Crizotinib: A comprehensive review.
Crizotinib: A comprehensive review.
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DOI：
10.4103/2278-330x.110506
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发表时间：
2013-04
影响因子：
0.5
通讯作者：
Desai S
中科院分区：
文献类型：
--
作者：
Sahu A;Prabhash K;Noronha V;Joshi A;Desai S
间变性淋巴瘤激酶（ALK）基因重排存在于一小部分非小细胞肺癌中。ALK阳性赋予小分子ALK激酶抑制剂敏感性，如克唑替尼。将克里唑替尼纳入非小细胞肺癌的标准治疗实践将取决于对新诊断的非小细胞肺癌患者有效筛查系统的广泛实施，该系统具有足够的灵活性，可以随着治疗方法的发展而纳入新的靶点。克唑替尼在alk阳性肺癌中的I期和II期研究显示出显著的活性和令人印象深刻的临床益处，这使得其在2011年获得了美国fda的早期批准。虽然克唑替尼可引起缓解并延长患者的生命，但有报道称克唑替尼治疗出现耐药性。在这篇综述中，我们讨论了alk阳性肺癌患者的历史、作用机制、用途、不良反应、剂量调整以及未来的挑战和机遇。
Anaplastic lymphoma kinase (ALK) gene rearrangements are present in a small subset of non-small-cell lung cancers. ALK-positivity confers sensitivity to small-molecule ALK kinase inhibitors, such as crizotinib. The integration of crizotinib into standard treatment practice in NSCLC will rest on the widespread implementation of an effective screening system for newly diagnosed patients with NSCLC which is flexible enough to incorporate new targets as treatments are developed for them. Phase I and II studies of crizotinib in ALK-positive lung cancer have demonstrated significant activity and impressive clinical benefit, which led to its early approval by USFDA in 2011. Although crizotinib induces remissions and extends the lives of patients, there have been reports of emerging resistance to Crizotinib therapy. In this review, we discuss the history, mechanism of action, uses, adverse effects, dose modifications and future challenges and opportunities for patients with ALK-positive lung cancers.