Mobocertinib是一种靶向EGFR的口服激酶抑制剂,用于治疗非小细胞肺癌

Mayur S. Jain, Shashikant D. Barhate, Rahul D. Shimpi
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引用次数: 0

摘要

Mobocertinib是一种靶向人表皮生长因子受体(EGFR)的激酶抑制剂。它特别用于治疗由EGFR基因外显子20突变引起的非小细胞肺癌(NSCLC),这通常与较差的预后有关(与导致NSCLC的“经典”EGFR突变相比),并与标准靶向EGFR抑制剂的抗性有关。Mobocertinib似乎是治疗这种治疗耐药的非小细胞肺癌的有效手段,对EGFR外显子20插入突变体变体发挥抑制作用,浓度比抑制野生型EGFR所需的浓度低1.5- 10倍。于2021年9月获得FDA的加速协议,用于治疗EGFR外显子20插入突变且先前治疗失败的局部晚期或转移性NSCLC患者
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Mobocertinib is an Oral kinase inhibitor targeted against EGFR and used in the treatment of Non-small cell Lung cancer: A Review
Mobocertinib is a kinase inhibitor targeted against human epidermal growth factor receptor (EGFR). It is used particularly in the action of non-small cell lung cancer (NSCLC) caused by exon 20 placing mutations in the EGFR gene, which are classically linked through a poorer prognosis (as compared to "classical" EGFR mutants causing NSCLC) and are linked with opposition to standard targeted EGFR inhibitors. Mobocertinib appears to be an effective means of treating this otherwise treatment-resistant NSCLC, exerting an inhibitory effect on EGFR exon 20 insertion mutant variants at concentrations 1.5- to 10-fold lower than those required to inhibit wild-type EGFR.2 Mobocertinib, below the brand name Exkivity (Takeda Pharmaceuticals Inc.), was granted accelerated agreement by the FDA in September 2021 for the action of locally advanced or metastatic NSCLC in patients with EGFR exon 20 insertion mutations who have failed previous therapies.1
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