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.)
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, and differentiated thyroid carcinoma.
- Binimetinib or MEK162, had phase 1 trial for biliary tract cancer and melanoma
- PD-325901, for 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
- Wang, Ding; Boerner, Scott A.; Winkler, James D.; Lorusso, Patricia M. (2007). "Clinical experience of MEK inhibitors in cancer therapy". Biochim Biophys Acta 1773 (8): 1248–55. doi:10.1016/j.bbamcr.2006.11.009. PMID 17194493.
- "ASCO: MEK Inhibitors—Alone or Paired With a BRAF Inhibitor—Increase Options, Benefits for Patients With BRAF-Mutated Advanced Melanoma". 2012.
- KRAS/BRAF mutation status and ERK1/2 activation as biomarkers for MEK1/2 inhibitor therapy in colorectal cancer. 2009
- Jänne, Pasi A; Shaw, Alice T; Pereira, José Rodrigues; Jeannin, Gaëlle; Vansteenkiste, Johan; Barrios, Carlos; Franke, Fabio Andre; Grinsted, Lynda; Zazulina, Victoria; Smith, Paul; Smith, Ian; Crinò, Lucio (2013). "Selumetinib plus docetaxel for KRAS-mutant advanced non-small-cell lung cancer: A randomised, multicentre, placebo-controlled, phase 2 study". The Lancet Oncology 14 (1): 38–47. doi:10.1016/S1470-2045(12)70489-8. PMID 23200175.
- A phase I study of MEK inhibitor MEK162 (ARRY-438162) in patients with biliary tract cancer. 2012
- MEK Inhibitor PD-325901 To Treat Advanced Breast Cancer, Colon Cancer, And Melanoma
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