[關(guān)鍵詞]
[摘要]
c-Met在很多腫瘤中過度表達,并在控制多信號轉(zhuǎn)導途徑(包括腫瘤生長和轉(zhuǎn)移)中發(fā)揮重要作用。Tivantinib是一個口服有效的小分子c-Met受體酪氨酸激酶抑制劑,為新型的靶向抗腫瘤藥,由美國ArQule公司、日本Daiichi和Kyowa Hakko Kirin公司聯(lián)合開發(fā),用于治療多種癌癥。目前,本品正在進行的臨床研究涉及的腫瘤種類主要有小眼轉(zhuǎn)錄因子(microphthalmia transcription factor,MiT)型腫瘤、非小細胞肺癌、結(jié)腸直腸癌、胃癌、肝細胞癌、胰腺癌、生殖細胞癌和實體瘤等。Tivantinib顯示出抗腫瘤譜廣、療效確切、不良反應較輕、患者耐受性好等特點。
[Key word]
[Abstract]
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, hepatocellular 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.
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