MEK and the inhibitors: from bench to bedside

被引：221

作者：

Akinleye, Akintunde ^{[1
,2
]}

Furqan, Muhammad ^{[1
,2
]}

Mukhi, Nikhil ^{[1
,2
]}

Ravella, Pavan ^{[1
,2
]}

Liu, Delong ^{[1
,2
,3
,4
]}

机构：

[1] Westchester Cty Med Ctr, Dept Med, Valhalla, NY 10595 USA

[2] New York Med Coll, Valhalla, NY 10595 USA

[3] New York Med Coll, Div Hematol & Oncol, Valhalla, NY 10595 USA

[4] Westchester Cty Med Ctr, Valhalla, NY 10595 USA

来源：

JOURNAL OF HEMATOLOGY & ONCOLOGY | 2013年 / 6卷

关键词：

ACTIVATED PROTEIN-KINASE; PAPILLARY THYROID-CARCINOMA; SIGNAL-REGULATED KINASE-5; I DOSE-ESCALATION; CELL LUNG-CANCER; PHASE-II; OPEN-LABEL; TRANSCRIPTIONAL ACTIVATION; AZD6244; ARRY-142886; CURRENT MANAGEMENT;

D O I：

10.1186/1756-8722-6-27

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

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.

引用

页数：11

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