- Advanced search
- Immuno Portal
- Malaria Portal
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.✖
|No information available.|
|Summary of Clinical Use|
|The FDA granted Fast Track/Priority Review designation for the New Drug Application (NDA) that was submitted by the drug's developer Astellas in June 2018. This led to full approval in November 2018, for the use of gilteritinib (Xospata®) as a therapy for patients with relapsed/refractory acute myeloid leukemia (AML) with a confirmed FLT3 mutation. Phase 1/2 clinical trial results were published by Perl et al. in 2017 . The EMA had granted gilteritinib orphan drug designation as a treatment for AML in January 2018 . In September 2019, following accelerated assessment, the EMA Committee for Medicinal Products for Human Use (CHMP) reported that they were minded to grant marketing authorisation for the same patient group as indicated by the FDA approval , and full approval was granted in October 2019.|