quizartinib 🐶 Veterinary Use | 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: 6.58
  • 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

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01EX11 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
PROTEIN KINASE INHIBITORS
Other protein kinase inhibitors
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:62434 ALK inhibitor

Drug Use | Suggest Off label Use Form| |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




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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
TRAF2 and NCK-interacting protein kinase Kinase Kd 5.55 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
Platelet-derived growth factor receptor alpha Kinase Kd 8.80 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Kd 6.39 CHEMBL
High affinity nerve growth factor receptor Kinase Kd 5.64 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 5.24 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 5.68 CHEMBL
Ephrin type-A receptor 6 Kinase Kd 5.04 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
Ephrin type-A receptor 3 Kinase Kd 5.19 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
1132827-21-4 SECONDARY_CAS_RN
C2980091 UMLSCUI
CHEBI:90217 CHEBI
P30 PDB_CHEM_ID
CHEMBL576982 ChEMBL_ID
24889392 PUBCHEM_CID
DB12874 DRUGBANK_ID
CHEMBL2105709 ChEMBL_ID
D09956 KEGG_DRUG
9356 INN_ID
5658 IUPHAR_LIGAND_ID
C544967 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None