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Synonyms: ASP-2215 | ASP2215 | Xospata®
gilteritinib is an approved drug (FDA (2018), EMA (2019))
Compound class: Synthetic organic
Comment: Gilteritinib is an orally bioavailable inhibitor of the receptor tyrosine kinases (RTKs) FMS-related tyrosine kinase 3 (FLT3), AXL and anaplastic lymphoma kinase (ALK) , with clinical antineoplastic activity. Gilteritinib inhibits the activity of FLT3-activating mutations which are one of the most common genetic alterations in acute myeloid leukemia (AML).
SARS-CoV-2: AXL is a kinase upstream of p38 MAP kinases. p38 activity has been reported to be upregulated following SARS-CoV-2 infection of host cells in vitro, and gilteritinib produces an antiviral effect (IC50= 807 nM) .
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.✖
|The compound may be used as gilteritinib fumarate (PubChem CID 76970819).
In preclinical in vitro studies using leukemia cells expressing wild type (WT) or mutated FLT3, gilteritinib was a potent inhibitor of proliferation in all cell lines . For example, the IC50 vs. cells with WT FLT3 was 5 nM, and in FLT3-ITD mutant cells and cells with FLT3 point mutations it was <2 nM. The IC50 against cells with the F691L gatekeeper mutation was marginally higher at ~12 nM.
The IC50 values in the table below are estimates from the graph provided in Supplemental Figure 1 in the article that reports preclinical evaluation of gilteritinib activity, by Lee et al. (2017) . These values were determined using a DiscoverX® kinase selectivity screening assay.
|Selectivity at catalytic receptors|
|Key to terms and symbols||Click column headers to sort|