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Synonyms: BAY-869766 | RDEA119
Compound class: Synthetic organic
Comment: Refametinib (BAY-869766) is a potent and selective, allosteric inhibitor of MEK1/2 with potential antineoplastic activity . This compound is available via AstraZeneca's openinnovation toolbox resource, which indicates that refametinib is associated with a risk of fetal toxicity.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
|No information available.
|Summary of Clinical Use
|Phase 1 clinical trial results have been published . Phase 2 clinical trials are underway for advanced or metastatic cancer, including RAS mutant hepatocellular carcinoma (HCC), assessing refametinib alone or in combination with either sorafenib or regorafenib, which are both approved multikinase inhibitors. View these refametinib clinical trial records at ClinicalTrials.gov.
|Mechanism Of Action and Pharmacodynamic Effects
|The MEK enzyme is highly selective for its target ERK. Inhibition of MEK therefore selectively inhibits activation of the ERK signalling pathway which drives cell proliferation.