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

Stem definitionDrug idCAS RN
angiogenesis inhibitors 5258 475108-18-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • tivozanib
  • tivozanib hydrochloride monohydrate
  • fotivda
  • Kil8951
  • AV-951
  • KRN951
Tivozanib is an oral, once-daily, vascular endothelial growth factor (VEGF) tyrosine kinase inhibitor (TKI). It is a potent, selective and long half-life inhibitor of all three VEGF receptors and is designed to optimize VEGF blockade while minimizing off-target toxicities, potentially resulting in improved efficacy and minimal dose modifications. Tivozanib is indicated as first line treatment of adult patients with advanced renal cell carcinoma (RCC) and for adult patients who are VEGFR and mTOR pathway inhibitor-naive following disease progression after one prior treatment with cytokine therapy for advanced RCC.
  • Molecular weight: 454.87
  • Formula: C22H19ClN4O5
  • CLOGP: 4.62
  • LIPINSKI: 0
  • HAC: 9
  • HDO: 2
  • TPSA: 107.74
  • ALOGS: -3.94
  • ROTB: 6

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Aug. 24, 2017 EMA EUSA Pharma (UK) Limited

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
ATC L01XE34 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Protein kinase inhibitors

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Renal cell carcinoma indication 702391001 DOID:4450

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 10.87 acidic
pKa2 12.3 acidic
pKa3 4.95 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
Vascular endothelial growth factor receptor 1 Kinase INHIBITOR IC50 9.68 SCIENTIFIC LITERATURE DRUG LABEL
Vascular endothelial growth factor receptor 2 Kinase INHIBITOR IC50 9.80 SCIENTIFIC LITERATURE DRUG LABEL
Vascular endothelial growth factor receptor 3 Kinase INHIBITOR IC50 9.62 SCIENTIFIC LITERATURE DRUG LABEL
Mast/stem cell growth factor receptor Kit Kinase INHIBITOR IC50 8.79 SCIENTIFIC LITERATURE
Platelet-derived growth factor receptor beta Kinase INHIBITOR IC50 8.76 SCIENTIFIC LITERATURE
Receptor-type tyrosine-protein kinase FLT3 Kinase INHIBITOR IC50 6.37 SCIENTIFIC LITERATURE
Fibroblast growth factor receptor 1 Kinase INHIBITOR IC50 6.52 SCIENTIFIC LITERATURE
Hepatocyte growth factor receptor Kinase INHIBITOR IC50 5.87 SCIENTIFIC LITERATURE

External reference:

IDSource
172030934T UNII
9203 INN_ID
763513002 SNOMEDCT_US
34747 MMSL
017888 NDDF
738747006 SNOMEDCT_US
9911830 PUBCHEM_CID
AV9 PDB_CHEM_ID
DB11800 DRUGBANK_ID
D09683 KEGG_DRUG
CHEMBL1289494 ChEMBL_ID
CHEMBL2105756 ChEMBL_ID
6058 IUPHAR_LIGAND_ID
C553176 MESH_SUPPLEMENTAL_RECORD_UI

Pharmaceutical products:

None