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首页> 外文期刊>Bulletin of the Korean Chemical Society >Allosteric Inhibitor TREA-0236 Containing Non-hydrolysable Quinazoline-4-one for EGFR T790M/C797S Mutants Inhibition
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Allosteric Inhibitor TREA-0236 Containing Non-hydrolysable Quinazoline-4-one for EGFR T790M/C797S Mutants Inhibition

机译：含有非水解喹唑啉-4-ON的变构抑制剂TREA-0236用于EGFR T790M / C797S突变体抑制作用

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Non-small cell lung cancer (NSCLC) is one of the leading causes of cancer-related death globally. Epidermal growth factor receptor (EGFR) activating mutations such as EGFR L858R and EGFR ex19 deletions are responsible for 30-40% of NSCLC patients in East Asian populations and 10-15% in European descendants. All the approved EGFR-tyrosine kinase inhibitors (TKIs) give clinical benefits to EGFR-related NSCLC patients in terms of overall survival and quality of patient life. However so far approved EGFR-TKIs are ATP catalytic site inhibitors and their benefit is ultimately limited due to mutational resistance near the catalytic site. In a recent osimertinib and olmutinib clinical study, newly acquired resistance ‘EGFR C797S mutation’ has been reported. Since second and third generation EGFR-TKIs are featured as irreversible inhibitors to the EGFR C797, there are no more effective treatment options to the EGFR C797S mutation. Therefore there is an urgent unmet medical need for next generation EGFR-TKIs via non-irreversible inhibition to EGFR T790M/C797S mutations.
机译：非小细胞肺癌（NSCLC）是全球癌症相关死亡的主要原因之一。表皮生长因子受体（EGFR）激活突变，例如EGFR L858R和EGFR EX19缺失是对东亚人群的30-40％的NSCLC患者，欧洲后代10-15％。所有批准的EGFR-酪氨酸激酶抑制剂（TKIS）在整体存活和患者生活质量方面为EGFR相关的NSCLC患者提供临床益处。然而，到目前为止，批准的EGFR-TKI是ATP催化位点抑制剂，其益处最终受限于催化位点附近的突变性。在最近的口服尼和奥米替尼临床研究中，据报道了新获得的阻力“EGFR C797S突变”。由于二次和第三代EGFR-TKIS作为EGFR C797的不可逆转抑制剂，因此对EGFR C797S突变没有更有效的治疗方法。因此，通过对EGFR T790M / C797S突变的非不可逆转抑制，对下一代EGFR-TKI具有紧急的未满足医疗需求。

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