PharmaKB logo
Company Reports
Company Reports
Drug Reports
Drug Reports
Disease Reports
Disease Reports
Sets
Sets
Favorites
Favorites
Log in
Log in
AboutPricing
Drug ReportsGilteritinib
Xospata(gilteritinib)
Xospata (gilteritinib) is a small molecule pharmaceutical. Gilteritinib was first approved as Xospata on 2018-11-28. It is used to treat myeloid leukemia acute in the USA. It has been approved in Europe to treat myeloid leukemia acute. It is known to target tyrosine-protein kinase receptor UFO, high affinity nerve growth factor receptor, proto-oncogene tyrosine-protein kinase receptor Ret, tyrosine-protein kinase Mer, leukocyte tyrosine kinase receptor, proto-oncogene tyrosine-protein kinase ROS, receptor-type tyrosine-protein kinase FLT3, and ALK tyrosine kinase receptor.
Download report
Favorite
Events Timeline
Commercial
Clinical
Drug
Target
Variants
Financial
Trends
Safety
Events Timeline
5D
1M
3M
6M
YTD
1Y
2Y
5Y
Max
Events
FDA approval date
EMA approval date
Patent expiration date
Study first post date
Last update post date
Start date
Primary completion date
Completion date
Results first post date
Plot placeholder
Mock data
Subscribe for the real data
Commercial
Therapeutic Areas
Therapeutic Area
MeSH
neoplasmsD009369
hemic and lymphatic diseasesD006425
Trade Name
FDA
EMA
Xospata
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Gilteritinib fumarate
Tradename
Company
Number
Date
Products
XOSPATAAstellas PharmaN-211349 RX2018-11-28
1 products, RLD, RS
Labels
FDA
EMA
Brand Name
Status
Last Update
xospataNew Drug Application2022-04-29
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
myeloid leukemia acute—D015470C92.0
Agency Specific
FDA
EMA
Expiration
Code
GILTERITINIB FUMARATE, XOSPATA, ASTELLAS
2025-11-28ODE-222
Patent Expiration
Patent
Expires
Flag
FDA Information
Gilteritinib Fumarate, Xospata, Astellas
107865002036-07-01DP
89693362031-01-27DS, DP
94874912030-07-28U-2456
ATC Codes
L: Antineoplastic and immunomodulating agents
— L01: Antineoplastic agents
— L01E: Protein kinase inhibitors, antineoplastic and immunomodulating agents
— L01EX: Other protein kinase inhibitors in atc
— L01EX13: Gilteritinib
HCPCS
No data
Clinical
Clinical Trials
72 clinical trials
View more details
Plot placeholder
Mock data
Subscribe for the real data
Indications Phases 4
No data
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Myeloid leukemia acuteD015470—C92.01185—321
Myeloid leukemiaD007951—C92852—314
LeukemiaD007938—C95742—313
Myelodysplastic syndromesD009190—D46——1——1
PreleukemiaD011289————1——1
Refractory anemia with excess of blastsD000754—D46.2——1——1
SyndromeD013577————1——1
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
NeoplasmsD009369—C8032———3
Non-small-cell lung carcinomaD002289——21———2
Lung neoplasmsD008175—C34.9011———1
RecurrenceD012008———1———1
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Healthy volunteers/patients———2————2
Renal insufficiencyD051437—N191————1
Liver diseasesD008107EFO_0001421K70-K771————1
Hepatic insufficiencyD048550——1————1
PharmacokineticsD010599——1————1
Indications Without Phase
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Residual neoplasmD018365——————22
Pathologic complete responseD000095384——————22
Epidemiology
Epidemiological information for investigational and approved indications
View more details
Drug
General
Drug common nameGilteritinib
INNgilteritinib
Description
Gilteritinib is a member of the class of pyrazines that is pyrazine-2-carboxamide which is substituted by {3-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl}nitrilo, (oxan-4-yl)nitrilo and ethyl groups at positions 3,5 and 6, respectively. It is a potent inhibitor of FLT3 and AXL tyrosine kinase receptors (IC50 = 0.29 nM and 0.73 nM, respectively). Approved by the FDA for the treatment of acute myeloid leukemia in patients who have a FLT3 gene mutation. It has a role as an apoptosis inducer, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor and an antineoplastic agent. It is a N-methylpiperazine, a member of piperidines, a secondary amino compound, a monomethoxybenzene, a member of pyrazines, a primary carboxamide, an aromatic amine and a member of oxanes.
Classification
Small molecule
Drug classtyrosine kinase inhibitors
Image (chem structure or protein)Loading
Structure (InChI/SMILES or Protein Sequence)
CCc1nc(C(N)=O)c(Nc2ccc(N3CCC(N4CCN(C)CC4)CC3)c(OC)c2)nc1NC1CCOCC1
Identifiers
PDB—
CAS-ID1254053-43-4
RxCUI—
ChEMBL IDCHEMBL3301622
ChEBI ID—
PubChem CID49803313
DrugBankDB12141
UNII ID66D92MGC8M (ChemIDplus, GSRS)
Target
Agency Approved
No data
Alternate
RET
RET
Organism
Homo sapiens
Gene name
RET
Gene synonyms
CDHF12, CDHR16, PTC, RET51
NCBI Gene ID
5979
Protein name
proto-oncogene tyrosine-protein kinase receptor Ret
Protein synonyms
Cadherin family member 12, cadherin-related family member 16, Proto-oncogene c-Ret, rearranged during transfection, ret proto-oncogene (multiple endocrine neoplasia and medullary thyroid carcinoma 1, Hirschsprung disease), RET receptor tyrosine kinase
Uniprot ID
Q9BTB0
Mouse ortholog
Ret (19713)
proto-oncogene tyrosine-protein kinase receptor Ret (P35546)
Variants
No data
Financial
No data
Trends
PubMed Central
Top Terms for Disease or Syndrome:
Plot placeholder
Mock data
Subscribe for the real data
Additional graphs summarizing 2,432 documents
View more details
Safety
Black-box Warning
Black-box warning for: Xospata
Adverse Events
Top Adverse Reactions
Plot placeholder
Mock data
Subscribe for the real data
3,768 adverse events reported
View more details
© 2020-2025 Collaborative Drug Discovery Inc. (CDD) | Terms of Use