gilteritinib Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5306 1254053-43-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • gilteritinib fumarate
  • gilteritinib
  • xospata
  • ASP2215
Gilteritinib is a small molecule that inhibits multiple receptor tyrosine kinases, including FMS-like tyrosine kinase 3 (FLT3). Gilteritinib demonstrated the ability to inhibit FLT3 receptor signaling and proliferation in cells exogenously expressing FLT3 including FLT3-ITD, tyrosine kinase domain mutations (TKD) FLT3-D835Y and FLT3-ITD-D835Y, and it induced apoptosis in leukemic cells expressing FLT3-ITD.
  • Molecular weight: 552.72
  • Formula: C29H44N8O3
  • CLOGP: 2.12
  • LIPINSKI: 2
  • HAC: 11
  • HDO: 3
  • TPSA: 121.11
  • ALOGS: -4.39
  • ROTB: 9

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 21, 2018 PMDA Astellas Pharma Inc
Nov. 28, 2018 FDA ASTELLAS
Oct. 24, 2019 EMA ASTELLAS PHARMA EUROPE BV

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 243.27 43.85 97 1429 94530 46590006
Acute myeloid leukaemia 189.29 43.85 52 1474 15726 46668810
Hepatic function abnormal 141.62 43.85 50 1476 34371 46650165
Myelosuppression 109.17 43.85 29 1497 7674 46676862
Platelet count decreased 104.41 43.85 55 1471 99969 46584567
Cytopenia 94.82 43.85 26 1500 7742 46676794
Neutrophil count decreased 85.48 43.85 37 1489 43389 46641147
Differentiation syndrome 84.70 43.85 16 1510 895 46683641
Acute myeloid leukaemia recurrent 54.96 43.85 12 1514 1384 46683152
Acute febrile neutrophilic dermatosis 52.12 43.85 13 1513 2672 46681864
Blast cell count increased 44.19 43.85 8 1518 353 46684183

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Acute myeloid leukaemia 208.36 41.88 62 1303 17944 29933169
Febrile neutropenia 180.23 41.88 90 1275 106603 29844510
Myelosuppression 176.76 41.88 45 1320 7277 29943836
Hepatic function abnormal 115.98 41.88 50 1315 41895 29909218
Platelet count decreased 91.98 41.88 58 1307 106071 29845042
Differentiation syndrome 58.68 41.88 13 1352 1147 29949966

Pharmacologic Action:

SourceCodeDescription
ATC L01EX13 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
CHEBI has role CHEBI:35610 cytostatic
CHEBI has role CHEBI:62434 alk inhibitor
CHEBI has role CHEBI:68495 type i programmed cell-death inducer

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Acute myeloid leukemia, disease indication 91861009

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 11.78 acidic
pKa2 8.76 Basic
pKa3 5.0 Basic
pKa4 4.38 Basic
pKa5 3.81 Basic
pKa6 0.35 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 40MG BASE XOSPATA ASTELLAS N211349 Nov. 28, 2018 RX TABLET ORAL Nov. 28, 2023 NEW CHEMICAL ENTITY
EQ 40MG BASE XOSPATA ASTELLAS N211349 Nov. 28, 2018 RX TABLET ORAL Nov. 28, 2025 INDICATED FOR THE TREATMENT OF ADULT PATIENTS WHO HAVE RELAPSED OR REFRACTORY ACUTE MYELOID LEUKEMIA (AML) WITH A FMS-LIKE TYROSINE KINULLSE 3 (FLT3) MUTATION AS DETECTED BY AN FDA-APPROVED TEST

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR IC50 8.30 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
1254053-84-3 SECONDARY_CAS_RN
4038030 VANDF
C3896738 UMLSCUI
CHEBI:145372 CHEBI
C6F PDB_CHEM_ID
CHEMBL3301622 ChEMBL_ID
CHEMBL3301603 ChEMBL_ID
DB12141 DRUGBANK_ID
D10709 KEGG_DRUG
49803313 PUBCHEM_CID
C000609080 MESH_SUPPLEMENTAL_RECORD_UI
8708 IUPHAR_LIGAND_ID
10048 INN_ID
66D92MGC8M UNII
2105806 RXNORM
299484 MMSL
35657 MMSL
35755 MMSL
d09076 MMSL
017854 NDDF
017855 NDDF
782974005 SNOMEDCT_US
782987004 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Xospata HUMAN PRESCRIPTION DRUG LABEL 1 0469-1425 TABLET 40 mg ORAL NDA 29 sections