布加替尼用于ALK阳性转移性非小细胞肺癌：设计、研发及治疗地位
Brigatinib for -positive metastatic non-small-cell lung cancer: design, development and place in therapy.
作者信息
Ali Robert, Arshad Junaid, Palacio Sofia, Mudad Raja
机构信息
Department of Medicine, Division of Oncology, Jackson Memorial Hospital, University of Miami, Miller School of Medicine, Sylvester Comprehensive Cancer Centre, Miami, FL 33131, USA,
Department of Medicine, Division of Oncology, University of Miami, Miller School of Medicine, Sylvester Comprehensive Cancer Centre, Miami, FL 33136, USA,
出版信息
Drug Des Devel Ther. 2019 Feb 8;13:569-580. doi: 10.2147/DDDT.S147499. eCollection 2019.
Abstract
Despite the benefits of first and second generation anaplastic lymphoma kinase () inhibitors in the management of -rearranged advanced non-small-cell lung cancer (NSCLC), the development of acquired resistance poses an ongoing dilemma. Brigatinib has demonstrated a wider spectrum of preclinical activity against crizotinib-resistant mutant advanced NSCLC. The current review narrates a brief history of tyrosine kinases, the development and clinical background of brigatinib (including its pharmacology and molecular structure) and its use in -positive NSCLC.
摘要
尽管第一代和第二代间变性淋巴瘤激酶（ALK）抑制剂在治疗ALK重排的晚期非小细胞肺癌（NSCLC）方面具有诸多益处，但获得性耐药的出现仍构成了一个持续存在的难题。布加替尼已显示出针对克唑替尼耐药的ALK突变型晚期NSCLC具有更广泛的临床前活性。本综述简述了酪氨酸激酶的简史、布加替尼的研发及临床背景（包括其药理学和分子结构）及其在ALK阳性NSCLC中的应用。
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