第3代EGFR抑制剂Osimertinib Mesylate

Osimertinib Mesylate: the Third Generation EGFR Inhibitor

Osimertinibmesylate为阿斯利康公司研发的第3代EGFR抑制剂,不可逆地抑制EGFR-T790M,2015年11月13日获美国食品药品监督管理局(FDA)批准用于非小细胞肺癌治疗。介绍osimertinibmesylate的化学合成、临床前药理学研究、临床研究及专利保护情况等,为抗肿瘤药物研发提供参考。

In Nov. 13 2015, osimertinib mesylate was approved by the U.S. Food and Drug Administration（FDA） for the treatment of non-small cell lung cancer. Osimertinib mesylate was developed by Astra Zeneca as the 3rd generation EGFR tyrosine kinase inhibitors（TKIs） that irreversibly inhibited EGFR-T790 M. In this article, the chemical synthesis, preclinical pharmacology, clinical trials and patent protection of osimertinib mesylate were reviewed, so as to provide references for the RD of new anti-tumor drugs.