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Synonyms: CGP 41231 | CGP 41251 | N-benzoylstaurosporine | PKC412 | Rydapt®
midostaurin is an approved drug (FDA & EMA (2017))
Compound class: Synthetic organic
Comment: Midostaurin is an analogue of staurosporine, and was originally described as a PKC inhibitor . It was later reported as an inhibitor of fms-related tyrosine kinase 3 (FLT3) .
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 midostaurin accelerated approval in April 2017, and the EMA followed in September of the same year. These authorisations are for the treatment of adult patients with newly diagnosed acute myeloid leukemia (AML) who are FLT3 mutation-positive (as detected by an FDA-approved test) to be used in combination with standard cytarabine and daunorubicin induction and cytarabine consolidation. It was also approved for mastocytosis . The EMA had previously granted midostaurin orphan drug designation for the treatment of AML and mastocytosis (effective via inhibition of KIT receptors on mast cells, which are involved in stimulating proliferation of mast cells in mastocytosis).
Click here to link to ClinicalTrials.gov's list of Phase 2 midostaurin trials.
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)