Lorlatinib，又称劳拉替尼，是可口服的ALK/ROS1抑制剂，作用于ROS1、ALK-WT以及ALK-L1196M的Ki值分别为<0.02 nM、<0.07 nM和0.7 nM，具有较强的血脑屏障透过能力，可诱导癌细胞凋亡，表现出显著的抗肿瘤活性，临床上用于治疗非小细胞肺癌。
参考文献
[1] Johnson TW, Richardson PF, Bailey S, et al. Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain exposure and broad-spectrum potency against ALK-resistant mutations. J Med Chem. 2014 Jun 12;57(11):4720-44. doi: 10.1021/jm500261q(IF:6.054).
[2] Zou HY, Li Q, Engstrom LD, et al. PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations. Proc Natl Acad Sci U S A. 2015 Mar 17;112(11):3493-8. doi: 10.1073/pnas.1420785112(IF:9.58).
-25~-15℃保存，有效期3年。
