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April 12, 2013Journal of Hematology & Oncology293 citationsOpen Access

MEK and the inhibitors: from bench to bedside

AAAkintunde AkinleyeMFMuhammad FurqanNMNikhil Mukhi

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Abstract

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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Akinleye et al. (2013) studied this question.

synapsesocial.com/papers/6a2022d3f8c30f43cdfbee52https://doi.org/10.1186/1756-8722-6-27
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Also Consider

Synapse has enriched 5 closely related papers on similar clinical questions. Consider them for comparative context:

  1. 1Abstract B243: A phase I dose-escalation study of MEK inhibitor MEK162 (ARRY-438162) in patients with advanced solid tumors.2011 · 28 citations
  2. 2Abstract B128: A phase IB study of the MEK inhibitor GSK1120212 combined with everolimus in patients with solid tumors: Interim results.2011 · 8 citations
  3. 3RAS oncogenes: weaving a tumorigenic web2011 · 1,805 citations
  4. 4MEK1 mutations, but not ERK2 mutations, occur in melanomas and colon carcinomas, but none in thyroid carcinomas2009 · 73 citations
  5. 5Phase I Dose-Escalation Study of the Safety, Pharmacokinetics, and Pharmacodynamics of the MEK Inhibitor RO4987655 (CH4987655) in Patients with Advanced Solid Tumors2012 · 71 citations