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吉非替尼作为表皮生长因子受体络氨酸激酶抑制剂(EGFR-TKI)类靶向药物,广泛用于临床非小细胞肺癌(NSCLC)的治疗,但近几年的临床应用发现,肿瘤细胞对该类药物的敏感度逐渐下降,药物作用疗效呈现减低趋势,临床耐药问题逐渐凸显。近几年的深入研究表明,吉非替尼的耐药机制可能与表皮生长因子受体(EGFR)旁路效应、EGFR信号传导路径和EGFR靶基因的二次突变有关,基于此以吉非替尼作用机制为出发点对其获得性耐药机制进行归纳总结。
Gefitinib is widely used as a targeted drug for epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) in the treatment of clinical non-small cell lung cancer (NSCLC). However, in recent years, it has been found that tumors The sensitivity of cells to such drugs gradually decreased, the efficacy of drugs showed a downward trend, clinical drug resistance problems gradually highlighted. In recent years, in-depth studies have shown that the mechanism of resistance to gefitinib may be related to the EGFR bypass effect, EGFR signaling pathway and EGFR target gene secondary mutations related to gefitinib Nigeria mechanism of action as a starting point for its access to resistance mechanisms summarized.