Details of the Drug

General Information of Drug (ID: DMUKC5L)

Drug Name
Tivozanib
Synonyms ASP4130/AV-951
Indication
Disease Entry ICD 11 Status REF
Renal cell carcinoma 2C90 Approved [1]
ATC Code
L01EK03: Tivozanib
L01EK: Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors
L01E: PROTEIN KINASE INHIBITORS
L01: ANTINEOPLASTIC AGENTS
L: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 454.9
Logarithm of the Partition Coefficient (xlogp) 4
Rotatable Bond Count (rotbonds) 6
Hydrogen Bond Donor Count (hbonddonor) 2
Hydrogen Bond Acceptor Count (hbondacc) 7
ADMET Property
Absorption AUC
The area under the plot of plasma concentration (AUC) of drug is 1084 +/- 417.0 mcgh/L [2]
Absorption Cmax
The maximum plasma concentration (Cmax) of drug is 12.1 +/- 5.67 mcg/L [2]
Absorption Tmax
The time to maximum plasma concentration (Tmax) is 10 h [2]
Clearance
The clearance of drug is 0.75 L/h [2]
Elimination
After oral ingestion of a radiolabeled 1.34 mg dose of tivozanib in healthy volunteers, 79% of the administered dose was found in the feces (with 26% unchanged) and 12% was found in the urine solely as metabolites [3]
Half-life
The concentration or amount of drug in body reduced by one-half in 111 hours [2]
Metabolism
The drug is metabolized via the CYP3A4 [2]
Vd
The volume of distribution (Vd) of drug is 123 L [2]
Chemical Identifiers
Formula
C22H19ClN4O5
IUPAC Name
1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea
Canonical SMILES
CC1=CC(=NO1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)Cl
InChI
InChI=1S/C22H19ClN4O5/c1-12-8-21(27-32-12)26-22(28)25-16-5-4-13(9-15(16)23)31-18-6-7-24-17-11-20(30-3)19(29-2)10-14(17)18/h4-11H,1-3H3,(H2,25,26,27,28)
InChIKey
SPMVMDHWKHCIDT-UHFFFAOYSA-N
Cross-matching ID
PubChem CID
9911830
ChEBI ID
CHEMBL1289494
CAS Number
475108-18-0
UNII
172030934T
DrugBank ID
DB11800
TTD ID
D0W7JZ
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Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Vascular endothelial growth factor receptor 1 (FLT-1) TT2Q6G1 VGFR1_HUMAN Inhibitor [1]
Vascular endothelial growth factor receptor 2 (KDR) TTUTJGQ VGFR2_HUMAN Modulator [1]
Vascular endothelial growth factor receptor 3 (FLT-4) TTDCBX5 VGFR3_HUMAN Modulator [1]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Renal cell carcinoma
ICD Disease Classification 2C90
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Vascular endothelial growth factor receptor 2 (KDR) DTT KDR 1.98E-01 0.11 0.2
Vascular endothelial growth factor receptor 3 (FLT-4) DTT FLT4 6.00E-01 -0.04 -0.23
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

References

1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services
2 FDA Approved Drug Products: FOTIVDA (tivozanib) capsules, for oral use
3 Cotreau MM, Hale CL, Jacobson L, Oelke CS, Strahs AL, Kochan RG, Sanga M, Slichenmyer W, Vargo DL: Absorption, Metabolism, and Excretion of [(14) C]-Tivozanib, a Vascular Endothelial Growth Factor Receptor Tyrosine Kinase Inhibitor, in Healthy Male Participants: A Phase I, Open-Label, Mass-Balance Study. Clin Pharmacol Drug Dev. 2012 Jul;1(3):102-9. doi: 10.1177/2160763X12447303.