Tivozanib

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Name
Tivozanib
Accession Number
DB11800
Type
Small Molecule
Groups
Investigational
Description

Tivozanib has been used in trials studying the treatment and basic science of Solid Tumors, Glioblastoma, Ovarian Cancer, Prostate Cancer, and Stage IV Disease, among others.

Structure
Thumb
Synonyms
Not Available
External IDs
AV-951 / KIL-8951 / KRN-951
Product Ingredients
IngredientUNIICASInChI Key
Tivozanib Hydrochloride8A9H4VK35Z 682745-41-1RQXMKRRBJITKRN-UHFFFAOYSA-N
Approved Prescription Products
Not Available
Approved Generic Prescription Products
Not Available
Approved Over the Counter Products
Not Available
Unapproved/Other Products
Not Available
International/Other Brands
Not Available
Brand mixtures
Not Available
Categories
UNII
172030934T
CAS number
475108-18-0
Weight
Average: 454.863
Monoisotopic: 454.104397445
Chemical Formula
C22H19ClN4O5
InChI Key
SPMVMDHWKHCIDT-UHFFFAOYSA-N
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)
IUPAC Name
N'-{2-chloro-4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N-(5-methyl-2,3-dihydro-1,2-oxazol-3-ylidene)carbamimidic acid
SMILES
COC1=C(OC)C=C2C(OC3=CC(Cl)=C(C=C3)N=C(O)N=C3NOC(C)=C3)=CC=NC2=C1

Pharmacology

Indication
Not Available
Structured Indications
Not Available
Pharmacodynamics
Not Available
Mechanism of action
Not Available
Absorption
Not Available
Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life
Not Available
Clearance
Not Available
Toxicity
Not Available
Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Tivozanib.Approved
BevacizumabBevacizumab may increase the cardiotoxic activities of Tivozanib.Approved, Investigational
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Tivozanib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Tivozanib.Approved, Investigational
DeslanosideDeslanoside may decrease the cardiotoxic activities of Tivozanib.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Tivozanib.Approved
DigoxinDigoxin may decrease the cardiotoxic activities of Tivozanib.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Tivozanib.Approved, Investigational
OleandrinAnvirzel may decrease the cardiotoxic activities of Tivozanib.Experimental
OuabainOuabain may decrease the cardiotoxic activities of Tivozanib.Approved
PaclitaxelThe risk or severity of adverse effects can be increased when Paclitaxel is combined with Tivozanib.Approved, Vet Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Tivozanib.Approved, Investigational
Food Interactions
Not Available

References

Synthesis Reference
Not Available
General References
Not Available
External Links
ChemSpider
8087481
BindingDB
50331095
ChEBI
91327
ChEMBL
CHEMBL1289494
HET
AV9
ATC Codes
L01XE34 — Tivozanib
AHFS Codes
Not Available
PDB Entries
Not Available
FDA label
Not Available
MSDS
Not Available

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedNot AvailableAdvanced Solid Tumors1
1CompletedBasic ScienceHepatic Impairment1
1CompletedTreatmentAdvanced Solid Tumors / Locally Advanced or Metastatic Breast or Colorectal Cancer1
1CompletedTreatmentFood Effect of Tivozanib in Health Subjects1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentNon-Small-Cell Lung Carcinoma (NSCLC)1
1, 2Active Not RecruitingTreatmentAdvanced Adult Hepatocellular Carcinoma / Non-Resectable Hepatocellular Carcinoma1
1, 2CompletedTreatmentGastrointestinal Cancers1
1, 2WithdrawnTreatmentEGFR Unknown or Wild-type / Non-Small-Cell Lung Carcinoma (NSCLC) / Stage IV Disease1
2Active Not RecruitingTreatmentProstate Cancer1
2Active Not RecruitingTreatmentRecurrent Adult Soft Tissue Sarcoma / Stage III Adult Soft Tissue Sarcoma / Stage IV Adult Soft Tissue Sarcoma1
2CompletedTreatmentColorectal Cancers1
2CompletedTreatmentGlioblastomas1
2CompletedTreatmentMetastatic Renal Cell Carcinoma1
2CompletedTreatmentRenal Cell Adenocarcinoma2
2RecruitingTreatmentRecurrent Epithelial Ovarian Cancer / Recurrent Fallopian Tube Cancer / Recurrent Primary Peritoneal Cancer1
2TerminatedTreatmentCancer, Ovarian / Fallopian Tube Cancer / Primary Peritoneal Carcinoma1
2TerminatedTreatmentHepatocellular Cancer1
2TerminatedTreatmentTriple Negative Breast Cancer (TNBC)1
2WithdrawnTreatmentRenal Cell Adenocarcinoma1
3Active Not RecruitingTreatmentRenal Cell Adenocarcinoma1
3CompletedTreatmentAdvanced Renal Cell Carcinoma2
Not AvailableCompletedTreatmentTumors, Solid1
Not AvailableWithdrawnTreatmentStage II Renal Cell Cancer / Stage III Renal Cell Cancer1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00792 mg/mLALOGPS
logP3.87ALOGPS
logP3.78ChemAxon
logS-4.8ALOGPS
pKa (Strongest Acidic)6.61ChemAxon
pKa (Strongest Basic)5.74ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count8ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area106.79 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity130.91 m3·mol-1ChemAxon
Polarizability45.72 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted LC-MS/MS Spectrum - 10V, PositivePredicted LC-MS/MSNot Available
Predicted LC-MS/MS Spectrum - 20V, PositivePredicted LC-MS/MSNot Available
Predicted LC-MS/MS Spectrum - 40V, PositivePredicted LC-MS/MSNot Available
Predicted LC-MS/MS Spectrum - 10V, NegativePredicted LC-MS/MSNot Available
Predicted LC-MS/MS Spectrum - 20V, NegativePredicted LC-MS/MSNot Available
Predicted LC-MS/MS Spectrum - 40V, NegativePredicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of chemical entities known as diarylethers. These are organic compounds containing the dialkyl ether functional group, with the formula ROR', where R and R' are aryl groups.
Kingdom
Chemical entities
Super Class
Organic compounds
Class
Organic oxygen compounds
Sub Class
Organooxygen compounds
Direct Parent
Diarylethers
Alternative Parents
Quinolines and derivatives / N-phenylureas / Anisoles / Phenoxy compounds / Alkyl aryl ethers / Chlorobenzenes / Pyridines and derivatives / Imidolactams / Aryl chlorides / Isoxazoles
show 10 more
Substituents
Diaryl ether / N-phenylurea / Quinoline / Phenoxy compound / Anisole / Phenol ether / Alkyl aryl ether / Halobenzene / Chlorobenzene / Aryl chloride
show 21 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Drug created on October 20, 2016 14:49 / Updated on September 01, 2017 12:13