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

Stem definitionDrug idCAS RN
tyrosine kinase inhibitors 5341 950769-58-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • quizartinib
  • quizartinib hydrochloride
  • quizartinib dihydrochloride
  • vanflyta
  • AC220
  • AC010220
Quizartinib is the most selective type II FLT3 inhibitor and has shown the strongest single-agent activity in patient population with R/R-AML (acute myeloid leukemia) with FLT3 mutations. The FLT3 tyrosine kinase inhibitors act as direct inhibitors of FLT3 via competitive inhibition of ATP-binding sites in the FLT3 receptor. Type II FLT3 inhibitors bind the FLT3 receptor in the inactive conformation in a region adjacent to the ATP-binding domain. As a result of this binding affinity, these inhibitors prevent activity of ITD (the internal tandem duplication) mutations but do not target TKD (the tyrosine kinase domain) mutations
  • Molecular weight: 560.67
  • Formula: C29H32N6O4S
  • CLOGP: 6.63
  • LIPINSKI: 2
  • HAC: 10
  • HDO: 2
  • TPSA: 106.16
  • ALOGS: -4.04
  • ROTB: 8

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
June 18, 2019 PMDA DAIICHI SANKYO COMPANY, LIMITED

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX11 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

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Acute myeloid leukemia, disease indication 91861009
Acute myeloid leukemia with FMS-like tyrosine kinase-3 mutation indication 734522002

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.71 acidic
pKa2 13.3 acidic
pKa3 6.79 Basic
pKa4 1.89 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR Kd 8.80 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Tyrosine-protein kinase Lyn Kinase Kd 5.24 CHEMBL
Platelet-derived growth factor receptor alpha Kinase Kd 8.80 CHEMBL
Platelet-derived growth factor receptor beta Kinase Kd 8.80 CHEMBL
Tyrosine-protein kinase ABL1 Kinase Kd 6.50 CHEMBL
Mast/stem cell growth factor receptor Kit Kinase Kd 8.80 CHEMBL
Tyrosine-protein kinase Lck Kinase Kd 5.60 CHEMBL
Proto-oncogene tyrosine-protein kinase receptor Ret Kinase Kd 8.80 CHEMBL
Vascular endothelial growth factor receptor 1 Kinase Kd 7.39 CHEMBL
Vascular endothelial growth factor receptor 2 Kinase Kd 7.06 CHEMBL
Vascular endothelial growth factor receptor 3 Kinase Kd 7.39 CHEMBL
Macrophage colony-stimulating factor 1 receptor Kinase Kd 8.80 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Kd 6.39 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 5.68 CHEMBL
Ephrin type-A receptor 6 Kinase Kd 5.04 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 5.55 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 5.19 CHEMBL
Tyrosine-protein kinase FRK Kinase Kd 5.75 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 5 Kinase Kd 6.36 CHEMBL
Receptor-interacting serine/threonine-protein kinase 2 Kinase Kd 5.57 CHEMBL
High affinity nerve growth factor receptor Kinase Kd 5.64 CHEMBL
STE20-like serine/threonine-protein kinase Kinase Kd 5.34 CHEMBL
MAP kinase-interacting serine/threonine-protein kinase 2 Kinase Kd 5.58 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 7.09 CHEMBL
BDNF/NT-3 growth factors receptor Kinase Kd 6.21 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 5.50 CHEMBL
NT-3 growth factor receptor Kinase Kd 6.26 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 6.16 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4 Kinase Kd 5.60 CHEMBL
Muscle, skeletal receptor tyrosine-protein kinase Kinase Kd 6 CHEMBL
Mitogen-activated protein kinase 15 Kinase Kd 6.57 CHEMBL
Receptor-interacting serine/threonine-protein kinase 1 Kinase Kd 6.05 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 5.92 CHEMBL
Homeodomain-interacting protein kinase 4 Kinase Kd 6.50 CHEMBL
Mitogen-activated protein kinase kinase kinase 7 Kinase Kd 5.07 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 5.70 CHEMBL
Bone morphogenetic protein receptor type-1B Kinase Kd 5.64 CHEMBL
Myosin light chain kinase 3 Kinase Kd 6.39 CHEMBL
Myosin-10 Enzyme Kd 6.12 CHEMBL
Ephrin type-A receptor 7 Kinase Kd 5.43 CHEMBL

External reference:

IDSource
7LA4O6Q0D3 UNII
C2980091 UMLSCUI
CHEBI:90217 CHEBI
P30 PDB_CHEM_ID
CHEMBL576982 ChEMBL_ID
24889392 PUBCHEM_CID
DB12874 DRUGBANK_ID
CHEMBL2105709 ChEMBL_ID
D09956 KEGG_DRUG
C544967 MESH_SUPPLEMENTAL_RECORD_UI
5658 IUPHAR_LIGAND_ID
9356 INN_ID

Pharmaceutical products:

None