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Synonyms: E-7050 | E7050
Compound class: Synthetic organic
Comment: Golvatinib is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity . It is the first kinase inhibitor with this dual action.
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 2 clinical trials assessing golvatinib in combination with other antineoplastics, for various types of solid tumours have been completed. Click here to link to ClinicalTrials.gov's full list of golvatinib (as E7050) trials.
|Mechanism Of Action and Pharmacodynamic Effects
|The HGF/c-Met signalling pathway contributes to tumour proliferation, survival, migration, and infiltration in various types of cancer. The VEGF-induced activation of VEGFR2 induces proliferation and migration in endothelial cells and promotes angiogenesis, a crucial mechanism required to support tumour growth. It is proposed that by inhibiting both the c-Met and VEGFR2 pathways concommitantly, golvatinib should have more effective antitumour activity than compounds that inhibit only a single pathway .