| 许 斌,谌 亮,宋启斌.Tivantinib治疗肝细胞癌的研究进展[J].肿瘤学杂志,2018,24(7):722-728. |
| Tivantinib治疗肝细胞癌的研究进展 |
| Research Progress of Tivantinib in Treatment of Hepatocellular Carcinoma |
| 投稿时间：2017-06-21 |
| DOI：10.11735/j.issn.1671-170X.2018.07.B014 |
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| 中文关键词: Tivantinib ARQ-197 肝细胞癌 MET抑制剂 |
| 英文关键词:Tivantinib ARQ-197 hepatocellular carcinoma met inhibitor |
| 基金项目:武汉大学2016年度自主科研项目（自然科学类）（2042016kf0088） |
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| 中文摘要: |
| 摘 要：索拉菲尼（Sorafenib）是迄今为止最常用于治疗晚期肝细胞癌的药物，但其疗效尚有限。Tivantinib(ARQ-197)是c-MET的非ATP竞争性抑制剂。对于Sorafenib治疗失败或不耐受的晚期肝细胞癌患者，Tivantinib在Ⅰ期和Ⅱ期试验中显示生存获益。肿瘤细胞MET高表达可能与Tivantinib治疗获益有相关性。目前，两个大的随机、双盲、安慰剂对照的Ⅲ期试验［METIV-HCC (NCT01755767)和JET-HCC(NCT02029157)］正在评估Tivantinib在MET高表达的晚期肝细胞癌患者的总体生存率和无进展生存期中的作用。全文综述了Tivantinib治疗晚期肝细胞癌的证据以及Tivantinib使用相关的药理学、剂量、毒性和生物标志物等问题。 |
| 英文摘要: |
| Abstract：Sorafenib is the most commonly used drug for the treatment of advanced hepatocellular carcinoma(HCC). Tivantinib(ARQ-197) is a non-ATP competitive inhibitor of cellular mesenchymal-epithelial transcription factor(c-MET). In phase Ⅰ and Ⅱ trials，it showed a survival benefit for patients with advanced HCC who failed or were intolerant to sorafenib，and the efficacy of tivantinib therapy might be associated with high expression of MET(MET-high) in the cancer cells. Currently，in two ongoing large randomized double-blind placebo-controlled phase Ⅲ trials ［METIV-HCC(［NCT01755767) and JET-HCC(NCT02029157)］，the efficacy of tivantinib for patients with MET-high advanced HCC is being evaluated with overall survival and progression-free survival as the primary end points. This article reviews the recent progress of tivantinib in treatment of advanced HCC，focusing on the pharmacology，dosing，toxicity and biomarkers associated with ivantinib use. |
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