Tivantinib  

作　　者：田红[1] 肖桂芝[1] 于鹏[1] 陈常青[1] 

机构地区：[1]天津药物研究院医药信息中心,天津300193

出　　处：《现代药物与临床》2011年第3期240-243,共4页Drugs & Clinic

摘　　要：c-Met在很多肿瘤中过度表达,并在控制多信号转导途径(包括肿瘤生长和转移)中发挥重要作用。Tivantinib是一个口服有效的小分子c-Met受体酪氨酸激酶抑制剂,为新型的靶向抗肿瘤药,由美国ArQule公司、日本Daiichi和Kyowa HakkoKirin公司联合开发,用于治疗多种癌症。目前,本品正在进行的临床研究涉及的肿瘤种类主要有小眼转录因子(microphthalmia transcription factor,MiT)型肿瘤、非小细胞肺癌、结肠直肠癌、胃癌、肝细胞癌、胰腺癌、生殖细胞癌和实体瘤等。Tivantinib显示出抗肿瘤谱广、疗效确切、不良反应较轻、患者耐受性好等特点。c-Met is overexpressed in many tumors, and plays key roles in controlling multiple signal transduction pathways involved in tumour growth and metastasis. Tivantinib is an orally available, small molecule inhibitor of the c-Met receptor tyrosine kinase under development by ArQule, in collaboration with Daiichi Sankyo and Kyowa Hakko Kirin for the treatment of many types of cancer. Clinical development is underway for the treatment of microphthalmia transcription factor （MiT） tumours, non-small cell lung cancer, colorectal cancer, gastric cancer, hepatocellnlar carcinoma, pancreatic cancer, germ cell cancer, and solid tumours as well. MiT tumours include clear cell sarcoma, alveolar soft part sarcoma, and translocation-associated renal cell carcinoma. In clinical trials to date. Tivantinib indicates the charcaterists with broad-spectrum anti-tumor, curative effect, less adverse reactions well tolerated in patients, etc.

关 键 词：Tivantinib ARQ-197 c—Met受体酪氨酸激酶抑制剂 靶向药物 抗肿瘤 临床研究 

分 类 号：R97[医药卫生—药品]