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A MEK inhibitor is a chemical or drug that inhibits the mitogen ... approved by the FDA in June 2018 in combination with encorafenib for the treatment of ...
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 ...
Cobimetinib, sold under the brand name Cotellic, is an anti-cancer medication used to treat melanoma and histiocytic neoplasms. [2] [8] Cobimetinib is a MEK inhibitor. [2] ...
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Trametinib, sold under the brand name Mekinist among others, is an anticancer medication used for the treatment of melanoma [4] [5] and glioma. [6] [7] It is a MEK inhibitor drug with anti-cancer activity. [8]
Companies are not only focusing on improving the efficacy of BRAF inhibitors but also on reducing side effects and improving patient outcomes through combination regimens that include MEK inhibitors. The approval of combination therapies has set new standards in treatment, offering superior efficacy compared to BRAF inhibitor monotherapy.
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.
MEK inhibitors (trametinib, MEK162) are used in experiments, often in combination with BRAF inhibitors to treat melanoma; CDK inhibitors, e.g. PD-0332991, LEE011 in clinical trials; Hsp90 inhibitors, some in clinical trials; Hedgehog pathway inhibitors (e.g. FDA approved vismodegib and sonidegib).