多靶点抗肿瘤新药索拉非尼的研究进展

Recent advances in sorafenib:A multiple targeted anti-tumor agent

索拉非尼(sorafenib)是一种小分子的多靶点口服抗癌新药,不仅能抑制VEGFR、PDGFR、FLT3和KIT受体酪氨酸激酶活性,还是RAF激酶的强效抑制剂。索拉非尼既能抑制血管的形成又能直接抑制肿瘤细胞的增殖。索拉非尼的推荐剂量为400mg,每日两次。索拉非尼二线治疗转移性肾透明细胞癌较安慰剂明显延长患者的无进展生存期和总生存期,因此,已获得美国FDA批准。索拉非尼的主要不良反应包括手足综合征、高血压、腹泻、皮疹、乏力。

Sorafenib is a novel and oral multiple targeted agent which inhibits the tyrosine kinase activity of VEGFR, PDGFR, FLT3 and KIT as well as the serine/threonine kinase activity of RAF. Sorafenib exerts anti - tumor activity via dual mechanism ： inhibition of angiogenesis and directly anti - proliferation against tumor cell. The recommended dose of sorafenib is 400mg, bid. A large double - blinded randomized phase Ⅲ clinical trial has revealed that sorafenib significantly prolonged the PFS and OS of patients with metastatic clear renal cell carcinoma who had failed first line cytokine therapy. The most common adverse effect of sorafenib includes hand -foot syndrome, hypertension, skin rash and asthenia.