小分子酪氨酸激酶抑制剂regorafenib研究进展

The Progress of Small Tyrosinekinases Inhibitor Regorafenib

regorafenib(BAY 73-4506,Stivarga®)是新型的口服小分子多激酶抑制剂,可广泛抑制与血管生成和肿瘤发生相关的靶激酶。该药影响的作用通路以及用于监测该药物疗效的生物标记物是研究的热点之一。同时由于其广谱的激酶抑制活性,对该药多种适应症的研究也在广泛开展。鉴于regorafenib被批准时同时带框警告,其副作用也不容忽视。

Regorafenib （BAY 73-4506, Stivarga） is a new oral small molecule multi-kinases inhibitor. It can inhibit the target kinases associated with angiogenesis and tumorigenesis. The pathway influenced by regorafenib and the biomarkers for monitoring the efficacy of regorafenib become hot spots. Because of its wide spectrum kinase inhibitory activity, the utilization of regorafenib in many clinical indications are also carried out extensively. Since regorafenib is approved with the box warning, its side effects can not be ignored.