Division of Hematology, Oncology University of California San Diego Moores Cancer Center, San Diego, California, USA.
Division of Pharmacy, University of California San Diego, San Diego, California, USA.
Expert Opin Pharmacother. 2021 Oct;22(14):1815-1824. doi: 10.1080/14656566.2021.1948014. Epub 2021 Jul 26.
: Alectinib is a second-generation inhibitor of anaplastic lymphoma kinase (ALK) and RET. Phase III clinical trials have established its superiority to crizotinib in the first-line ALK inhibitor-naïve setting. Studies also support its use over chemotherapy in the post-crizotinib setting. It is currently one of several FDA- and EMA-approved ALK inhibitors, and it is listed as a preferred initial therapy for treatment-naïve ALK-positive non-small cell lung cancer (NSCLC).: Herein, the authors provide the reader with details of the chemical structure, pharmacologic properties, resistance mutations, phase I, II, and III clinical trials, and safety profile of alectinib. Furthermore, the authors provide the reader with the expert opinion and future perspectives on the drug.: Alectinib compares favorably to other second-generation ALK inhibitors with regards to safety, tolerability, and efficacy. Based on currently available data, it is an appropriate first-line option. Ongoing studies will better resolve the ideal sequencing of ALK inhibitors in the treatment of ALK-positive NSCLC.
阿来替尼是一种第二代间变性淋巴瘤激酶(ALK)和 RET 的抑制剂。III 期临床试验已经证实,它在一线 ALK 抑制剂初治患者中优于克唑替尼。研究还支持在克唑替尼治疗后使用它代替化疗。它目前是几种 FDA 和 EMA 批准的 ALK 抑制剂之一,并且被列为治疗初治 ALK 阳性非小细胞肺癌(NSCLC)的首选初始治疗药物。本文作者为读者提供了阿来替尼的化学结构、药理特性、耐药突变、I、II 和 III 期临床试验以及安全性概况的详细信息。此外,作者还就该药物的专家意见和未来前景为读者提供了信息。与其他第二代 ALK 抑制剂相比,阿来替尼在安全性、耐受性和疗效方面具有优势。基于目前可用的数据,它是一种合适的一线选择。正在进行的研究将更好地解决 ALK 阳性 NSCLC 中 ALK 抑制剂的理想治疗顺序。