Incyte Corporation, Experimental Station, Wilmington, DE 19880, USA.
Expert Opin Investig Drugs. 2011 Sep;20(9):1225-41. doi: 10.1517/13543784.2011.600687. Epub 2011 Jul 11.
The aberrantly upregulated c-mesenchymal-epithelia transition factor (c-MET) signaling pathway has been considered to be an attractive target for cancer intervention owing to the important roles it plays in tumor formation, progression, metastasis, angiogenesis and drug resistance. Based on the historical preclinical evidence, a number of c-MET pathway targeted agents are being developed in the clinic, and recent clinical data have begun to provide some insight into which tumor types and patient populations a c-MET pathway inhibitor may be beneficial for.
Through reviewing recent publications in the literature and information disclosed in other public forums, we describe the current understanding of c-MET biology in human malignancies and discuss the latest progress in the development of c-MET pathway inhibitors for cancer treatment.
The c-MET pathway inhibitors currently being evaluated in the clinic have demonstrated compelling evidence of clinical activity in different cancer types and may provide significant therapeutic opportunities. The challenges, however, are to identify the tumor types and patient populations that benefit most, and find the most effective combinations of therapies while minimizing potential toxicity.
异常上调的 c-间质上皮转化因子（c-MET）信号通路，由于其在肿瘤形成、进展、转移、血管生成和耐药性方面的重要作用，被认为是癌症干预的一个有吸引力的靶点。基于历史的临床前证据，许多 c-MET 通路靶向药物正在临床开发中，最近的临床数据开始为哪种肿瘤类型和患者群体可能受益于 c-MET 通路抑制剂提供了一些见解。
通过回顾文献中的最新出版物和其他公开论坛中披露的信息，我们描述了人类恶性肿瘤中 c-MET 生物学的当前认识，并讨论了 c-MET 通路抑制剂在癌症治疗中的最新进展。
目前正在临床评估的 c-MET 通路抑制剂在不同的癌症类型中显示出了令人信服的临床活性证据，可能提供了重要的治疗机会。然而，挑战在于确定受益最大的肿瘤类型和患者群体，并找到最有效的治疗组合，同时最小化潜在的毒性。
