Department of Medicine, Westchester Medical Center and New York Medical College, Valhalla, NY 10595, USA.
J Hematol Oncol. 2013 Apr 12;6:27. doi: 10.1186/1756-8722-6-27.
Four distinct MAP kinase signaling pathways involving 7 MEK enzymes have been identified. MEK1 and MEK2 are the prototype members of MEK family proteins. Several MEK inhibitors are in clinical trials. Trametinib is being evaluated by FDA for the treatment of metastatic melanoma with BRAF V600 mutation. Selumetinib has been studied in combination with docetaxel in phase II randomized trial in previously treated patients with advanced lung cancer. Selumetinib group had better response rate and progression-free survival. This review also summarized new MEK inhibitors in clinical development, including pimasertib, refametinib, PD-0325901, TAK733, MEK162 (ARRY 438162), RO5126766, WX-554, RO4987655 (CH4987655), GDC-0973 (XL518), and AZD8330.
已经确定了涉及 7 种 MEK 酶的四种不同的 MAP 激酶信号通路。MEK1 和 MEK2 是 MEK 家族蛋白的原型成员。有几种 MEK 抑制剂正在临床试验中。Trametinib 正在接受 FDA 的评估，用于治疗携带 BRAF V600 突变的转移性黑色素瘤。Selumetinib 已在 II 期随机试验中与多西他赛联合用于先前治疗的晚期肺癌患者。Selumetinib 组的反应率和无进展生存期更好。这篇综述还总结了处于临床开发阶段的新型 MEK 抑制剂，包括 pimasertib、refametinib、PD-0325901、TAK733、MEK162（ARRY 438162）、RO5126766、WX-554、RO4987655（CH4987655）、GDC-0973（XL518）和 AZD8330。
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