> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/asset/tivozanib-a703ca7a-f620-4d6d-8803-f01a7514a28d
> Record changed: 2026-10-13

# Tivozanib

Highest phase reached

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1289494)

Drug type

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1289494)

First approval year

2017

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1289494)

## Development status

**First approval year**

2017

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1289494)

**Listing at source**

Listed

**Highest phase reached**

Approved

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1289494)

## Names and chemistry

**Drug type**

Small molecule

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1289494)

**Drug name**

Tivozanib

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1289494)

**Molecular weight**

454.87

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1289494)

**Structure (SMILES)**

COc1cc2nccc(Oc3ccc(NC(=O)Nc4cc(C)on4)c(Cl)c3)c2cc1OC

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1289494)

### Other names (37)

- 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.

## Identifiers

**ATC classification codes**

- L01EK03

Sources for recorded values

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1289494)

**CAS registry numbers**

- 475108-18-0

**ChEMBL ID**

CHEMBL1289494

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1289494)

**InChIKey**

SPMVMDHWKHCIDT-UHFFFAOYSA-N

Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL1289494)

**PubChem compound IDs**

- 9911830

**RxNorm IDs (RxCUI)**

- 2534233

**FDA ingredient codes (UNII)**

- 172030934T

## Regulatory information

### United States

**Applicant**

AVEO PHARMS

**Approval date**

10 Mar 2021

**Application number**

NDA212904

### Other regulatory facts

**First in class**

No

**Orphan designation**

No

**Availability**

Prescription only

## Pharmacology

### Drug classification

**Pharmacology name**

tivozanib

**Type**

Synthetic organic

**Drug name stem**

\-anib

**Approval recorded by Guide to Pharmacology**

Yes

#### Administration routes

- Oral

### Mechanisms of action (6)

- **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

### Open Targets mechanisms (3)

- **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

### DrugCentral mechanisms (8)

- **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

### Investigated indications (13)

- **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

### Open Targets indications (27)

- **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.

### Reported adverse events (3)

- **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

### Trial references (24)

- NCT00502307  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00502307)
- NCT00563147  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00563147)
- NCT01030783  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01030783)
- NCT01076010  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01076010)
- NCT01297244  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01297244)
- NCT01673386  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01673386)
- NCT01834183  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01834183)
- NCT03136627  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03136627)
- NCT00660153  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00660153)
- NCT01478594  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01478594)
- NCT00717340  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00717340)
- NCT00826878  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00826878)
- NCT01728181  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01728181)
- NCT01210846  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01210846)
- NCT01782313  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01782313)
- NCT01807156  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01807156)
- NCT01835223  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01835223)
- NCT03970616  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT03970616)
- NCT01846871  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01846871)
- NCT01853644  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01853644)
- NCT01885949  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT01885949)
- NCT04645160  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04645160)
- NCT04987203  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT04987203)
- NCT06053658  
Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT06053658)

## Dosing

**Dose**

1.34 mg

**Route**

Oral

**How often**

21 days on treatment followed by 7 days off treatment every 28 days

### Conditions of use (3)

- Do not open capsule
- Swallow capsule whole with water
- Take with or without food

## Chemical properties

**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

## Evidence counts

**Recorded assays**

1,686

**Active assays**

249

### Active assay types (3)

- Confirmatory
- Other
- Screening

## Pharmacologic actions

- Protein Kinase Inhibitors  
Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D047428.html)

## 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](https://trialight.com/data/condition/breast-cancer-8ac10da3-93bd-54c5-a93b-265bc6699689.md) Phase 1
- [Cholangiocarcinoma](https://trialight.com/data/condition/cholangiocarcinoma-3777afe4-5189-5eb1-82f8-0c3446cb902f.md) Phase 1
- [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) Phase 2
- [Fallopian tube cancer](https://trialight.com/data/condition/fallopian-tube-cancer-b95d05ee-41d5-565a-87e1-041170b88760.md) Phase 2
- Glioblastoma Phase 2
- [Hepatocellular carcinoma](https://trialight.com/data/condition/hepatocellular-carcinoma-fc1014ac-5a3c-551d-98ea-95306009e299.md) Phase 2
- Neoplasm Phase 3
- [Non-small cell lung carcinoma](https://trialight.com/data/condition/non-small-cell-lung-carcinoma-a86c1d60-523f-5ea7-a5e1-39ed4a2296f8.md) Phase 1
- [Ovarian cancer](https://trialight.com/data/condition/ovarian-cancer-f64f2018-55a5-553a-8960-76cb4906aa17.md) Phase 2
- [Prostate cancer](https://trialight.com/data/condition/prostate-cancer-3659fc70-617b-5868-a093-ae819ffc6755.md) Phase 2
- Renal cell adenocarcinoma Phase 3
- [Renal cell carcinoma](https://trialight.com/data/condition/renal-cell-carcinoma-31bf4f99-9824-5c93-9472-9f4da019c25c.md) Phase 3
- [Soft tissue sarcoma](https://trialight.com/data/condition/soft-tissue-sarcoma-3abd95b0-f8eb-5f0b-9e18-b37874e7f988.md) Phase 2

### Targets (5)

- [FLT1](https://trialight.com/data/target/flt1-2cfcec95-3fff-5be9-8423-701697547fa0.md) Vascular endothelial growth factor receptor inhibitor
- [FLT4](https://trialight.com/data/target/flt4-c94058e2-ff1e-553b-92a5-8e7ee9305a80.md) Vascular endothelial growth factor receptor inhibitor
- [KDR](https://trialight.com/data/target/kdr-4ab08263-0477-533e-ac3f-96e20d343c4b.md) Vascular endothelial growth factor receptor inhibitor
- [KIT](https://trialight.com/data/target/kit-4430e375-befc-5469-b7bf-a28dfc518a97.md) Stem cell growth factor receptor inhibitor
- [PDGFRB](https://trialight.com/data/target/pdgfrb-b0fcbfa5-50cf-5648-aa6d-c7487708468d.md) Platelet-derived growth factor receptor beta inhibitor

---

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