Abstract：
The cell-surface receptor tyrosine kinase c-mesenchymal-epithelial transition factor (c-Met) is overexpressed in a wide range of solid tumors, making it an appropriate target antigen for the development of anticancer therapeutics. Various antitumor c-Met-targeting therapies (including monoclonal antibodies [mAbs] and tyrosine kinases) have been developed for the treatment of c-Met-overexpressing tumors, most of which have so far failed to enter the clinic because of their efficacy and complications. Antibody-drug conjugates (ADCs), a new emerging class of cancer therapeutic agents that harness the target specificity of mAbs to deliver highly potent small molecules to the tumor with the minimal damage to normal cells, could be an attractive therapeutic approach to circumvent these limitations in patients with c-Met-overexpressing tumors. Of great note, there are currently nine c-Met-targeting ADCs being examined in different phases of clinical studies as well as eight preclinical studies for treating various solid tumors. The purpose of this study is to present a broad overview of clinical- and preclinical-stage c-Met-targeting ADCs.
摘要：
细胞表面受体酪氨酸激酶c-间质上皮转化因子(c-Met)在多种实体瘤中过度表达,使其成为开发抗癌疗法的合适靶抗原。已经开发了各种抗肿瘤c-Met靶向疗法（包括单克隆抗体[mAb]和酪氨酸激酶）用于治疗c-Met过表达的肿瘤。到目前为止，大多数由于疗效和并发症而未能进入临床。抗体-药物缀合物（ADC），一种新出现的癌症治疗剂，它利用单克隆抗体的靶特异性向肿瘤提供高效的小分子，对正常细胞的损伤最小。在c-Met过表达肿瘤的患者中，可能是一种有吸引力的治疗方法来规避这些限制。值得注意的是，目前有9个c-Met靶向ADC在不同阶段的临床研究以及8个临床前研究中用于治疗各种实体瘤.这项研究的目的是提供临床和临床前阶段c-Met靶向ADC的广泛概述。
