MEK and the inhibitors: from bench to bedside

被引:0
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作者
Akintunde Akinleye
Muhammad Furqan
Nikhil Mukhi
Pavan Ravella
Delong Liu
机构
[1] Westchester Medical Center and New York Medical College,Department of Medicine
[2] New York Medical College and Westchester Medical Center,Division of Hematology and Oncology
关键词
Melanoma; Docetaxel; Papillary Thyroid Cancer; Malignant Mesothelioma; Vemurafenib;
D O I
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学科分类号
摘要
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.
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