Linifanib
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Also known as A-741439ABT-869AL-39324RG-3635SID103904340SID137275904LINIFANIB (ABT-869)LinifanibÊLinifanibÂ
Summary
Linifanib (CHEMBL223360) is a phase-3 clinical-stage small-molecule antineoplastic agent targeting PDGFRB, KIT, and CSF1R; indicated across 10 conditions including hepatocellular carcinoma and renal cell carcinoma; with CIViC clinical evidence for 4 variant-indication associations (e.g. FLT3 D593del in cancer).
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 11 (PDGFRB, KIT, CSF1R…)
- Indications: 10 conditions
- Clinical trials: 19
- Precision-oncology evidence (CIViC): 4 variant–indication associations
- Chemistry: 375.4 Da · C21H18FN5O
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL223360 |
| Name | Linifanib |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 11485656 |
| ChEBI | CHEBI:91435 |
| Molecular formula | C21H18FN5O |
| Molecular weight | 375.4 |
| InChIKey | MPVGZUGXCQEXTM-UHFFFAOYSA-N |
SMILES: CC1=CC(=C(C=C1)F)NC(=O)NC2=CC=C(C=C2)C3=C4C(=CC=C3)NN=C4N
IUPAC name: 1-[4-(3-amino-1H-indazol-4-yl)phenyl]-3-(2-fluoro-5-methylphenyl)urea
ChEBI definition: A member of the class of phenylureas that is urea in which one of the nitrogens is substituted by a 2-fluoro-5-methylphenyl group, while the other is substituted by a p-(3-amino-1H-indazol-4-yl)phenyl group. It is a potent, selective inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptor tyrosine kinases.
Pharmacological roles (ChEBI): antineoplastic agent, EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, angiogenesis inhibitor.
Also known as: A-741439, ABT-869, AL-39324, Linifanib, RG-3635, SID103904340, LINIFANIB, SID137275904, LINIFANIB (ABT-869), LinifanibÊ, Linifanib (ABT-869), LinifanibÂ
Patent coverage: 1,533 distinct patent families (3,925 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 3,792 (97%) 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 | 7.18 | 2.3% | P09619 |
| KIT | KIT proto-oncogene, receptor tyrosine kinase | Inhibition | 7.85 | 0.5% | P10721 |
| CSF1R | colony stimulating factor 1 receptor | Inhibition | 8.52 | 0% | P07333 |
| FLT3 | fms related receptor tyrosine kinase 3 | Inhibition | 8.4 | 0.9% | P36888 |
| FLT1 | fms related receptor tyrosine kinase 1 | Inhibition | 8.52 | 0.1% | P17948 |
| KDR | kinase insert domain receptor | Inhibition | 8.4 | 1.1% | P35968 |
| FLT4 | fms related receptor tyrosine kinase 4 | Inhibition | 6.72 | 0.2% | P35916 |
| TEK | TEK receptor tyrosine kinase | Inhibition | 6.77 | 0% | Q02763 |
| CDK19 | cyclin dependent kinase 19 | Inhibition | 7.92 | 0.1% | Q9BWU1 |
| CDK8 | cyclin dependent kinase 8 | Inhibition | 8.16 | 6.5% | P49336 |
| RET | ret proto-oncogene | Inhibition | 5.72 | 0.4% | P07949 |
Broader ChEMBL bioactivity targets: 135 (assay-derived). Sample: Homeodomain-interacting protein kinase 4, Cyclin-dependent kinase 13, Macrophage colony-stimulating factor 1 receptor, Tyrosine-protein kinase ABL1, Protein deacetylase HDAC6, 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.
Bioactivity
ChEMBL activities: 311 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 |
|---|---|---|---|---|---|
| FLT3 | 9.2 | Kd | 0.63 | nM | CHEMBL_ACT_2907377 |
| FLT3 | 9.2 | Kd | 0.63 | nM | CHEMBL_ACT_7583484 |
| CDK8 | 9 | Ki | 1 | nM | CHEMBL_ACT_9644434 |
| FLT3 | 8.89 | Kd | 1.3 | nM | CHEMBL_ACT_7583488 |
| KIT | 8.77 | Kd | 1.7 | nM | CHEMBL_ACT_2897021 |
| KIT | 8.77 | Kd | 1.7 | nM | CHEMBL_ACT_7583337 |
| PDGFRB | 8.72 | Kd | 1.9 | nM | CHEMBL_ACT_2899063 |
| KIT | 8.72 | Kd | 1.9 | nM | CHEMBL_ACT_7583336 |
| PDGFRB | 8.72 | Kd | 1.9 | nM | CHEMBL_ACT_7583422 |
| KIT | 8.7 | Kd | 2 | nM | CHEMBL_ACT_2895921 |
| KIT | 8.7 | Kd | 2 | nM | CHEMBL_ACT_6220441 |
| KIT | 8.7 | Kd | 2 | nM | CHEMBL_ACT_7583332 |
| KDR | 8.64 | IC50 | 2.3 | nM | CHEMBL_ACT_14746904 |
| FLT3 | 8.59 | Kd | 2.6 | nM | CHEMBL_ACT_2890843 |
| FLT3 | 8.59 | Kd | 2.6 | nM | CHEMBL_ACT_7583489 |
| FLT3 | 8.57 | Kd | 2.7 | nM | CHEMBL_ACT_2907415 |
| FLT3 | 8.57 | Kd | 2.7 | nM | CHEMBL_ACT_7583485 |
| FLT1 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_1826430 |
| CSF1R | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_1826433 |
| FLT1 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_18568749 |
| CSF1R | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_18568752 |
| FLT1 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_26132432 |
| CSF1R | 8.47 | Kd | 3.4 | nM | CHEMBL_ACT_2902370 |
| CSF1R | 8.47 | Kd | 3.4 | nM | CHEMBL_ACT_7583545 |
| KIT | 8.42 | Kd | 3.8 | nM | CHEMBL_ACT_2896945 |
| KIT | 8.42 | Kd | 3.8 | nM | CHEMBL_ACT_7583338 |
| KDR | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_1826115 |
| KDR | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_1826380 |
| KDR | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_18568745 |
| FLT3 | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_18568746 |
Target pathways
Aggregated over 11 target gene(s): PDGFRB, KIT, CSF1R, FLT3, FLT1, KDR, FLT4, TEK, CDK19, CDK8, RET.
Top Reactome pathways
109 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| RAF/MAP kinase cascade | 5 | FLT3, KIT, PDGFRB, RET, TEK |
| PIP3 activates AKT signaling | 3 | FLT3, KIT, PDGFRB |
| Developmental Biology | 3 | CDK19, CDK8, KIT |
| Signal Transduction | 3 | CDK8, KIT, TEK |
| Disease | 3 | CDK19, CDK8, KIT |
| VEGF binds to VEGFR leading to receptor dimerization | 3 | FLT1, FLT4, KDR |
| Constitutive Signaling by Aberrant PI3K in Cancer | 3 | FLT3, KIT, PDGFRB |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 3 | FLT3, KIT, PDGFRB |
| Metabolism | 2 | CDK19, CDK8 |
| Neuropilin interactions with VEGF and VEGFR | 2 | FLT1, KDR |
| PPARA activates gene expression | 2 | CDK19, CDK8 |
| Generic Transcription Pathway | 2 | CDK8, KIT |
| Transcriptional regulation of white adipocyte differentiation | 2 | CDK19, CDK8 |
| Regulation of lipid metabolism by PPARalpha | 2 | CDK19, CDK8 |
| Metabolism of lipids | 2 | CDK19, CDK8 |
| Diseases of signal transduction by growth factor receptors and second messengers | 2 | CDK8, KIT |
| Infectious disease | 2 | CDK19, CDK8 |
| MAPK family signaling cascades | 2 | KIT, TEK |
| MAPK1/MAPK3 signaling | 2 | KIT, TEK |
| RNA Polymerase II Transcription | 2 | CDK8, KIT |
| Gene expression (Transcription) | 2 | CDK8, KIT |
| Respiratory Syncytial Virus Infection Pathway | 2 | CDK19, CDK8 |
| Viral Infection Pathways | 2 | CDK19, CDK8 |
| RSV-host interactions | 2 | CDK19, CDK8 |
| Adipogenesis | 2 | CDK19, CDK8 |
| High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells | 2 | FLT4, KDR |
| Hemostasis | 1 | TEK |
| PI3K Cascade | 1 | FLT3 |
| Signaling by SCF-KIT | 1 | KIT |
| Regulation of KIT signaling | 1 | KIT |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| protein phosphorylation | 11 |
| cell surface receptor protein tyrosine kinase signaling pathway | 9 |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 8 |
| positive regulation of cell population proliferation | 7 |
| positive regulation of cell migration | 7 |
| protein autophosphorylation | 7 |
| cell migration | 7 |
| positive regulation of MAPK cascade | 7 |
| peptidyl-tyrosine phosphorylation | 6 |
| angiogenesis | 5 |
| positive regulation of ERK1 and ERK2 cascade | 5 |
| hemopoiesis | 5 |
| signal transduction | 4 |
| negative regulation of apoptotic process | 4 |
| vascular endothelial growth factor signaling pathway | 4 |
Indications & clinical
Indications
10 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 |
|---|---|---|---|
| hepatocellular carcinoma | 3 | MONDO:0007256 | EFO:0000182 |
| renal cell carcinoma | 2 | MONDO:0005086 | EFO:0000681 |
| age-related macular degeneration | 2 | MONDO:0005150 | EFO:0001365 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| colorectal adenocarcinoma | 2 | MONDO:0005008 | EFO:0000365 |
| rectal cancer | 2 | MONDO:0006519 | EFO:1000657 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| colonic neoplasm | 2 | MONDO:0005401 | MONDO:0021063 |
| neoplasm | 1 | MONDO:0005070 | EFO:0000616 |
| endometriosis | 1 | MONDO:0005133 | EFO:0001065 |
Clinical trials
Total trials: 19.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 10 |
| PHASE2 | 7 |
| PHASE3 | 1 |
| PHASE1/PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01009593 | PHASE3 | TERMINATED | Efficacy and Tolerability of ABT-869 Versus Sorafenib in Advanced Hepatocellular Carcinoma (HCC) |
| NCT00486538 | PHASE2 | COMPLETED | Study of ABT-869 in Subjects With Advanced Renal Cell Carcinoma Who Have Previously Received Treatment With Sunitinib |
| NCT00517790 | PHASE2 | COMPLETED | Study of ABT-869 in Subjects With Advanced Non-small Cell Lung Cancer (NSCLC) |
| NCT00517920 | PHASE2 | COMPLETED | Phase 2 Study of ABT-869 in Advanced Hepatocellular Carcinoma (HCC) |
| NCT00645177 | PHASE2 | COMPLETED | Phase 2 Study of ABT-869 in Combination With Paclitaxel Versus Paclitaxel Alone to Treat Metastatic Breast Cancer |
| NCT00707889 | PHASE2 | COMPLETED | Phase 2 Study of ABT-869 in Combination With mFOLFOX6 Versus Bevacizumab in Combination With mFOLFOX6 to Treat Advanced Colorectal Cancer |
| NCT00716534 | PHASE2 | COMPLETED | Study of Carboplatin/Paclitaxel in Combination With ABT-869 in Subjects With Advanced or Metastatic Non-Small Cell Lung Cancer (NSCLC) |
| NCT01365910 | PHASE2 | TERMINATED | Linifanib in Treating Patients With Advanced, Refractory Colorectal Cancer |
| NCT03481842 | PHASE1/PHASE2 | WITHDRAWN | Safety, Tolerability and Efficacy of Vaginal Suppositories for Treatment of the Endometriosis |
| NCT00718380 | PHASE1 | COMPLETED | A Phase 1 Study of ABT-869 in Subjects With Solid Tumors |
| NCT00733187 | PHASE1 | COMPLETED | Pharmacokinetic Study To Evaluate Effect of Food and Diurnal Variation on ABT-869 |
| NCT00754104 | PHASE1 | WITHDRAWN | Study of ABT-869 in Combination With Tarceva in Subjects With Solid Tumors |
| NCT01114191 | PHASE1 | COMPLETED | A Study to Assess the Effect of Ketoconazole on the Pharmacokinetics of Linifanib (ABT-869) |
| NCT01225302 | PHASE1 | COMPLETED | A Study of Linifanib (ABT-869) in Combination With Carboplatin/Paclitaxel in Japanese Subjects With Non-Small Cell Lung Cancer (NSCLC) |
| NCT01286974 | PHASE1 | TERMINATED | A Pharmacokinetic Study to Access How the Body Absorbs and Removes Linifanib in Male Patients With Advanced Solid Tumors. |
| NCT01381341 | PHASE1 | COMPLETED | To Compare Relative Bioavailability of Two Clinical Formulations of Linifanib. |
| NCT01401933 | PHASE1 | COMPLETED | Effect of Rifampin on the Pharmacokinetics of Linifanib in Subjects With Advanced or Metastatic Solid Tumors |
| NCT01413893 | PHASE1 | COMPLETED | An Extension Study of Linifanib (ABT-869) in Subjects With Advanced or Metastatic Solid Tumors |
| NCT01506934 | PHASE1 | TERMINATED | A Study Evaluating the Bioavailability of Two Formulations of Linifanib and Food Effect on Pharmacokinetics of Linifanib in Subjects With Advanced or Metastatic Solid Tumors |
Clinical evidence (CIViC)
Variant × indication × effect (4 predictive associations from 4 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| FLT3 D593del | Cancer | Sensitivity/Response | Sorafenib + Sunitinib + Quizartinib + Linifanib | CIViC D | EID11094 |
| FLT3 D835Y | Cancer | Sensitivity/Response | Quizartinib + KW2449 + R406 + Ponatinib + AG1295 + Sorafenib + Sunitinib + AGS324 + Linifanib | CIViC D | EID11086 |
| FLT3 ITD | Cancer | Sensitivity/Response | FLT3 Tyrosine Kinase Inhibitor TTT-3002 + R406 + Ponatinib + Crenolanib + KW2449 + Sorafenib + Sunitinib + Quizartinib + Linifanib + AGS324 + AG1295 + Lestaurtinib + Midostaurin | CIViC D | EID11084 |
| FLT3 Overexpression AND FLT3LG Expression | Cancer | Sensitivity/Response | Quizartinib + Linifanib + Lestaurtinib + Midostaurin + Ponatinib + FLT3 Tyrosine Kinase Inhibitor TTT-3002 + Sunitinib | CIViC D | EID11088 |
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.
272 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| Afatinib | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CDK8, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| Crizotinib | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CDK8, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CDK8, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| QUIZARTINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CDK8, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| SORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CDK8, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| DORAMAPIMOD | ChEMBL | Phase 2 | CDK19, CDK8, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| FORETINIB | ChEMBL | Phase 2 | CDK19, CDK8, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| Selumetinib | PubChem | Approved | CDK19, CDK8, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| AXITINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| FEDRATINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| GEFITINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CDK8, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, RET, TEK |
| MIDOSTAURIN | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| VANDETANIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| LESTAURTINIB | ChEMBL | Phase 3 | CDK8, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| RAF-265 | ChEMBL | Phase 2 | CDK19, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| TOZASERTIB | ChEMBL | Phase 2 | CDK19, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| PONATINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CDK8, CSF1R, FLT1, FLT3, KDR, KIT, PDGFRB, RET |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| SUNITINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| CEDIRANIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| VATALANIB | ChEMBL | Phase 3 | CDK19, CDK8, CSF1R, FLT1, FLT4, KDR, KIT, PDGFRB, RET |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| ILORASERTIB | ChEMBL | Phase 2 | CDK8, CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| R-406 | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| ERLOTINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| TIVOZANIB | ChEMBL | Phase 4 (approved) | FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| BRIVANIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT4, KDR, KIT, PDGFRB, RET, TEK |
| DOVITINIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| MOTESANIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| SEMAXANIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| CENISERTIB | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| REBASTINIB | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, RET, TEK |
| SU-014813 | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB, RET |
| Idelalisib | PubChem | Approved | CSF1R, FLT1, FLT3, FLT4, KIT, PDGFRB, RET, TEK |
| BOSUTINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CSF1R, FLT3, KIT, PDGFRB, RET, TEK |
| NILOTINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CSF1R, FLT3, KIT, PDGFRB, RET, TEK |
| PEXIDARTINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CSF1R, FLT1, FLT3, KDR, KIT, PDGFRB |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT3, FLT4, KDR, KIT, RET, TEK |
| DASATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, KDR, KIT, PDGFRB, RET |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, RET |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT3, FLT4, KDR, KIT, RET, TEK |
| CEP-32496 | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, KDR, KIT, PDGFRB, RET |
| OSI-632 | ChEMBL | Phase 2 | FLT1, FLT3, FLT4, KDR, PDGFRB, RET, TEK |
| TANDUTINIB | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRB |
| IMATINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CSF1R, FLT3, KDR, KIT, PDGFRB |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, FLT4, KDR, KIT, RET |
| LENVATINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR, KIT, PDGFRB, RET |
| CANERTINIB | ChEMBL | Phase 3 | FLT1, FLT3, KDR, KIT, PDGFRB, RET |
| BFH-772 | ChEMBL | Phase 2 | FLT1, FLT4, KDR, KIT, PDGFRB, RET |
| CEP-11981 | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, KDR, RET, TEK |
| MK-2461 | ChEMBL | Phase 2 | FLT1, FLT3, FLT4, KDR, PDGFRB, RET |
| NERATINIB | ChEMBL + PubChem | Phase 4 (approved) | CDK19, CSF1R, FLT3, KDR, TEK |
| ALVOCIDIB | ChEMBL | Phase 3 | CDK19, CDK8, CSF1R, FLT3, KIT |
| BARASERTIB | ChEMBL | Phase 3 | FLT3, KDR, KIT, PDGFRB, RET |
| ORANTINIB | ChEMBL | Phase 3 | FLT1, FLT3, KDR, PDGFRB, RET |
| SARACATINIB | ChEMBL | Phase 3 | FLT3, KDR, KIT, PDGFRB, RET |
| AT-9283 | ChEMBL | Phase 2 | FLT1, FLT3, FLT4, KDR, RET |
| DANUSERTIB | ChEMBL | Phase 2 | FLT3, FLT4, KDR, KIT, RET |
| ENMD-2076 | ChEMBL | Phase 2 | CSF1R, FLT3, KDR, KIT, RET |
Related Atlas pages
- Genes: PDGFRB, KIT, CSF1R, FLT3, FLT1, KDR, FLT4, TEK, CDK19, CDK8, RET
- Diseases: hepatocellular carcinoma, cancer
- Drugs: Afatinib, Crizotinib, Pazopanib, Quizartinib, Sorafenib, Selumetinib, Axitinib, Fedratinib, Gefitinib, Midostaurin, Vandetanib, Lestaurtinib, Ponatinib, Regorafenib, Sunitinib, Nintedanib, Cediranib, Vatalanib, Erlotinib, Tivozanib, Brivanib, Dovitinib, Motesanib, Semaxanib, Idelalisib, Bosutinib, Nilotinib, Pexidartinib, Cabozantinib, Dasatinib, Entrectinib, Infigratinib, Imatinib, Brigatinib, Lenvatinib, Canertinib, Neratinib, Alvocidib, Barasertib, Orantinib, Saracatinib