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A MEK inhibitor is a chemical or drug that inhibits the mitogen-activated protein kinase kinase enzymes MEK1 and/or MEK2. They can be used to affect the MAPK/ERK pathway which is often overactive in some cancers. (See MAPK/ERK pathway#Clinical significance.) Hence MEK inhibitors have potential for treatment of some cancers, especially BRAF-mutated melanoma,〔(【引用サイトリンク】title=ASCO: MEK Inhibitors—Alone or Paired With a BRAF Inhibitor—Increase Options, Benefits for Patients With BRAF-Mutated Advanced Melanoma )〕 and KRAS/BRAF mutated colorectal cancer.〔(KRAS/BRAF mutation status and ERK1/2 activation as biomarkers for MEK1/2 inhibitor therapy in colorectal cancer. 2009 )〕 Some MEK inhibitors: * Trametinib (GSK1120212), FDA-approved to treat BRAF-mutated melanoma. Also studied in combination with BRAF inhibitor dabrafenib to treat BRAF-mutated melanoma. * Selumetinib, had a phase 2 clinical trial for non-small cell lung cancer (NSCLC) which demonstrated an improvement in PFS, and is now in phase III development in KRAS mutation positive NSCLC (SELECT-1,NCT01933932). Other clinical trials underway include uveal melanoma, differentiated thyroid carcinoma, and inoperable plexiforms associated with neurofibromatosis type 1 * Binimetinib (MEK162), had phase 1 trial for biliary tract cancer and melanoma〔(A phase I study of MEK inhibitor MEK162 (ARRY-438162) in patients with biliary tract cancer. 2012 )〕 and in Sept 2014 reported encouraging results from a phase II clinical trial for NRAS melanoma.〔(Phase 2 Trial Of Binimetinib In NRAS Melanoma Shows Promising Clinical Activity. Sept 2014 )〕 * PD-325901, for breast cancer, colon cancer, and melanoma〔(MEK Inhibitor PD-325901 To Treat Advanced Breast Cancer, Colon Cancer, And Melanoma )〕 * Cobimetinib or XL518, in a Phase III trial, in combination with vemurafenib (Zelboraf(R)), for treatment of advanced melanoma * CI-1040, PD035901 ==References== 抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』 ■ウィキペディアで「MEK inhibitor」の詳細全文を読む スポンサード リンク
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