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A MEK inhibitor is a chemical or drug that inhibits the mitogen-activated protein kinase enzymes MEK1 and/or MEK2. They can be used to affect the MAPK/ERK pathway which is often overactive in some cancers.
Pages in category "MEK inhibitors" The following 6 pages are in this category, out of 6 total. This list may not reflect recent changes. ...
Tyrosine kinase inhibitor (TKI) with selective activity against RET, VEGFR-2 and EGFR: Medullary thyroid cancer. Diarrhoea, hypertension, QT interval prolongation, depression, electrolyte anomalies, hypothyroidism and GI perforation (uncommon). 2.3 mTOR inhibitors: Everolimus: PO: mTOR inhibitor.
The first drug licensed to act on this pathway is sorafenib — a Raf kinase inhibitor. Other Raf inhibitors include SB590885, PLX4720, XL281, RAF265, encorafenib, dabrafenib, and vemurafenib. [18] Some MEK inhibitors include cobimetinib, CI-1040, PD0325901, binimetinib (MEK162), selumetinib, [18] and trametinib (GSK1120212) [20]
Binimetinib is a selective inhibitor of MEK, a central kinase in the tumor-promoting MAPK pathway. [5] Inappropriate activation of the pathway has been shown to occur in many cancers. [ 5 ] In June 2018 it was approved by the FDA in combination with encorafenib for the treatment of patients with unresectable or metastatic BRAF V600E or V600K ...
Mitogen-activated protein kinase kinase (also known as MAP2K, MEK, MAPKK) is a dual-specificity kinase enzyme which phosphorylates mitogen-activated protein kinase (MAPK). MAP2K is classified as EC 2.7.12.2 .
It is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. [10] [11] U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC 50 of 72 nM for MEK1 and 58 nM for MEK2.
Selumetinib is a kinase inhibitor, more specifically a selective inhibitor of the enzyme mitogen-activated protein kinase kinase (MAPK kinase or MEK) subtypes 1 and 2. These enzymes are part of the MAPK/ERK pathway, which regulates cell proliferation (i.e., growth and division) and is overly active in many types of cancer. [18]
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