Tivozanib
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2017
- First approval year
- 2017
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Tivozanib
- Molecular weight
- 454.87
- Structure (SMILES)
- COc1cc2nccc(Oc3ccc(NC(=O)Nc4cc(C)on4)c(Cl)c3)c2cc1OC
- asp 4130
- ASP-4130
- av 951
- AV-951
- dc 001164tivozanibav9511 2 chloro 4 6 7 dimethoxyquinolin 4 yl oxy phenyl 3 5 methylisoxazo 3 yl urea
- DC-001164TIVOZANIBAV9511-(2-CHLORO-4((6,7-DIMETHOXYQUINOLIN-4-YL)OXY)PHENYL)-3-(5-METHYLISOXAZO-3-YL)UREA
- fotivda
- FOTIVDA
- kil 8951
- Kil-8951
- KIL-8951
- kil8951
- KIL8951
- krn 951
- Krn-951
- KRN-951
- krn951
- KRN951
- ophthotech
- OPHTHOTECH
- tivozanib
- Tivozanib
- TIVOZANIB
- TIVOZANIB (AV-951)
- TIVOZANIB (OPHTHALMIC)
And 12 more, listed on the interactive page.
- ATC classification codes
- L01EK03
Sources for recorded values
- CAS registry numbers
- 475108-18-0
- ChEMBL ID
- CHEMBL1289494
- InChIKey
- SPMVMDHWKHCIDT-UHFFFAOYSA-N
- PubChem compound IDs
- 9911830
- RxNorm IDs (RxCUI)
- 2534233
- FDA ingredient codes (UNII)
- 172030934T
- Applicant
- AVEO PHARMS
- Approval date
- 10 Mar 2021
- Application number
- NDA212904
- First in class
- No
- Orphan designation
- No
- Availability
- Prescription only
- Pharmacology name
- tivozanib
- Type
- Synthetic organic
- Drug name stem
- -anib
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- Oral
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- fms related receptor tyrosine kinase 1
- Gene symbol
- FLT1
- Protein identifier
- P17948
- Median affinity
- 9.68
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- fms related receptor tyrosine kinase 4
- Gene symbol
- FLT4
- Protein identifier
- P35916
- Median affinity
- 9.62
- Affinity units
- pIC50
- Primary target
- Yes
- Action
- Inhibition
- Action type
- Inhibitor
- Target
- kinase insert domain receptor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Median affinity
- 9.8
- Affinity units
- pIC50
- Primary target
- Yes
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Protein identifier
- P17948
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Protein identifier
- P35916
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Protein identifier
- P35968
- Mechanism
- Platelet-derived growth factor receptor beta inhibitor
- Action type
- Inhibitor
- Target
- Platelet-derived growth factor receptor beta
- Mechanism
- Stem cell growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Mast/stem cell growth factor receptor Kit
- Mechanism
- Vascular endothelial growth factor receptor inhibitor
- Action type
- Inhibitor
- Target
- Vascular endothelial growth factor receptor
- Action type
- Inhibitor
- Gene symbol
- MET
- Protein identifier
- P08581
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- PDGFRB
- Protein identifier
- P09619
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- KIT
- Protein identifier
- P10721
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- FGFR1
- Protein identifier
- P11362
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- FLT1
- Protein identifier
- P17948
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- FLT4
- Protein identifier
- P35916
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- KDR
- Protein identifier
- P35968
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Inhibitor
- Gene symbol
- FLT3
- Protein identifier
- P36888
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Carcinoma, Hepatocellular
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000182
- Subject identifier
- D006528
- Condition
- Glioblastoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:0000519
- Subject identifier
- D005909
- Condition
- Neoplasms
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000616
- Subject identifier
- D009369
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000681
- Subject identifier
- D002292
- Condition
- Carcinoma, Non-Small-Cell Lung
- Highest recorded phase
- 1
- Condition identifier
- EFO:0003060
- Subject identifier
- D002289
- Condition
- Cholangiocarcinoma
- Highest recorded phase
- 1
- Condition identifier
- EFO:0005221
- Subject identifier
- D018281
- Condition
- Carcinoma, Renal Cell
- Highest recorded phase
- 3
- Condition identifier
- EFO:0005708
- Subject identifier
- D002292
- Condition
- Sarcoma
- Highest recorded phase
- 2
- Condition identifier
- EFO:1001968
- Subject identifier
- D012509
- Condition
- Fallopian Tube Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0002158
- Subject identifier
- D005185
- Condition
- Colorectal Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0005575
- Subject identifier
- D015179
- Condition
- Breast Neoplasms
- Highest recorded phase
- 1
- Condition identifier
- MONDO:0007254
- Subject identifier
- D001943
- Condition
- Ovarian Neoplasms
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0008170
- Subject identifier
- D010051
- Condition
- Prostatic Neoplasms, Castration-Resistant
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0008315
- Subject identifier
- D064129
- Condition identifier
- EFO_0000182
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000519
- Highest recorded phase
- 2
- Condition identifier
- EFO_0000616
- Condition identifier
- EFO_0000681
- Condition identifier
- EFO_0003060
- Condition identifier
- EFO_0005708
- Highest recorded phase
- 3
- Condition identifier
- EFO_1001968
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0002158
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0003060
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005005
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005070
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005086
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005220
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0005233
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0005549
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005575
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0007254
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0007256
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008170
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0008315
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0009831
- Highest recorded phase
- 1
- Condition identifier
- MONDO_0015686
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0017884
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0017885
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0018078
- Highest recorded phase
- 2
And 2 more, listed on the interactive page.
- Event
- disease progression
- Reports
- 5
- Reporting signal score
- 9.66673
- Event
- sepsis
- Reports
- 5
- Reporting signal score
- 10.7188
- Event
- sinus tachycardia
- Reports
- 4
- Reporting signal score
- 13.0715
- NCT00502307
- NCT00563147
- NCT01030783
- NCT01076010
- NCT01297244
- NCT01673386
- NCT01834183
- NCT03136627
- NCT00660153
- NCT01478594
- NCT00717340
- NCT00826878
- NCT01728181
- NCT01210846
- NCT01782313
- NCT01807156
- NCT01835223
- NCT03970616
- NCT01846871
- NCT01853644
- NCT01885949
- NCT04645160
- NCT04987203
- NCT06053658
- Dose
- 1.34 mg
- Route
- Oral
- How often
- 21 days on treatment followed by 7 days off treatment every 28 days
- Do not open capsule
- Swallow capsule whole with water
- Take with or without food
- Hydrogen bond acceptors
- 7
- Hydrogen bond donors
- 2
- Polar surface area
- 107.74
- Calculated partition coefficient (ALogP)
- 5.64
- Calculated partition coefficient (XLogP)
- 4
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 6
- Heavy atoms
- 32
- Molecular formula
- C22H19ClN4O5
- Monoisotopic mass
- 454.1043974
- Natural product
- Yes
- Recorded assays
- 1,686
- Active assays
- 249
- Confirmatory
- Other
- Screening
- Protein Kinase Inhibitors
Related records
Trials (167)
- A Biomarker Study of Tivozanib in Subjects With Advanced Renal Cell Carcinoma
- A Cardiac Safety Study of Tivozanib to Evaluate the Electrocardiogram and Pharmacokinetic-Electrocardiogram Dynamics in Subjects With Advanced Solid Tumors
- A Multicenter Study Assessing the Efficacy and Safety of STN1010904 Ophthalmic Suspension 0.03% and 0.1% Compared With Vehicle in Subjects With Fuchs Endothelial Corneal Dystrophy (FECD)
- A Pharmacokinetics (PK) Study in Healthy Adults
- A Phase 1 Study to Evaluate The Effect of Ketoconazole on the Pharmacokinetics of Tivozanib in Healthy Subjects
- A Phase 1 Study to Evaluate the Effect of Rifampin on the Pharmacokinetics of Tivozanib in Healthy Subjects
- A Phase 1b, Open-Label, Dose-Finding Study to Evaluate the Safety of Tivozanib (AV-951) in Combination With Temsirolimus in Subjects With Metastatic Renal Cell Carcinoma
- A Phase 1b/2a, Open-Label, Multi-Center Study of Tivozanib (AV-951) in Combination With Paclitaxel in Subjects With Advanced or Metastatic Breast Cancer
- A Phase 2 Double-masked Study of VVN539 in Subjects With Elevated Intraocular Pressure
- A Phase 2 Study of RCI001 Ophthalmic Solution in Participants With Dry Eye Disease
- A Phase 2 Study of VVN461 Ophthalmic Solution for Noninfectious Anterior Uveitis
- A Phase 3 Study of VVN461 Ophthalmic Solution for Noninfectious Anterior Uveitis
- A Phase 3, Multi-Center Study Evaluating PL9643 in Patients with Dry Eye
- A Phase I/II Study of Tivozanib and Erlotinib as Initial Treatment for Metastatic Non-small Cell Lung Cancer Assigned by VeriStrat® Serum Proteomic Evaluation
- A Phase II Study of STSP-0902 Ophthalmic Solution in Patients With Neurotrophic Keratitis
- A Phase II Study of Tivozanib in Patients With Metastatic and Non-resectable Soft Tissue Sarcomas
- A Randomized, Open-label, Active-controlled, Phase 2a Clinical Trial to Evaluate the Efficacy and Safety of TFC-003 in Patients With Primary Open-angle Glaucoma or Ocular Hypertension
- A Rollover Protocol to Allow Continued Access to Tivozanib (AV 951) for Subjects Enrolled in Other Tivozanib Protocols
- A Safety Study of IVMED-85 Ophthalmic Solution in Healthy Adults
- A Safety, Efficacy and Pharmacokinetic Study of AGN-199201 and AGN-190584 in Patients With Presbyopia
In development for (13)
- Breast cancer Phase 1
- Cholangiocarcinoma Phase 1
- Colorectal cancer Phase 2
- Fallopian tube cancer Phase 2
- Glioblastoma Phase 2
- Hepatocellular carcinoma Phase 2
- Neoplasm Phase 3
- Non-small cell lung carcinoma Phase 1
- Ovarian cancer Phase 2
- Prostate cancer Phase 2
- Renal cell adenocarcinoma Phase 3
- Renal cell carcinoma Phase 3
- Soft tissue sarcoma Phase 2