Passaro A, Prelaj A, Pochesci A, Spitaleri G, Rossi G, Del Signore E, Catania C, de Marinis F
Division of Thoracic Oncology, European Institute of Oncology (IEO), Milan, Italy.
Division of Thoracic Oncology, European Institute of Oncology (IEO), Milan, Italy and Department of Medical Oncology, Policlinico Umberto I, "Sapienza" University of Rome, Rome, Italy.
Drugs Today (Barc). 2017 Aug;53(8):435-446. doi: 10.1358/dot.2017.53.8.2676119.
Brigatinib (AP-26113, Alunbrig) is a second-generation anaplastic lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) that is highly active in non-small cell lung 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 metastatic NSCLC who have progressed on or are intolerant to crizotinib.
布加替尼（AP-26113，Alunbrig）是一种第二代间变性淋巴瘤激酶（ALK）酪氨酸激酶抑制剂（TKI），对携带ALK易位的非小细胞肺癌（NSCLC）具有高活性。布加替尼被发现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，特别是G1269A、ALK C1156Y、I1171S/T、V1180L等。不同的临床试验评估了布加替尼在克唑替尼耐药患者中的活性，证实其不仅在实质性疾病中，而且在颅内疾病中都具有高活性和持久反应。如今，布加替尼正在不同的临床试验中接受评估，探索在一线治疗中初治的患者。基于其显著的活性结果，布加替尼获得了美国食品药品监督管理局（FDA）的批准，用于治疗对克唑替尼进展或不耐受的ALK阳性转移性NSCLC患者。
