Tivozanib
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Also known as ASP-4130AV-951KIL8951Krn-951Kil-8951TIVOZANIB HCLTIVOZANIB (AV-951)TIVOZANIB (OPHTHALMIC)OPHTHOTECHKRN951FOTIVDASID124955473TivozanibÊTivozanibÂ
Summary
Tivozanib (CHEMBL1289494) is an approved small-molecule vascular endothelial growth factor receptor antagonist (ATC L01EK03) targeting FLT1, KDR, and FLT4; indicated across 13 conditions including neoplasm and renal cell carcinoma.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EK03
- Targets: 3 (FLT1, KDR, FLT4)
- Indications: 13 conditions
- Clinical trials: 36
- Chemistry: 454.9 Da · C22H19ClN4O5
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1289494 |
| Name | Tivozanib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 9911830 |
| ChEBI | CHEBI:91327 |
| ATC | L01EK03 |
| Molecular formula | C22H19ClN4O5 |
| Molecular weight | 454.9 |
| InChIKey | SPMVMDHWKHCIDT-UHFFFAOYSA-N |
SMILES: CC1=CC(=NO1)NC(=O)NC2=C(C=C(C=C2)OC3=C4C=C(C(=CC4=NC=C3)OC)OC)Cl
IUPAC name: 1-[2-chloro-4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-3-(5-methyl-1,2-oxazol-3-yl)urea
ChEBI definition: A member of the class of quinolines that is 6,7-dimethoxyquinoline substituted by a 3-chloro-4-{[(5-methyl-1,2-oxazol-3-yl)carbamoyl]amino}phenoxy group at position 4. It is a potent and selective inhibitor of VEGF receptor tyrosine kinases and was previously in clinical development for the treatment of metastatic renal cell carcinoma.
Pharmacological roles (ChEBI): vascular endothelial growth factor receptor antagonist, antineoplastic agent, apoptosis inducer.
Also known as: ASP-4130, AV-951, KIL8951, Krn-951, KRN-951, Kil-8951, Tivozanib, TIVOZANIB, TIVOZANIB HCL, TIVOZANIB (AV-951), TIVOZANIB (OPHTHALMIC), OPHTHOTECH
Parent form; salt/anhydrous children: CHEMBL2105756, CHEMBL3426917, CHEMBL4784300
Patent coverage: 1,753 distinct patent families (4,455 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 4,192 (94%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| FLT1 | fms related receptor tyrosine kinase 1 | Inhibition | 9.68 | 0.1% | P17948 |
| KDR | kinase insert domain receptor | Inhibition | 9.8 | 1.1% | P35968 |
| FLT4 | fms related receptor tyrosine kinase 4 | Inhibition | 9.62 | 0.2% | P35916 |
Broader ChEMBL bioactivity targets: 42 (assay-derived). Sample: Receptor-interacting serine/threonine-protein kinase 3, Tyrosine-protein kinase ABL1, Vascular endothelial growth factor receptor 1, Platelet-derived growth factor receptor beta, Mast/stem cell growth factor receptor Kit, Vascular endothelial growth factor receptor 3, Receptor-type tyrosine-protein kinase FLT3, Platelet-derived growth factor receptor alpha, Proto-oncogene tyrosine-protein kinase receptor Ret, Ephrin type-A receptor 2, Aurora kinase B, 5-hydroxytryptamine receptor 2A, Alpha-1A adrenergic receptor, Sodium-dependent dopamine transporter, cGMP-inhibited 3’,5’-cyclic phosphodiesterase 3A, Tyrosine-protein kinase Lck, Proto-oncogene tyrosine-protein kinase Src, Vascular endothelial growth factor receptor 2, 3’,5’-cyclic-AMP phosphodiesterase 4D, Ephrin type-B receptor 2.
Bioactivity
ChEMBL activities: 61 potent at pChembl ≥ 5 of 65 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| MAPK3 | 9.89 | IC50 | 0.13 | nM | CHEMBL_ACT_26238416 |
| KDR | 9.8 | IC50 | 0.16 | nM | CHEMBL_ACT_12138557 |
| KDR | 9.8 | IC50 | 0.16 | nM | CHEMBL_ACT_26238405 |
| KDR | 9.8 | IC50 | 0.16 | nM | CHEMBL_ACT_3595762 |
| MAPK1 | 9.74 | IC50 | 0.18 | nM | CHEMBL_ACT_26238417 |
| FLT1 | 9.68 | IC50 | 0.21 | nM | CHEMBL_ACT_12138558 |
| P35969 | 9.68 | IC50 | 0.21 | nM | CHEMBL_ACT_26238406 |
| FLT4 | 9.62 | IC50 | 0.24 | nM | CHEMBL_ACT_12138556 |
| FLT4 | 9.62 | IC50 | 0.24 | nM | CHEMBL_ACT_26238407 |
| KIT | 8.79 | IC50 | 1.63 | nM | CHEMBL_ACT_26238408 |
| PDGFRB | 8.76 | IC50 | 1.72 | nM | CHEMBL_ACT_26238409 |
| KDR | 8.67 | IC50 | 2.14 | nM | CHEMBL_ACT_15249768 |
| PDGFRA | 8.65 | IC50 | 2.26 | nM | CHEMBL_ACT_15249764 |
| PEBP1 | 8.52 | Kd | 3 | nM | CHEMBL_ACT_17925316 |
| FLT4 | 8.51 | IC50 | 3.11 | nM | CHEMBL_ACT_15249766 |
| KDR | 8.47 | IC50 | 3.38 | nM | CHEMBL_ACT_26150872 |
| FLT1 | 8.2 | IC50 | 6.26 | nM | CHEMBL_ACT_15249770 |
| KDR | 8.19 | IC50 | 6.5 | nM | CHEMBL_ACT_26238376 |
| KDR | 8.19 | Ki | 6.5 | nM | CHEMBL_ACT_27790679 |
| RET | 7.92 | Kd | 12 | nM | CHEMBL_ACT_17935227 |
| FLT4 | 7.82 | IC50 | 15 | nM | CHEMBL_ACT_26238377 |
| EPHB2 | 7.76 | IC50 | 17.5 | nM | CHEMBL_ACT_15249762 |
| EPHB2 | 7.62 | IC50 | 24 | nM | CHEMBL_ACT_26238378 |
| FLT1 | 7.52 | IC50 | 30 | nM | CHEMBL_ACT_26238375 |
| PDGFRA | 7.4 | IC50 | 40 | nM | CHEMBL_ACT_26238379 |
| PDGFRB | 7.31 | IC50 | 49 | nM | CHEMBL_ACT_26238380 |
| ABCG2 | 7.16 | IC50 | 70 | nM | CHEMBL_ACT_24777477 |
| KIT | 7.11 | IC50 | 78 | nM | CHEMBL_ACT_26238381 |
| TEK | 7.11 | IC50 | 78 | nM | CHEMBL_ACT_26238382 |
| FRK | 6.84 | Kd | 145 | nM | CHEMBL_ACT_17903841 |
| EPHA2 | 6.83 | Kd | 147 | nM | CHEMBL_ACT_17899534 |
| BCR | 6.8 | Kd | 160 | nM | CHEMBL_ACT_17884559 |
| DDR1 | 6.72 | Kd | 190 | nM | CHEMBL_ACT_17896053 |
| ABL1 | 6.71 | Kd | 195 | nM | CHEMBL_ACT_17878449 |
| ABL2 | 6.52 | Kd | 302 | nM | CHEMBL_ACT_17878735 |
| FGFR1 | 6.52 | IC50 | 299 | nM | CHEMBL_ACT_26238411 |
| EPHB4 | 6.51 | Kd | 310 | nM | CHEMBL_ACT_17900802 |
| KDR | 6.47 | IC50 | 340 | nM | CHEMBL_ACT_15044437 |
| FLT3 | 6.38 | IC50 | 422 | nM | CHEMBL_ACT_26238410 |
| EPHB2 | 6.35 | Kd | 448 | nM | CHEMBL_ACT_17900440 |
| EPHB4 | 6.32 | IC50 | 480 | nM | CHEMBL_ACT_26238383 |
| FGFR1 | 6.28 | IC50 | 530 | nM | CHEMBL_ACT_26238384 |
| MET | 6.26 | IC50 | 550 | nM | CHEMBL_ACT_26238385 |
| DDR2 | 6.23 | Kd | 592 | nM | CHEMBL_ACT_17896287 |
| EPHA5 | 6.22 | Kd | 601 | nM | CHEMBL_ACT_17899967 |
| ABL1 | 6.21 | IC50 | 620 | nM | CHEMBL_ACT_26238386 |
| PTK6 | 6.1 | Kd | 787 | nM | CHEMBL_ACT_17933073 |
| RIPK2 | 6.1 | Kd | 801 | nM | CHEMBL_ACT_17935485 |
| SRC | 6.02 | IC50 | 960 | nM | CHEMBL_ACT_26238387 |
| RIPK3 | 5.87 | Kd | 1346 | nM | CHEMBL_ACT_17935722 |
| MET | 5.87 | IC50 | 1360 | nM | CHEMBL_ACT_26238412 |
| AURKB | 5.81 | Kd | 1562 | nM | CHEMBL_ACT_17884292 |
| LYN | 5.7 | Kd | 2019 | nM | CHEMBL_ACT_17910037 |
| LCK | 5.66 | Kd | 2183 | nM | CHEMBL_ACT_17909495 |
| MAP4K2 | 5.62 | Kd | 2375 | nM | CHEMBL_ACT_17913628 |
| PDGFRB | 5.62 | Kd | 2409 | nM | CHEMBL_ACT_17924682 |
| SLC6A3 | 5.58 | AC50 | 2600 | nM | CHEMBL_ACT_25123713 |
| STK10 | 5.33 | Kd | 4622 | nM | CHEMBL_ACT_17940570 |
| MET | 5.27 | Kd | 5403 | nM | CHEMBL_ACT_17919122 |
| EPHB3 | 5.26 | Kd | 5433 | nM | CHEMBL_ACT_17900587 |
| EPHA4 | 5.25 | Kd | 5563 | nM | CHEMBL_ACT_17899724 |
Target pathways
Aggregated over 3 target gene(s): FLT1, KDR, FLT4.
Top Reactome pathways
8 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| VEGF binds to VEGFR leading to receptor dimerization | 3 | FLT1, FLT4, KDR |
| Neuropilin interactions with VEGF and VEGFR | 2 | FLT1, KDR |
| High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells | 2 | FLT4, KDR |
| Integrin cell surface interactions | 1 | KDR |
| VEGFA-VEGFR2 Pathway | 1 | KDR |
| VEGFR2 mediated cell proliferation | 1 | KDR |
| NOTCH4 Intracellular Domain Regulates Transcription | 1 | FLT4 |
| Signaling by membrane-tethered fusions of PDGFRA or PDGFRB | 1 | KDR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| cell surface receptor protein tyrosine kinase signaling pathway | 3 |
| positive regulation of cell population proliferation | 3 |
| cell migration | 3 |
| peptidyl-tyrosine phosphorylation | 3 |
| positive regulation of cell migration | 3 |
| cellular response to vascular endothelial growth factor stimulus | 3 |
| positive regulation of MAPK cascade | 3 |
| protein autophosphorylation | 3 |
| vascular endothelial growth factor receptor signaling pathway | 3 |
| angiogenesis | 3 |
| protein phosphorylation | 3 |
| vascular endothelial growth factor signaling pathway | 3 |
| sprouting angiogenesis | 2 |
| cell differentiation | 2 |
| positive regulation of angiogenesis | 2 |
Indications & clinical
Indications
3 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).
| Indication | Phase | MONDO | EFO |
|---|---|---|---|
| neoplasm | 3 | MONDO:0005070 | EFO:0000616 |
| renal cell carcinoma | 3 | MONDO:0005086 | EFO:0000681 |
| renal cell adenocarcinoma | 3 | MONDO:0005549 | EFO:0005708 |
9 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.
| Disease (in trials) | Phase | MONDO | EFO |
|---|---|---|---|
| hepatocellular carcinoma | 2 | MONDO:0007256 | EFO:0000182 |
| glioblastoma | 2 | MONDO:0018177 | EFO:0000519 |
| soft tissue sarcoma | 2 | MONDO:0018078 | EFO:1001968 |
| fallopian tube neoplasm | 2 | MONDO:0021092 | MONDO:0002158 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| colorectal neoplasm | 2 | MONDO:0005335 | MONDO:0005575 |
| non-small cell lung carcinoma | 1 | MONDO:0005233 | EFO:0003060 |
| breast neoplasm | 1 | MONDO:0021100 | MONDO:0007254 |
| cholangiocarcinoma | 1 | MONDO:0019087 | EFO:0005221 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 36.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 13 |
| PHASE1 | 10 |
| PHASE1/PHASE2 | 7 |
| PHASE3 | 4 |
| Not specified | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT06661720 | PHASE3 | RECRUITING | Testing the Addition of the Anti-Cancer Drug Tivozanib to Immunotherapy (Pembrolizumab) After Surgery to Remove All Known Sites of Kidney Cancer |
| NCT01030783 | PHASE3 | COMPLETED | A Study to Compare Tivozanib (AV-951) to Sorafenib in Subjects With Advanced Renal Cell Carcinoma |
| NCT01076010 | PHASE3 | COMPLETED | An Extension Treatment Protocol for Subjects Who Have Participated in a Study of Tivozanib Versus Sorafenib in Kidney Carcinoma (Protocol AV-951-09-301). |
| NCT04987203 | PHASE3 | COMPLETED | Study to Compare Tivozanib in Combination With Nivolumab to Tivozanib Monotherapy in Subjects With Renal Cell Carcinoma |
| NCT04645160 | PHASE1/PHASE2 | RECRUITING | Evaluating Efficacy of Tivozanib (AV-951) in Biliary Tract Cancers |
| NCT06053658 | PHASE2 | RECRUITING | Phase 2 Study of Combination Tivozanib and Nivolumab in Advanced Non-Clear Cell Renal Cell Carcinoma |
| NCT07218692 | PHASE2 | NOT_YET_RECRUITING | RP2 and Tivozanib for the Treatment of Metastatic Renal Cell Cancer After Progression on Immunotherapy |
| NCT00502307 | PHASE2 | COMPLETED | A Study of Tivozanib (AV-951), an Oral VEGF Receptor Tyrosine Kinase Inhibitor, in the Treatment of Renal Cell Carcinoma |
| NCT01058655 | PHASE1/PHASE2 | COMPLETED | RAD001 and AV-951 in Patients With Refractory, Metastatic Colorectal Cancer |
| NCT01297244 | PHASE2 | COMPLETED | A Biomarker Study of Tivozanib in Subjects With Advanced Renal Cell Carcinoma |
| NCT01478594 | PHASE2 | COMPLETED | A Study Combining mFOLFOX6 With Tivozanib or Bevacizumab in Patients With Metastatic Colorectal Cancer as First Line Therapy |
| NCT01673386 | PHASE2 | TERMINATED | A Subject Treatment Preference Study of Tivozanib Versus Sunitinib in Subjects With Metastatic RCC |
| NCT01728181 | PHASE1/PHASE2 | WITHDRAWN | 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 |
| NCT01782313 | PHASE2 | COMPLETED | A Phase II Study of Tivozanib in Patients With Metastatic and Non-resectable Soft Tissue Sarcomas |
| NCT01807156 | PHASE2 | TERMINATED | Phase II Trial of Tivozanib in Advanced Hepatocellular Cancer |
| NCT01834183 | PHASE2 | WITHDRAWN | Tivozanib + Gemcitabine in Metastatic RCC |
| NCT01835223 | PHASE1/PHASE2 | COMPLETED | Tivozanib in Treating Patients With Liver Cancer That Is Metastatic or Cannot Be Removed by Surgery |
| NCT01846871 | PHASE2 | COMPLETED | Tivozanib for Recurrent Glioblastoma |
| NCT01853644 | PHASE2 | COMPLETED | Tivozanib in Recurrent, Platinum-Resistant Ovarian, Fallopian Tube or Primary Peritoneal Cancer |
| NCT01885949 | PHASE2 | TERMINATED | Tivozanib + Enzalutamide in Adv Prostate Cancer |
| NCT01972516 | PHASE2 | TERMINATED | Tivozanib As Maintenance Therapy In GYN |
| NCT03136627 | PHASE1/PHASE2 | COMPLETED | Phase 1/2 Study of Tivozanib in Combination With Nivolumab in Subjects With RCC |
| NCT03970616 | PHASE1/PHASE2 | TERMINATED | A Study of Tivozanib in Combination With Durvalumab in Subjects With Advanced Hepatocellular Carcinoma |
| NCT05000294 | PHASE1/PHASE2 | SUSPENDED | Atezolizumab Plus Tivozanib in Immunologically Cold Tumor Types |
| NCT00563147 | PHASE1 | COMPLETED | 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 |
| NCT00660153 | PHASE1 | COMPLETED | Study of Tivozanib (AV-951) Plus FOLFOX6 in Subjects With Advanced Colorectal Cancer and Other Gastrointestinal Cancers |
| NCT00717340 | PHASE1 | COMPLETED | 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 |
| NCT00826878 | PHASE1 | COMPLETED | An Open-Label Study of QD Oral Administration of Tivozanib (AV-951) in Subjects With Non-Small Cell Lung Cancer (NSCLC) |
| NCT00970411 | PHASE1 | COMPLETED | Study of KRN951 in Patients With Solid Tumors |
| NCT01210846 | PHASE1 | COMPLETED | A Cardiac Safety Study of Tivozanib to Evaluate the Electrocardiogram and Pharmacokinetic-Electrocardiogram Dynamics in Subjects With Advanced Solid Tumors |
| NCT01306630 | PHASE1 | COMPLETED | A Trial of Tivozanib (AV-951) in Combination With Capecitabine (Xeloda®) in Subjects With Advanced Solid Tumors |
| NCT01316848 | PHASE1 | COMPLETED | A Single Center, Open-label, Randomized, Two-period Crossover Food Effect Study of Single Doses of Tivozanib (AV-951) in Healthy Subjects |
| NCT01363778 | PHASE1 | COMPLETED | A Phase 1 Study to Evaluate The Effect of Ketoconazole on the Pharmacokinetics of Tivozanib in Healthy Subjects |
| NCT01363804 | PHASE1 | COMPLETED | A Phase 1 Study to Evaluate the Effect of Rifampin on the Pharmacokinetics of Tivozanib in Healthy Subjects |
| NCT01369433 | Not specified | TERMINATED | A Rollover Protocol to Allow Continued Access to Tivozanib (AV 951) for Subjects Enrolled in Other Tivozanib Protocols |
| NCT01769885 | Not specified | WITHDRAWN | Tivozanib Before Surgery in Treating Patients With Localized Kidney Cancer |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
174 molecules share ≥1 primary target. Top 100 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | FLT1, FLT4, KDR |
| Gefitinib | ChEMBL + PubChem | Phase 4 (approved) | FLT1, FLT4, KDR |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | FLT1, FLT4, KDR |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | FLT1, FLT4, KDR |
| AXITINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| FRUQUINTINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| LENVATINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| NINTEDANIB ESYLATE | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| QUIZARTINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| SORAFENIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| SUNITINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| VANDETANIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR |
| BRIVANIB | ChEMBL | Phase 3 | FLT1, FLT4, KDR |
| CEDIRANIB | ChEMBL | Phase 3 | FLT1, FLT4, KDR |
| CEP-1347 | ChEMBL | Phase 3 | FLT1, FLT4, KDR |
| DOVITINIB | ChEMBL | Phase 3 | FLT1, FLT4, KDR |
| LESTAURTINIB | ChEMBL | Phase 3 | FLT1, FLT4, KDR |
| LINIFANIB | ChEMBL | Phase 3 | FLT1, FLT4, KDR |
| MOTESANIB | ChEMBL | Phase 3 | FLT1, FLT4, KDR |
| SEMAXANIB | ChEMBL | Phase 3 | FLT1, FLT4, KDR |
| SURUFATINIB | ChEMBL | Phase 3 | FLT1, FLT4, KDR |
| VATALANIB | ChEMBL | Phase 3 | FLT1, FLT4, KDR |
| AT-9283 | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| BFH-772 | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| CENISERTIB | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| DORAMAPIMOD | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| FORETINIB | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| ILORASERTIB | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| LUCITANIB | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| MK-2461 | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| OSI-632 | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| R-406 | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| RAF-265 | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| REBASTINIB | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| SU-014813 | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| TANDUTINIB | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| TOZASERTIB | ChEMBL | Phase 2 | FLT1, FLT4, KDR |
| Afatinib | PubChem | Approved | FLT1, FLT4, KDR |
| Selumetinib | PubChem | Approved | FLT1, FLT4, KDR |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | FLT4, KDR |
| DASATINIB | ChEMBL | Phase 4 (approved) | FLT1, KDR |
| FILGOTINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4 |
| PEXIDARTINIB | ChEMBL | Phase 4 (approved) | FLT1, KDR |
| PONATINIB | ChEMBL | Phase 4 (approved) | FLT1, KDR |
| ALISERTIB | ChEMBL | Phase 3 | FLT1, KDR |
| CANERTINIB | ChEMBL | Phase 3 | FLT1, KDR |
| DEFACTINIB | ChEMBL | Phase 3 | FLT1, KDR |
| ORANTINIB | ChEMBL | Phase 3 | FLT1, KDR |
| AEE-788 | ChEMBL | Phase 2 | FLT1, KDR |
| CEP-11981 | ChEMBL | Phase 2 | FLT1, KDR |
| CEP-32496 | ChEMBL | Phase 2 | FLT1, KDR |
| DANUSERTIB | ChEMBL | Phase 2 | FLT4, KDR |
| ELLAGIC ACID | ChEMBL | Phase 2 | FLT4, KDR |
| SOTRASTAURIN | ChEMBL | Phase 2 | FLT4, KDR |
| TAK-715 | ChEMBL | Phase 2 | FLT4, KDR |
| TELATINIB | ChEMBL | Phase 2 | FLT4, KDR |
| Idelalisib | PubChem | Approved | FLT1, FLT4 |
| GENTIAN VIOLET | ChEMBL + PubChem | Phase 4 (approved) | KDR |
| ABEMACICLIB | ChEMBL | Phase 4 (approved) | KDR |
| ABROCITINIB | ChEMBL | Phase 4 (approved) | KDR |
| ACALABRUTINIB | ChEMBL | Phase 4 (approved) | KDR |
| ALECTINIB | ChEMBL | Phase 4 (approved) | KDR |
| AUROTHIOGLUCOSE | ChEMBL | Phase 4 (approved) | KDR |
| CABOZANTINIB S-MALATE | ChEMBL | Phase 4 (approved) | KDR |
| CERITINIB | ChEMBL | Phase 4 (approved) | KDR |
| ENASIDENIB | ChEMBL | Phase 4 (approved) | KDR |
| ERDAFITINIB | ChEMBL | Phase 4 (approved) | KDR |
| ESTRAMUSTINE | ChEMBL | Phase 4 (approved) | KDR |
| FOSTAMATINIB DISODIUM | ChEMBL | Phase 4 (approved) | KDR |
| FUTIBATINIB | ChEMBL | Phase 4 (approved) | KDR |
| GLAFENINE | ChEMBL | Phase 4 (approved) | KDR |
| HEXACHLOROPHENE | ChEMBL | Phase 4 (approved) | KDR |
| IBRUTINIB | ChEMBL | Phase 4 (approved) | KDR |
| IMATINIB | ChEMBL | Phase 4 (approved) | KDR |
| INDIGOTINDISULFONATE | ChEMBL | Phase 4 (approved) | KDR |
| ISOXICAM | ChEMBL | Phase 4 (approved) | KDR |
| MEBENDAZOLE | ChEMBL | Phase 4 (approved) | KDR |
| MESALAMINE | ChEMBL | Phase 4 (approved) | KDR |
| NERATINIB | ChEMBL | Phase 4 (approved) | KDR |
| NICLOSAMIDE | ChEMBL | Phase 4 (approved) | KDR |
| NOVOBIOCIN | ChEMBL | Phase 4 (approved) | KDR |
| OLMUTINIB | ChEMBL | Phase 4 (approved) | KDR |
| OLSALAZINE | ChEMBL | Phase 4 (approved) | KDR |
| OSIMERTINIB | ChEMBL | Phase 4 (approved) | KDR |
| PHENYL AMINOSALICYLATE | ChEMBL | Phase 4 (approved) | KDR |
| PIPERAZINE | ChEMBL | Phase 4 (approved) | KDR |
| SELPERCATINIB | ChEMBL | Phase 4 (approved) | KDR |
| SORAFENIB TOSYLATE | ChEMBL | Phase 4 (approved) | KDR |
| STIRIPENTOL | ChEMBL | Phase 4 (approved) | KDR |
| SUNITINIB MALATE | ChEMBL | Phase 4 (approved) | KDR |
| TOFACITINIB | ChEMBL | Phase 4 (approved) | KDR |
| UPADACITINIB | ChEMBL | Phase 4 (approved) | KDR |
Related Atlas pages
- Genes: FLT1, KDR, FLT4
- Indicated for: neoplasm, renal cell carcinoma, renal cell adenocarcinoma
- In clinical trials for: hepatocellular carcinoma, glioblastoma, soft tissue sarcoma, fallopian tube neoplasm, ovarian cancer, colorectal neoplasm
- Drugs: Crizotinib, Gefitinib, Pazopanib, Regorafenib, Axitinib, Cabozantinib, Entrectinib, Erlotinib, Fedratinib, Fruquintinib, Infigratinib, Lenvatinib, Midostaurin, Nintedanib, Quizartinib, Sorafenib, Sunitinib, Vandetanib, Brivanib, Cediranib, CEP-1347, Dovitinib, Lestaurtinib, Linifanib, Motesanib, Semaxanib, Surufatinib, Vatalanib, Afatinib, Selumetinib, Brigatinib, Dasatinib, Filgotinib, Pexidartinib, Ponatinib, Alisertib, Canertinib, Defactinib, Orantinib, Idelalisib, Abemaciclib, Abrocitinib, Acalabrutinib, Alectinib, Aurothioglucose, Ceritinib, Enasidenib, Erdafitinib, Estramustine, Futibatinib, Glafenine, Hexachlorophene, Ibrutinib, Imatinib, Isoxicam, Mebendazole, Mesalamine, Neratinib, Niclosamide, Novobiocin, Olmutinib, Olsalazine, Osimertinib, Phenyl Aminosalicylate, Piperazine, Selpercatinib, Stiripentol, Tofacitinib, Upadacitinib