugs for patients with non-small cell lung cancer (NSCLC);However,patients could acquire resistance to EGFR-TKI with great possibilities during treatment.Unfortunately,potent treatments to acquired resistance are unavailable.U3-1402,an antibody-drug conjugate targeting HER3 antigen that is being developed by Daiichi Sankyo,has exhibited effective excellence against a variety of EGFR-TKI resistant mutations and even tumors with unknown mechanisms of resistance according to clinical studies.With a disease control rate of 100%,U3-1402 is expected to become a promising treatment for NSCLC patients with acquired resistance.The properties,mechanism,preclinical trials and clinical trials of U3-1402 was reviewed in this article.