乐伐替尼治疗中晚期肿瘤的临床研究进展

Progress in the treatment of advanced cancer with lenvatinib

乐伐替尼(lenvatinib)作为一种多靶点酪氨酸酶抑制(tyrosine kinase inhibitor,TKI),可以抑制血管内皮生长因子受体(vascular endothelial growth factor receptors,VEGFRs)1,2,3,成纤维细胞生长因子受体(fibroblast growth factor receptors,FGFR)1,2,3和4,血小板衍生生长因子受体α(platelet-derived growth factor receptor alpha,PDGFRα),KIT以及RET信号通路,于2015年2月13日获FDA批准用于晚期放射性碘难治性分化型甲状腺癌(radioactive iodine-refractory differentiated thyroid cancer,RR-DTC)的治疗。但由于乐伐替尼可以通过多条途径抑制肿瘤抑制生长,因此近年来乐伐替尼逐渐开始应用于其他晚期肿瘤的治疗,且可以获得一定的临床疗效。本文主要就乐伐替尼在黑色素瘤、肾癌、肝癌、非小细胞肺癌(non-small-cell lung carcinoma,NSCLC)以及子宫内膜癌患者中的作用机制、临床疗效以及不良反应展开研究。

Lenvatinib is a multi-targeted tyrosine kinase inhibitor（TKI） of vascular endothelial growth factor receptors（VEGFRs） 1,2 and 3,fibroblast growth factor receptors（FGFR） 1,2,3 and 4,platelet-derived growth factor receptor alpha（PDGFRα）,and RET and KIT signalling networks,and it was approved by FDA for the treatment of advanced radioactive iodine-refractory differentiated thyroid cancer（RR-DTC） on february 13,2015.As lenvatinib can suppress the growth of tumors in different ways,lenvatinib is applied to other kinds of tumors in recent years,such as malignant molenoma,renal cancer,liver cancer,NSCLC and endometrial cancer gradually,and some patients benifitted from it. In this article,a review was made on the mechanism,clinical efficacy and adverse events of lenvatinib in the treatment of advanced cancer.