Crizotinib。
文章的细节
-
引用
复制到剪贴板 -
Heigener DF, Reck M
Crizotinib。
癌症res 2018;211:57-65。doi: 10.1007 / 978 - 3 - 319 - 91442 - 8 - _4。
- PubMed ID
-
30069759 (PubMed视图］
- 摘要
-
克唑替尼是一种atp竞争性受体酪氨酸激酶(RTK) C-Met, ALK和ROS1的小分子抑制剂。在eml4 - alk重排导致ALK-RTK的体质激活的非小细胞肺癌(NSCLC)中具有强大的有效性。该药物被批准用于该实体，占所有NSCLC的不超过3-5%。然而，在这个人群中，产生了令人印象深刻的应答率。ROS-1重排也是如此;然而，这些仅发生在约1%的NSCLC中。在小系列研究中，也报道了在肿瘤中含有MET外显子4跳跃突变(约。占所有NSCLC的3%)。毒性包括视力损害、恶心、外周水肿、qt延长和肝酶升高。此外，肾囊肿的发生也有报道。 The detection of ALK-protein by immunohistochemistry is a predictor of efficacy for crizotinib. In cases of doubt, fluorescence in situ hybridisation (FISH) detecting the ALK-rearrangement has to be performed on tumour tissue. FISH is also the method of choice to detect ROS1-rearrangement, whereas MET-mutations are detected by sequencing methods. The high efficacy of crizotinib in ALK- and ROS-rearranged as well as MET mutated lung cancer as new molecular targets beside the epidermal growth factor receptor (EGFR) underscores the importance of molecular typing in NSCLC.
引用本文的药物库数据
- 药物