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Brigatinib for the treatment of ALK-positive advanced non-small cell lung cancer patients

机译:Brigatinib用于治疗ALK阳性晚期非小细胞肺癌患者

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摘要

Brigatinib (AP-26113, Alunbrig) is a second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase hibitor (TKI) that is highly active in non-small cell mg cancer(NSCLC) harboring ALK translocation. Brigatinib was found to be very active against different ALK resistance mutations that mediate acquired resistance biology processes, particularly G1269A ALK C1156Y, I1171S/T, V1180L and others. Different clinical trials evaluated the activity of brigatinib in crizotinib-resistant patients, confirming high activity with durable response not only in parenchymal disease, but also in intracranial disease. Nowadays, brigatinib is under evaluation in different clinical trials exploring TKI-naive patients in the first-line setting. On the basis of its significant activity results, brigatinib received approval by the FDA for the treatment of patients with ALK-positive metostotic NSCLC who have progressed on or are intolerant to crizotinib.
机译:Brigatinib(AP-26113,Alunbrig)是第二代间变性淋巴瘤激酶(ALK)酪氨酸激酶抑制剂(TKI),在含有ALK易位的非小细胞mg癌(NSCLC)中高度活跃。研究发现,Brigatinib对介导获得性耐药生物学过程的不同ALK耐药突变非常有效,尤其是G1269A ALK C1156Y、I1171S/T、V1180L等。不同的临床试验评估了环唑替尼耐药患者的布里加替尼活性,证实不仅在实质性疾病中,而且在颅内疾病中,布里加替尼活性高,反应持久。如今,brigatinib正在不同的临床试验中接受评估,这些试验在一线环境中探索TKI未经治疗的患者。基于其显著的活性结果,brigatinib获得了FDA的批准,用于治疗ALK阳性胃食管非小细胞肺癌患者,这些患者对克唑替尼有进展或不耐受。

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