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[摘要]:As an oncogene, hepatocyte growth factor receptor (proto-oncogene c-Met; MET) is known to be overexpressed and/or mutated in many types of cancer and plays a critical role in cancer cell survival, proliferation, angiogenesis, invasion and metastasis. c-Met encodes fora tyrosine-protein kinase receptor that is activated by hepatocyte growth factor (HGF). Tivantinib is a selective, orally active c-Met inhibitor. Tivantinib binds directly to the c-Met protein in a selective manner and disrupts the c-Met signal transduction pathway. Preclinical studies have demonstrated unique inhibition of c-Met activation in numerous human cancer cell lines. Phase I and II clinical trials indicate that this c-Met inhibitor shows clinical promise in terms of safety, tolerability and efficacy for the treatment of c-Met-associated cancers. |
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