quizartinib 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,ACVRL1,AKT2,AKT3,ALK,AURKA,AURKB,AURKC,AXL,BLK,BRAF,CAMK2B,CAMK2D,CDK1,CDK19,CDK5,CDK9,CHEK1,CSF1R,DDR1,DYRK1B,EGFR,EIF2AK3,EPHA2,EPHB4,ERBB2,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK2,IKBKB,INSR,IRAK1,ITK,JAK1,JAK2,KDR,KIT,LCK,LYN,MAP3K1,MAP3K10,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K2,MAP4K3,MAP4K5,MAPK10,MAPK11,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MELK,MET,MTOR,NTRK1,NTRK2,NTRK3,PDGFRB,PDK1,PDK2,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,SIK2,SIK3,SRC,STK10,STK33,SYK,TEK,TNIK,TTK,TYRO3,ULK1,YES1 89
kinase-selectivity-class ACVR2A,ACVR2B,ALK,AURKA,AURKB,AURKC,AXL,BLK,BRAF,CAMK2D,CDK1,CDK9,CLK4,CSF1R,DDR1,DYRK1B,EPHB4,ERBB2,FGFR1,FLT1,FLT3,FLT4,FYN,GAK,GRK2,IRAK1,IRAK3,JAK1,KDR,KIT,LCK,LYN,MAP3K1,MAP3K11,MAP3K21,MAP3K7,MAP4K1,MAP4K3,MAP4K5,MAPK12,MAPK14,MAPK7,MARK4,MET,MKNK2,MST1R,MTOR,NTRK1,NTRK3,PDGFRB,PDK1,PDK4,PIK3CA,PIK3CB,PIK3CD,PIK3CG,PRKCD,PRKDC,RET,RIPK1,SIK2,SIK3,STK33,SYK,TEK,TNIK,TTK,TYRO3,ULK1,ULK2 70
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
June 18, 2019 PMDA DAIICHI SANKYO COMPANY, LIMITED
July 20, 2023 FDA DAIICHI SANKYO INC
Nov. 6, 2023 EMA DAIICHI SANKYO EUROPE GMBH

FDA Adverse Event Reporting System (Female)

None

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
No adverse event 92.96 56.13 23 152 38998 42582162

FDA Adverse Event Reporting System (Geriatric)

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
No adverse event 125.53 70.64 33 392 73806 110515068

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
MeSH PA D000092004 Tyrosine Kinase Inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D047428 Protein Kinase Inhibitors
FDA EPC N0000175605 Kinase Inhibitor
FDA MoA N0000194085 FMS-like Receptor Tyrosine Kinase 3 (FLT3) Inhibitors
CHEBI has role CHEBI:35610 antineoplastic agent
CHEBI has role CHEBI:62434 EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor
CHEBI has role CHEBI:167704 necroptosis inhibitor

Related Drugs by ATC class:

L01EX Other protein kinase inhibitors 21 drugs
avapritinibcabozantinibcapivasertibentrectinibgilteritiniblarotrectiniblenvatinibmidostaurinnintedanibpazopanibpexidartinibpralsetinib show all 21 →

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)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 17.7MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL 8129374 March 16, 2027 COMBINATION WITH STANDARD CYTARABINE AND ANTHRACYCLINE INDUCTION AND CYTARABINE CONSOLIDATION, AND AS MAINTENANCE MONOTHERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR ADULT PATIENTS WITH NEWLY DIAGNOSED FLT3-ITD POSITIVE ACUTE MYELOID LEUKEMIA
EQ 17.7MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL 9585892 March 16, 2027 COMBINATION WITH STANDARD CYTARABINE AND ANTHRACYCLINE INDUCTION AND CYTARABINE CONSOLIDATION, AND AS MAINTENANCE MONOTHERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR ADULT PATIENTS WITH NEWLY DIAGNOSED FLT3-ITD POSITIVE ACUTE MYELOID LEUKEMIA
EQ 26.5MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL 8129374 March 16, 2027 COMBINATION WITH STANDARD CYTARABINE AND ANTHRACYCLINE INDUCTION AND CYTARABINE CONSOLIDATION, AND AS MAINTENANCE MONOTHERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR ADULT PATIENTS WITH NEWLY DIAGNOSED FLT3-ITD POSITIVE ACUTE MYELOID LEUKEMIA
EQ 26.5MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL 9585892 March 16, 2027 COMBINATION WITH STANDARD CYTARABINE AND ANTHRACYCLINE INDUCTION AND CYTARABINE CONSOLIDATION, AND AS MAINTENANCE MONOTHERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR ADULT PATIENTS WITH NEWLY DIAGNOSED FLT3-ITD POSITIVE ACUTE MYELOID LEUKEMIA
EQ 17.7MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL 7968543 Aug. 15, 2029 COMBINATION WITH STANDARD CYTARABINE AND ANTHRACYCLINE INDUCTION AND CYTARABINE CONSOLIDATION, AND AS MAINTENANCE MONOTHERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR ADULT PATIENTS WITH NEWLY DIAGNOSED FLT3-ITD POSITIVE ACUTE MYELOID LEUKEMIA
EQ 26.5MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL 7968543 Aug. 15, 2029 COMBINATION WITH STANDARD CYTARABINE AND ANTHRACYCLINE INDUCTION AND CYTARABINE CONSOLIDATION, AND AS MAINTENANCE MONOTHERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR ADULT PATIENTS WITH NEWLY DIAGNOSED FLT3-ITD POSITIVE ACUTE MYELOID LEUKEMIA
EQ 17.7MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL 8836218 March 23, 2030 COMBINATION WITH STANDARD CYTARABINE AND ANTHRACYCLINE INDUCTION AND CYTARABINE CONSOLIDATION, AND AS MAINTENANCE MONOTHERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR ADULT PATIENTS WITH NEWLY DIAGNOSED FLT3-ITD POSITIVE ACUTE MYELOID LEUKEMIA
EQ 26.5MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL 8836218 March 23, 2030 COMBINATION WITH STANDARD CYTARABINE AND ANTHRACYCLINE INDUCTION AND CYTARABINE CONSOLIDATION, AND AS MAINTENANCE MONOTHERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR ADULT PATIENTS WITH NEWLY DIAGNOSED FLT3-ITD POSITIVE ACUTE MYELOID LEUKEMIA
EQ 17.7MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL 9555040 May 14, 2030 COMBINATION WITH STANDARD CYTARABINE AND ANTHRACYCLINE INDUCTION AND CYTARABINE CONSOLIDATION, AND AS MAINTENANCE MONOTHERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR ADULT PATIENTS WITH NEWLY DIAGNOSED FLT3-ITD POSITIVE ACUTE MYELOID LEUKEMIA
EQ 26.5MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL 9555040 May 14, 2030 COMBINATION WITH STANDARD CYTARABINE AND ANTHRACYCLINE INDUCTION AND CYTARABINE CONSOLIDATION, AND AS MAINTENANCE MONOTHERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR ADULT PATIENTS WITH NEWLY DIAGNOSED FLT3-ITD POSITIVE ACUTE MYELOID LEUKEMIA
EQ 17.7MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL 8357690 Feb. 26, 2031 COMBINATION WITH STANDARD CYTARABINE AND ANTHRACYCLINE INDUCTION AND CYTARABINE CONSOLIDATION, AND AS MAINTENANCE MONOTHERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR ADULT PATIENTS WITH NEWLY DIAGNOSED FLT3-ITD POSITIVE ACUTE MYELOID LEUKEMIA
EQ 26.5MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL 8357690 Feb. 26, 2031 COMBINATION WITH STANDARD CYTARABINE AND ANTHRACYCLINE INDUCTION AND CYTARABINE CONSOLIDATION, AND AS MAINTENANCE MONOTHERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR ADULT PATIENTS WITH NEWLY DIAGNOSED FLT3-ITD POSITIVE ACUTE MYELOID LEUKEMIA

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 17.7MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL July 20, 2028 NEW CHEMICAL ENTITY
EQ 26.5MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL July 20, 2028 NEW CHEMICAL ENTITY
EQ 17.7MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL July 20, 2030 FOR USE IN COMBINATION WITH STANDARD INDUCTION AND CONSOLIDATION, AND AS MAINTENANCE THERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR THE TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) THAT IS FLT3 INTERNAL TANDEM DUPLICATION (ITD)-POSITIVE AS DETECTED BY AN FDA-APPROVED TEST
EQ 26.5MG BASE VANFLYTA DAIICHI SANKYO INC N216993 July 20, 2023 RX TABLET ORAL July 20, 2030 FOR USE IN COMBINATION WITH STANDARD INDUCTION AND CONSOLIDATION, AND AS MAINTENANCE THERAPY FOLLOWING CONSOLIDATION CHEMOTHERAPY, FOR THE TREATMENT OF ADULT PATIENTS WITH NEWLY DIAGNOSED ACUTE MYELOID LEUKEMIA (AML) THAT IS FLT3 INTERNAL TANDEM DUPLICATION (ITD)-POSITIVE 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 Kd 8.80 SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Ephrin type-A receptor 7 Kinase Kd 5.43 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
Mitogen-activated protein kinase 9 Kinase Kd 5.05 CHEMBL
Calcium/calmodulin-dependent protein kinase kinase 1 Kinase Kd 5.32 CHEMBL
Epithelial discoidin domain-containing receptor 1 Kinase Kd 7.09 CHEMBL
Mitogen-activated protein kinase kinase kinase 19 Kinase Kd 5.70 CHEMBL
Cyclin-dependent kinase 7 Kinase Kd 5 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
Tyrosine-protein kinase Yes Kinase Kd 4.66 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
Ribosomal protein S6 kinase alpha-3 Kinase Kd 4.57 CHEMBL
Myosin light chain kinase, smooth muscle Kinase Kd 6.39 CHEMBL
High affinity nerve growth factor receptor Kinase Kd 5.64 CHEMBL
Angiopoietin-1 receptor Kinase Kd 4.96 CHEMBL
Tyrosine-protein kinase Lyn Kinase Kd 5.24 CHEMBL
Serine/threonine-protein kinase 10 Kinase Kd 5.68 CHEMBL
Aurora kinase C Kinase Kd 4.55 CHEMBL
Serine/threonine-protein kinase 17A Kinase Kd 4.57 CHEMBL
Ephrin type-A receptor 6 Kinase Kd 5.04 CHEMBL
TRAF2 and NCK-interacting protein kinase Kinase Kd 5.55 CHEMBL
Mitogen-activated protein kinase 12 Kinase Kd 5.10 CHEMBL
Ephrin type-A receptor 3 Kinase Kd 5.19 CHEMBL
Mitogen-activated protein kinase 14 Kinase Kd 5.43 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
Cyclin-dependent kinase 16 Kinase Kd 4.62 CHEMBL
Tyrosine-protein kinase ITK/TSK Kinase Kd 4.66 CHEMBL
Tyrosine-protein kinase ZAP-70 Kinase Kd 4.52 CHEMBL
Tyrosine-protein kinase receptor UFO Kinase Kd 4.75 CHEMBL
BDNF/NT-3 growth factors receptor Kinase Kd 6.21 CHEMBL
Cyclin-dependent kinase 17 Kinase Kd 4.68 CHEMBL
Cyclin-dependent kinase 18 Kinase Kd 4.66 CHEMBL
Mitogen-activated protein kinase kinase kinase MLT Kinase Kd 5.06 CHEMBL
Tyrosine-protein kinase receptor Tie-1 Kinase Kd 5.50 CHEMBL
NT-3 growth factor receptor Kinase Kd 6.26 CHEMBL
SRSF protein kinase 1 Kinase IC50 4.66 CHEMBL
Discoidin domain-containing receptor 2 Kinase Kd 6.16 CHEMBL
Aurora kinase B Kinase Kd 6.50 CHEMBL
Tyrosine-protein kinase Blk Kinase IC50 7.68 CHEMBL
Mitogen-activated protein kinase kinase kinase kinase 4 Kinase Kd 5.60 CHEMBL
Tyrosine-protein kinase Mer Kinase Kd 4.62 CHEMBL
Cyclin-dependent kinase 19 Kinase Kd 4.82 CHEMBL
Cyclin-dependent kinase 8 Kinase Kd 4.68 CHEMBL
Serine/threonine-protein kinase 24 Kinase Kd 4.60 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
Casein kinase I isoform alpha Kinase Kd 4.77 CHEMBL
Misshapen-like kinase 1 Kinase Kd 5.80 CHEMBL
Interleukin-1 receptor-associated kinase 4 Kinase IC50 8.69 CHEMBL
Cyclin-dependent kinase-like 2 Kinase Kd 4.96 CHEMBL
Serine/threonine-protein kinase PAK 3 Kinase Kd 5.37 CHEMBL
Homeodomain-interacting protein kinase 3 Kinase Kd 4.70 CHEMBL
Homeodomain-interacting protein kinase 4 Kinase Kd 6.50 CHEMBL
Mitogen-activated protein kinase kinase kinase 7 Kinase Kd 5.07 CHEMBL
Bone morphogenetic protein receptor type-1B Kinase Kd 5.64 CHEMBL
Myosin light chain kinase 3 Kinase Kd 6.39 CHEMBL
Receptor-interacting serine/threonine-protein kinase 3 Kinase IC50 6.21 CHEMBL
Myosin-10 Enzyme Kd 6.12 CHEMBL
Ephrin type-B receptor 6 Kinase Kd 5.92 CHEMBL

External reference:

IDSource
7LA4O6Q0D3 UNII
1132827-21-4 SECONDARY_CAS_RN
4042448 VANDF
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
C544967 MESH_SUPPLEMENTAL_RECORD_UI
5658 IUPHAR_LIGAND_ID
42444711000001107 SNOMEDCT_US
42444811000001104 SNOMEDCT_US
369642 MMSL
41829 MMSL
41843 MMSL
d10084 MMSL
019499 NDDF
019500 NDDF
2643048 RXNORM
7LA4O6Q0D3 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
VANFLYTA HUMAN PRESCRIPTION DRUG LABEL 1 65597-504 TABLET, FILM COATED 17.70 mg ORAL NDA 31 sections
VANFLYTA HUMAN PRESCRIPTION DRUG LABEL 1 65597-504 TABLET, FILM COATED 17.70 mg ORAL NDA 31 sections
VANFLYTA HUMAN PRESCRIPTION DRUG LABEL 1 65597-511 TABLET, FILM COATED 26.50 mg ORAL NDA 31 sections
VANFLYTA HUMAN PRESCRIPTION DRUG LABEL 1 65597-511 TABLET, FILM COATED 26.50 mg ORAL NDA 31 sections