Pazopanib
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Also known as GW-786034GW786034NSC-752782VotrientSID103905642SID124899319SID144206725SID170465625Pazopanib hydrochlorideÊPazopanib hydrochlorideÂ
Summary
Pazopanib (CHEMBL477772) is an approved small-molecule antineoplastic agent (ATC L01EX03) targeting PDGFRB, KIT, and CSF1R; indicated across 52 conditions including neoplasm and renal cell carcinoma.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EX03
- Targets: 7 (PDGFRB, KIT, CSF1R…)
- Indications: 52 conditions
- Clinical trials: 201
- Chemistry: 437.5 Da · C21H23N7O2S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL477772 |
| Name | Pazopanib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 10113978 |
| ChEBI | CHEBI:71219 |
| ATC | L01EX03 |
| Molecular formula | C21H23N7O2S |
| Molecular weight | 437.5 |
| InChIKey | CUIHSIWYWATEQL-UHFFFAOYSA-N |
SMILES: CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N
IUPAC name: 5-[[4-[(2,3-dimethylindazol-6-yl)-methylamino]pyrimidin-2-yl]amino]-2-methylbenzenesulfonamide
ChEBI definition: A pyrimidine that is 5-(pyrimidin-2-yl}amino-2-methylbenzenesulfonamide substituted at position 4 by a (2,3-dimethylindazol-6-yl)(methyl)amino group. Used as its hydrochloride salt for treatment of kidney cancer.
Pharmacological roles (ChEBI): antineoplastic agent, tyrosine kinase inhibitor, vascular endothelial growth factor receptor antagonist, angiogenesis modulating agent.
Also known as: GW-786034, GW786034, NSC-752782, Pazopanib, Votrient, pazopanib, SID103905642, SID124899319, SID144206725, SID170465625, PAZOPANIB, Pazopanib hydrochlorideÊ
Parent form; salt/anhydrous children: CHEMBL1201733
Patent coverage: 6,092 distinct patent families (15,540 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 15,403 (99%) 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 |
|---|---|---|---|---|---|
| PDGFRB | platelet derived growth factor receptor beta | Inhibition | 7.08 | 2.3% | P09619 |
| KIT | KIT proto-oncogene, receptor tyrosine kinase | Inhibition | 6.85 | 0.5% | P10721 |
| CSF1R | colony stimulating factor 1 receptor | Inhibition | 6.84 | 0% | P07333 |
| FGFR1 | fibroblast growth factor receptor 1 | Inhibition | 7.13 | 11.5% | P11362 |
| FLT1 | fms related receptor tyrosine kinase 1 | Inhibition | 8 | 0.1% | P17948 |
| KDR | kinase insert domain receptor | Inhibition | 7.52 | 1.1% | P35968 |
| FLT4 | fms related receptor tyrosine kinase 4 | Inhibition | 7.33 | 0.2% | P35916 |
Broader ChEMBL bioactivity targets: 120 (assay-derived). Sample: Serine/threonine-protein kinase TAO2, ATP-binding cassette sub-family C member 4, Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma, Receptor-interacting serine/threonine-protein kinase 3, Tyrosine-protein kinase Fyn, Macrophage colony-stimulating factor 1 receptor, Tyrosine-protein kinase ABL1, Vascular endothelial growth factor receptor 1, RAF proto-oncogene serine/threonine-protein kinase, Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma.
Bioactivity
ChEMBL activities: 309 potent at pChembl ≥ 5 of 314 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| CA12 | 9.05 | Ki | 0.9 | nM | CHEMBL_ACT_25998291 |
| KIT | 8.74 | Kd | 1.8 | nM | CHEMBL_ACT_7596447 |
| PDGFRB | 8.7 | Kd | 2 | nM | CHEMBL_ACT_2899080 |
| PDGFRB | 8.7 | Kd | 2 | nM | CHEMBL_ACT_7596533 |
| KIT | 8.64 | Kd | 2.3 | nM | CHEMBL_ACT_2897038 |
| KIT | 8.64 | Kd | 2.3 | nM | CHEMBL_ACT_7596448 |
| KIT | 8.55 | Kd | 2.8 | nM | CHEMBL_ACT_2895938 |
| KIT | 8.55 | Kd | 2.8 | nM | CHEMBL_ACT_6220451 |
| KIT | 8.55 | Kd | 2.8 | nM | CHEMBL_ACT_7596443 |
| KDR | 8.5 | Ki | 3.16 | nM | CHEMBL_ACT_9630097 |
| PDGFRB | 8.4 | Ki | 3.98 | nM | CHEMBL_ACT_9588166 |
| PDGFRA | 8.31 | Kd | 4.9 | nM | CHEMBL_ACT_2899042 |
| PDGFRA | 8.31 | Kd | 4.9 | nM | CHEMBL_ACT_7598232 |
| KDR | 8.3 | IC50 | 5.01 | nM | CHEMBL_ACT_13418835 |
| KIT | 8.19 | Kd | 6.5 | nM | CHEMBL_ACT_2896962 |
| KIT | 8.19 | Kd | 6.5 | nM | CHEMBL_ACT_7596449 |
| KDR | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_2561556 |
| CSF1R | 8.1 | Kd | 7.9 | nM | CHEMBL_ACT_2902387 |
| CSF1R | 8.1 | Kd | 7.9 | nM | CHEMBL_ACT_7598193 |
| CA9 | 8.04 | Ki | 9.1 | nM | CHEMBL_ACT_23184223 |
| CA9 | 8.04 | Ki | 9.1 | nM | CHEMBL_ACT_25998267 |
| FLT1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_18854172 |
| FLT1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_23289736 |
| FLT1 | 8 | IC50 | 10 | nM | CHEMBL_ACT_2561549 |
| CA1 | 7.92 | Ki | 12.1 | nM | CHEMBL_ACT_25998223 |
| KDR | 7.85 | Kd | 14 | nM | CHEMBL_ACT_2891412 |
| FLT1 | 7.85 | Kd | 14 | nM | CHEMBL_ACT_2907356 |
| FLT1 | 7.85 | Kd | 14 | nM | CHEMBL_ACT_7596511 |
| KDR | 7.85 | Kd | 14 | nM | CHEMBL_ACT_7596518 |
| FLT1 | 7.8 | Ki | 15.85 | nM | CHEMBL_ACT_9661388 |
Target pathways
Aggregated over 7 target gene(s): PDGFRB, KIT, CSF1R, FGFR1, FLT1, KDR, FLT4.
Top Reactome pathways
70 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| PIP3 activates AKT signaling | 3 | FGFR1, KIT, PDGFRB |
| VEGF binds to VEGFR leading to receptor dimerization | 3 | FLT1, FLT4, KDR |
| Constitutive Signaling by Aberrant PI3K in Cancer | 3 | FGFR1, KIT, PDGFRB |
| RAF/MAP kinase cascade | 3 | FGFR1, KIT, PDGFRB |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 3 | FGFR1, KIT, PDGFRB |
| 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 |
| PI3K Cascade | 1 | FGFR1 |
| Developmental Biology | 1 | KIT |
| Signaling by SCF-KIT | 1 | KIT |
| Regulation of KIT signaling | 1 | KIT |
| Signal Transduction | 1 | KIT |
| Disease | 1 | KIT |
| Signaling by FGFR1 amplification mutants | 1 | FGFR1 |
| Signaling by activated point mutants of FGFR1 | 1 | FGFR1 |
| Downstream signal transduction | 1 | PDGFRB |
| Signaling by PDGF | 1 | PDGFRB |
| FGFR1b ligand binding and activation | 1 | FGFR1 |
| FGFR1c ligand binding and activation | 1 | FGFR1 |
| FGFR1c and Klotho ligand binding and activation | 1 | FGFR1 |
| Negative regulation of the PI3K/AKT network | 1 | KIT |
| Generic Transcription Pathway | 1 | KIT |
| Integrin cell surface interactions | 1 | KDR |
| PI3K/AKT Signaling in Cancer | 1 | KIT |
| NCAM signaling for neurite out-growth | 1 | FGFR1 |
| VEGFA-VEGFR2 Pathway | 1 | KDR |
| Signal transduction by L1 | 1 | FGFR1 |
| Other interleukin signaling | 1 | CSF1R |
| VEGFR2 mediated cell proliferation | 1 | KDR |
| Phospholipase C-mediated cascade: FGFR1 | 1 | FGFR1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| positive regulation of cell population proliferation | 7 |
| protein autophosphorylation | 7 |
| protein phosphorylation | 7 |
| cell migration | 7 |
| cell surface receptor protein tyrosine kinase signaling pathway | 6 |
| peptidyl-tyrosine phosphorylation | 6 |
| positive regulation of cell migration | 6 |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 6 |
| angiogenesis | 5 |
| positive regulation of MAPK cascade | 5 |
| positive regulation of ERK1 and ERK2 cascade | 4 |
| signal transduction | 3 |
| positive regulation of MAP kinase activity | 3 |
| chemotaxis | 3 |
| regulation of cell shape | 3 |
Indications & clinical
Indications
52 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| neoplasm | 3 | MONDO:0005070 | EFO:0000616 |
| renal cell carcinoma | 3 | MONDO:0005086 | EFO:0000681 |
| sarcoma | 3 | MONDO:0005089 | EFO:0000691 |
| ovarian neoplasm | 3 | MONDO:0021068 | EFO:0003893 |
| clear cell renal carcinoma | 3 | MONDO:0005005 | EFO:0000349 |
| soft tissue sarcoma | 3 | MONDO:0018078 | EFO:1001968 |
| ovarian cancer | 3 | MONDO:0008170 | MONDO:0008170 |
| leiomyosarcoma | 2 | MONDO:0005058 | EFO:0000564 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| liposarcoma | 2 | MONDO:0005060 | EFO:0000569 |
| prostate adenocarcinoma | 2 | MONDO:0005082 | EFO:0000673 |
| osteosarcoma | 2 | MONDO:0009807 | EFO:0000637 |
| small cell lung carcinoma | 2 | MONDO:0008433 | EFO:0000702 |
| germ cell tumor | 2 | MONDO:0005040 | EFO:0000514 |
| head and neck squamous cell carcinoma | 2 | MONDO:0010150 | EFO:0000181 |
| chondrosarcoma | 2 | MONDO:0008977 | EFO:0000333 |
| breast neoplasm | 2 | MONDO:0021100 | EFO:0003869 |
| thyroid gland carcinoma | 2 | MONDO:0015075 | EFO:0002892 |
| acute myeloid leukemia | 2 | MONDO:0018874 | EFO:0000222 |
| melanoma | 2 | MONDO:0005105 | EFO:0000756 |
| exocrine pancreatic carcinoma | 2 | MONDO:0005192 | EFO:0002618 |
| angiosarcoma | 2 | MONDO:0016982 | EFO:0003968 |
| alveolar soft part sarcoma | 2 | MONDO:0011655 | EFO:0007143 |
| gliosarcoma | 2 | MONDO:0016681 | EFO:1001465 |
| neuroendocrine neoplasm | 2 | MONDO:0019496 | EFO:1001901 |
| macular degeneration | 2 | MONDO:0003004 | EFO:0009606 |
| salivary gland cancer | 2 | MONDO:0004669 | MONDO:0000521 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| peritoneal neoplasm | 2 | MONDO:0006901 | MONDO:0002087 |
| fallopian tube neoplasm | 2 | MONDO:0021092 | MONDO:0002158 |
| kidney cancer | 2 | MONDO:0002367 | MONDO:0002367 |
| lung neoplasm | 2 | MONDO:0021117 | MONDO:0008903 |
| solitary fibrous tumor | 2 | MONDO:0016238 | MONDO:0016238 |
| gastrointestinal stromal tumor | 2 | MONDO:0011719 | MONDO:0011719 |
| dermatofibrosarcoma protuberans | 2 | MONDO:0011934 | MONDO:0011934 |
| hereditary hemorrhagic telangiectasia | 2 | MONDO:0019180 | MONDO:0019180 |
| lymphedema | 2 | MONDO:0019297 | MONDO:0019297 |
| kidney neoplasm | 2 | MONDO:0021163 | EFO:0003865 |
| central nervous system neoplasm | 2 | MONDO:0006130 | EFO:1000158 |
| paraganglioma | 2 | MONDO:0000448 | EFO:1000453 |
| colorectal adenocarcinoma | 1 | MONDO:0005008 | EFO:0000365 |
| glioblastoma | 1 | MONDO:0018177 | EFO:0000519 |
| hepatocellular carcinoma | 1 | MONDO:0007256 | EFO:0000182 |
| corneal neovascularization | 1 | MONDO:0006713 | EFO:1000880 |
| lymphoma | 1 | MONDO:0005062 | EFO:0000574 |
| psoriasis | 1 | MONDO:0005083 | EFO:0000676 |
6 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 201.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 98 |
| PHASE1 | 53 |
| PHASE1/PHASE2 | 16 |
| PHASE3 | 13 |
| Not specified | 11 |
| PHASE4 | 4 |
| PHASE2/PHASE3 | 4 |
| EARLY_PHASE1 | 2 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01205230 | PHASE4 | COMPLETED | VEG113971: An Open-Label Study of the Effects of Ketoconazole or Esomeprazole on Pazopanib PK |
| NCT01521715 | PHASE4 | COMPLETED | First Line Pazopanib in Poor Risk Patients With Metastatic Renal Cell Carcinoma |
| NCT02555748 | PHASE4 | COMPLETED | Therapeutic Drug Monitoring of Sunitinib and Pazopanib in Advanced or Metastatic Renal Cell Carcinoma |
| NCT05949424 | PHASE4 | UNKNOWN | OPTI - DOSE: Optimal Dosing of Oral Anticancer Drugs in Older Adults |
| NCT02180867 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | Radiation Therapy With or Without Combination Chemotherapy or Pazopanib Before Surgery in Treating Patients With Newly Diagnosed Non-rhabdomyosarcoma Soft Tissue Sarcomas That Can Be Removed by Surgery |
| NCT03592472 | PHASE3 | RECRUITING | A Study of Pazopanib With or Without Abexinostat in Patients With Locally Advanced or Metastatic Renal Cell Carcinoma (RENAVIV) |
| NCT03850964 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | Effects of Pazopanib on Hereditary Hemorrhagic Telangiectasia Related Epistaxis and Anemia (Paz) |
| NCT05432791 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | Testing Olaparib and Temozolomide Versus the Usual Treatment for Uterine Leiomyosarcoma After Chemotherapy Has Stopped Working |
| NCT06263231 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Investigate Efficacy & Safety of Intratumoral INT230-6 Compared to US Standard of Care in Adults With Soft Tissue Sarcomas (INVINCIBLE-3) |
| NCT06726421 | PHASE3 | RECRUITING | Systemic Therapy Alone or With Stereotactic Body Radiotherapy for Oligometastatic Kidney Cancer (STROKER Study) |
| NCT00334282 | PHASE3 | COMPLETED | Safety and Efficacy of GW786034 (Pazopanib) In Metastatic Renal Cell Carcinoma |
| NCT00387764 | PHASE3 | COMPLETED | Extension Study to VEG105192 to Assess Pazopanib in Patients With Advanced/Metastatic Renal Cell Cancer |
| NCT00720941 | PHASE3 | COMPLETED | Pazopanib Versus Sunitinib in the Treatment of Locally Advanced and/or Metastatic Renal Cell Carcinoma |
| NCT00753688 | PHASE3 | COMPLETED | Pazopanib Versus Placebo in Patients With Soft Tissue Sarcoma Whose Disease Has Progressed During or Following Prior Therapy |
| NCT00775307 | PHASE2/PHASE3 | COMPLETED | Adjuvant Pazopanib in Stage I NSCLC |
| NCT00866697 | PHASE3 | COMPLETED | Efficacy and Safety of Pazopanib Monotherapy After First Line Chemotherapy in Ovarian, Fallopian Tube, or Primary Peritoneal Cancer |
| NCT01064310 | PHASE3 | COMPLETED | Patient Preference Study of Pazopanib Versus Sunitinib in Advanced or Metastatic Kidney Cancer |
| NCT01235962 | PHASE3 | COMPLETED | A Study to Evaluate Pazopanib as an Adjuvant Treatment for Localized Renal Cell Carcinoma (RCC) |
| NCT01613846 | PHASE3 | COMPLETED | Phase III Sequential Open-label Study to Evaluate the Efficacy and Safety of Sorafenib Followed by Pazopanib Versus Pazopanib Followed by Sorafenib in the Treatment of Advanced / Metastatic Renal Cell Carcinoma (SWITCH-II) |
| NCT02979899 | PHASE3 | COMPLETED | Trial of TRC105 and Pazopanib Versus Pazopanib Alone in Patients With Advanced Angiosarcoma |
| NCT03260894 | PHASE3 | COMPLETED | Pembrolizumab (MK-3475) Plus Epacadostat vs Standard of Care in mRCC (KEYNOTE-679/ECHO-302) |
| NCT01217931 | PHASE2 | ACTIVE_NOT_RECRUITING | Sequential Two-agent Assessment in Renal Cell Carcinoma Therapy: The START Trial |
| NCT02203760 | PHASE2 | ACTIVE_NOT_RECRUITING | Pazopanib Vs. Pazopanib Plus Gemcitabine |
| NCT02331498 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Phase I/II Study of Pazopanib+ Temozolomide in Patients With Newly Diagnosed Glioblastoma Multiforme |
| NCT05180695 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | HDM201 and Pazopanib in Patients With P53 Wild-type Advanced/Metastatic Soft Tissue Sarcomas |
| NCT05679921 | PHASE2 | RECRUITING | Pazopanib With or Without Pembrolizumab for Metastatic Soft Tissue Sarcoma |
| NCT06239272 | PHASE1/PHASE2 | RECRUITING | NRSTS2021, A Risk Adapted Study Evaluating Maintenance Pazopanib, Limited Margin, Dose-Escalated Radiation Therapy and Selinexor in Non-Rhabdomyosarcoma Soft Tissue Sarcoma (NRSTS) |
| NCT06739395 | PHASE2 | RECRUITING | Precision Medicine Trial Based on Molecular Matching Therapy for Patients With Standard Treatment Exhaustion |
| NCT06816771 | PHASE2 | RECRUITING | Evaluation of the Efficacy and Safety of Pazopanib in Combination with TGI/CIV for Recurrent or Refractory Rhabdomyosarcoma in Children or Adolescents |
| NCT06895733 | PHASE1/PHASE2 | RECRUITING | Study of Pazopanib Combined With Palbociclib for Refractory Solid Tumors With Co-amplified in the 11q13(FGF3/4/19/CCND1) |
| NCT07087158 | PHASE2 | NOT_YET_RECRUITING | A Study of IBR854 Combined With Pazopanib Versus Pazopanib in Advanced Renal Cell Carcinoma |
| NCT00244764 | PHASE2 | COMPLETED | GW786034 In Subjects With Locally Recurrent Or Metastatic Clear Cell Renal Cell Carcinoma |
| NCT00256880 | PHASE2 | COMPLETED | Pazopanib (GW786034) In Subjects With Relapsed Or Refractory Multiple Myeloma |
| NCT00281632 | PHASE2 | COMPLETED | A Phase II, Open-Label Study Evaluating the Effect Of GW786034 In Subjects With Ovarian Cancer |
| NCT00297258 | PHASE2 | COMPLETED | Pazopanib In Patients With Relapsed Or Refractory Soft Tissue Sarcoma |
| NCT00347919 | PHASE2 | COMPLETED | Pazopanib Plus Lapatinib Compared To Lapatinib Alone In Subjects With Advanced Or Metastatic Breast Cancer |
| NCT00350727 | PHASE2 | COMPLETED | Pazopanib In Combination With Lapatinib In Adult Patients With Relapsed Malignant Glioma |
| NCT00367679 | PHASE2 | COMPLETED | Pazopanib As Pre-Surgical Therapy In Treatment-Naive Subjects With Non-Small Cell Lung Cancer |
| NCT00430781 | PHASE2 | COMPLETED | Pazopanib Plus Lapatinib Compared to Lapatinib Alone and Pazopanib Alone In Subjects With Metastatic Cervical Cancer |
| NCT00549328 | PHASE2 | TERMINATED | Monotherapy Pazopanib in Subjects With Advanced Non-Small Cell Lung 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.
235 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| Crizotinib | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| AXITINIB | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| SORAFENIB | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| SUNITINIB | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| VANDETANIB | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| BRIVANIB | ChEMBL | Phase 3 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| CEDIRANIB | ChEMBL | Phase 3 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| DOVITINIB | ChEMBL | Phase 3 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| LESTAURTINIB | ChEMBL | Phase 3 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| LINIFANIB | ChEMBL | Phase 3 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| MOTESANIB | ChEMBL | Phase 3 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| SEMAXANIB | ChEMBL | Phase 3 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| CENISERTIB | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| DORAMAPIMOD | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| FORETINIB | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| ILORASERTIB | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| R-406 | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| RAF-265 | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| SU-014813 | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| TANDUTINIB | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| TOZASERTIB | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| Afatinib | PubChem | Approved | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| Selumetinib | PubChem | Approved | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| GEFITINIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT |
| DASATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FLT1, KDR, KIT, PDGFRB |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT |
| LENVATINIB | ChEMBL | Phase 4 (approved) | FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| PONATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FLT1, KDR, KIT, PDGFRB |
| QUIZARTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT4, KDR, KIT, PDGFRB |
| TIVOZANIB | ChEMBL | Phase 4 (approved) | FGFR1, FLT1, FLT4, KDR, KIT, PDGFRB |
| VATALANIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT4, KDR, KIT, PDGFRB |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | CSF1R, FLT1, FLT4, KDR, KIT, PDGFRB |
| REBASTINIB | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT1, FLT4, KDR, KIT |
| Idelalisib | PubChem | Approved | CSF1R, FGFR1, FLT1, FLT4, KIT, PDGFRB |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FLT4, KDR, KIT |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | FGFR1, FLT1, FLT4, KDR, KIT |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR, KIT, PDGFRB |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | FGFR1, FLT1, FLT4, KDR, KIT |
| NINTEDANIB ESYLATE | ChEMBL | Phase 4 (approved) | FGFR1, FLT1, FLT4, KDR, PDGFRB |
| PEXIDARTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, KDR, KIT, PDGFRB |
| BFH-772 | ChEMBL | Phase 2 | FLT1, FLT4, KDR, KIT, PDGFRB |
| CEP-32496 | ChEMBL | Phase 2 | CSF1R, FLT1, KDR, KIT, PDGFRB |
| LUCITANIB | ChEMBL | Phase 2 | FGFR1, FLT1, FLT4, KDR, PDGFRB |
| MK-2461 | ChEMBL | Phase 2 | FGFR1, FLT1, FLT4, KDR, PDGFRB |
| OSI-632 | ChEMBL | Phase 2 | FGFR1, FLT1, FLT4, KDR, PDGFRB |
| IMATINIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, KDR, KIT, PDGFRB |
| CANERTINIB | ChEMBL | Phase 3 | FLT1, KDR, KIT, PDGFRB |
| ENZASTAURIN | ChEMBL | Phase 3 | FGFR1, FLT4, KIT, PDGFRB |
| ORANTINIB | ChEMBL | Phase 3 | FGFR1, FLT1, KDR, PDGFRB |
| SURUFATINIB | ChEMBL | Phase 3 | FGFR1, FLT1, FLT4, KDR |
| AT-9283 | ChEMBL | Phase 2 | FGFR1, FLT1, FLT4, KDR |
| CEP-11981 | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT1, KDR |
| DANUSERTIB | ChEMBL | Phase 2 | FGFR1, FLT4, KDR, KIT |
| ENMD-2076 | ChEMBL | Phase 2 | CSF1R, FGFR1, KDR, KIT |
| MILCICLIB | ChEMBL | Phase 2 | FGFR1, FLT4, KIT, PDGFRB |
| TELATINIB | ChEMBL | Phase 2 | FLT4, KDR, KIT, PDGFRB |
Related Atlas pages
- Genes: PDGFRB, KIT, CSF1R, FGFR1, FLT1, KDR, FLT4
- Diseases: neoplasm, renal cell carcinoma, sarcoma, ovarian neoplasm, clear cell renal carcinoma, soft tissue sarcoma, ovarian cancer
- Drugs: Crizotinib, Regorafenib, Axitinib, Fedratinib, Midostaurin, Nintedanib, Sorafenib, Sunitinib, Vandetanib, Brivanib, Cediranib, Dovitinib, Lestaurtinib, Linifanib, Motesanib, Semaxanib, Afatinib, Selumetinib, Gefitinib, Dasatinib, Entrectinib, Lenvatinib, Ponatinib, Quizartinib, Tivozanib, Vatalanib, Idelalisib, Brigatinib, Cabozantinib, Erlotinib, Infigratinib, Pexidartinib, Imatinib, Canertinib, Enzastaurin, Orantinib, Surufatinib
- Biomarker genes: EPAS1, FGFR2, FGFR3, HIF1A, TP53, VHL