Dovitinib
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Also known as CHIR-258GFKI-258NVP-TKI258Tki-258CHIR-258/TKI-258SID103904684SID137275871DOVITINIB (TKI-258, CHIR-258)Dovitinib (TKI-258CHIR-258)Divitinib
Summary
Dovitinib (CHEMBL522892) is a phase-3 clinical-stage small molecule targeting EGFR, INSR, and PDGFRA; indicated across 26 conditions including renal cell carcinoma and clear cell renal carcinoma.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- Targets: 12 (EGFR, INSR, PDGFRA…)
- Indications: 26 conditions
- Clinical trials: 34
- Chemistry: 392.4 Da · C21H21FN6O
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL522892 |
| Name | Dovitinib |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 135398510 |
| Molecular formula | C21H21FN6O |
| Molecular weight | 392.4 |
| InChIKey | PIQCTGMSNWUMAF-UHFFFAOYSA-N |
SMILES: CN1CCN(CC1)C2=CC3=C(C=C2)N=C(N3)C4=C(C5=C(C=CC=C5F)NC4=O)N
IUPAC name: 4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one
Also known as: CHIR-258, Dovitinib, GFKI-258, NVP-TKI258, Tki-258, TKI-258, CHIR-258/TKI-258, SID103904684, SID137275871, DOVITINIB, DOVITINIB (TKI-258, CHIR-258), Dovitinib (TKI-258; CHIR-258)
Parent form; salt/anhydrous children: CHEMBL4297063, CHEMBL5570498
Patent coverage: 1,940 distinct patent families (4,944 SureChEMBL compound mentions), from 7 matched compound structure(s). One matched structure accounts for 4,067 (82%) 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 |
|---|---|---|---|---|---|
| EGFR | epidermal growth factor receptor | Inhibition | 5.7 | 17.5% | P00533 |
| INSR | Insulin receptor | Inhibition | 5.7 | 0.8% | P06213 |
| PDGFRA | platelet derived growth factor receptor alpha | Inhibition | 6.68 | 6.2% | P16234 |
| PDGFRB | platelet derived growth factor receptor beta | Inhibition | 8.3 | 2.3% | P09619 |
| KIT | KIT proto-oncogene, receptor tyrosine kinase | Inhibition | 8.7 | 0.5% | P10721 |
| CSF1R | colony stimulating factor 1 receptor | Inhibition | 8.52 | 0% | P07333 |
| FLT3 | fms related receptor tyrosine kinase 3 | Inhibition | 9 | 0.9% | P36888 |
| FGFR1 | fibroblast growth factor receptor 1 | Inhibition | 8.1 | 11.5% | P11362 |
| FGFR3 | fibroblast growth factor receptor 3 | Inhibition | 8.52 | 0.5% | P22607 |
| FLT1 | fms related receptor tyrosine kinase 1 | Inhibition | 8.52 | 0.1% | P17948 |
| KDR | kinase insert domain receptor | Inhibition | 1.1% | P35968 | |
| FLT4 | fms related receptor tyrosine kinase 4 | Inhibition | 8.52 | 0.2% | P35916 |
Broader ChEMBL bioactivity targets: 210 (assay-derived). Sample: Leucine-rich repeat serine/threonine-protein kinase 2, Rhodopsin kinase GRK7, Serine/threonine-protein kinase 38, STE20/SPS1-related proline-alanine-rich protein kinase, Mitogen-activated protein kinase kinase kinase 13, Microtubule-associated serine/threonine-protein kinase 1, Serine/threonine-protein kinase SBK1, Hormonally up-regulated neu tumor-associated kinase, Tyrosine-protein kinase Fyn, Macrophage colony-stimulating factor 1 receptor.
Bioactivity
ChEMBL activities: 533 potent at pChembl ≥ 5 of 536 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| FLT3 | 9.52 | Kd | 0.3 | nM | CHEMBL_ACT_17903640 |
| FLT3 | 9.19 | Kd | 0.64 | nM | CHEMBL_ACT_2907383 |
| FLT3 | 9.19 | Kd | 0.64 | nM | CHEMBL_ACT_7591693 |
| CAMK1G | 9 | Kd | 1 | nM | CHEMBL_ACT_17886447 |
| PDGFRB | 9 | IC50 | 1 | nM | CHEMBL_ACT_17979951 |
| KIT | 9 | IC50 | 1 | nM | CHEMBL_ACT_17979952 |
| FLT3 | 9 | IC50 | 1 | nM | CHEMBL_ACT_17979953 |
| CSF1R | 9 | IC50 | 1 | nM | CHEMBL_ACT_17979967 |
| KIT | 8.96 | IC50 | 1.1 | nM | CHEMBL_ACT_13370872 |
| FLT3 | 8.96 | Kd | 1.1 | nM | CHEMBL_ACT_7591697 |
| YES1 | 8.85 | IC50 | 1.4 | nM | CHEMBL_ACT_13395969 |
| KIT | 8.8 | Kd | 1.6 | nM | CHEMBL_ACT_7590016 |
| TNIK | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_16433822 |
| P11799 | 8.7 | Kd | 2 | nM | CHEMBL_ACT_2901473 |
| MYLK3 | 8.7 | Kd | 2 | nM | CHEMBL_ACT_7591947 |
| FLT4 | 8.6 | IC50 | 2.51 | nM | CHEMBL_ACT_13418834 |
| FLT1 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_2250295 |
| FLT4 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_2250296 |
| FGFR3 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_2250297 |
| KIT | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_2250298 |
| CSF1R | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_2250299 |
| FLT3 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_2250300 |
| KIT | 8.51 | Kd | 3.1 | nM | CHEMBL_ACT_2896989 |
| KIT | 8.51 | Kd | 3.1 | nM | CHEMBL_ACT_7590019 |
| FLT3 | 8.5 | Ki | 3.16 | nM | CHEMBL_ACT_9599368 |
| FLT3 | 8.44 | Kd | 3.6 | nM | CHEMBL_ACT_2890811 |
| FLT3 | 8.44 | Kd | 3.6 | nM | CHEMBL_ACT_7591696 |
| PDGFRB | 8.42 | Kd | 3.8 | nM | CHEMBL_ACT_2899069 |
| PDGFRB | 8.42 | Kd | 3.8 | nM | CHEMBL_ACT_7591631 |
| FLT3 | 8.32 | Kd | 4.8 | nM | CHEMBL_ACT_2890849 |
Target pathways
Aggregated over 12 target gene(s): EGFR, INSR, PDGFRA, PDGFRB, KIT, CSF1R, FLT3, FGFR1, FGFR3, FLT1, KDR, FLT4.
Top Reactome pathways
146 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| PIP3 activates AKT signaling | 8 | EGFR, FGFR1, FGFR3, FLT3, INSR, KIT, PDGFRA, PDGFRB |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 8 | EGFR, FGFR1, FGFR3, FLT3, INSR, KIT, PDGFRA, PDGFRB |
| Constitutive Signaling by Aberrant PI3K in Cancer | 7 | EGFR, FGFR1, FGFR3, FLT3, KIT, PDGFRA, PDGFRB |
| RAF/MAP kinase cascade | 7 | EGFR, FGFR1, FGFR3, FLT3, KIT, PDGFRA, PDGFRB |
| PI3K Cascade | 3 | FGFR1, FGFR3, FLT3 |
| VEGF binds to VEGFR leading to receptor dimerization | 3 | FLT1, FLT4, KDR |
| Signal Transduction | 2 | INSR, KIT |
| Downstream signal transduction | 2 | PDGFRA, PDGFRB |
| Signaling by PDGF | 2 | PDGFRA, PDGFRB |
| Neuropilin interactions with VEGF and VEGFR | 2 | FLT1, KDR |
| Negative regulation of the PI3K/AKT network | 2 | INSR, KIT |
| Signal transduction by L1 | 2 | EGFR, FGFR1 |
| TFAP2 (AP-2) family regulates transcription of growth factors and their receptors | 2 | EGFR, KIT |
| Intracellular signaling by second messengers | 2 | INSR, KIT |
| Signaling by Receptor Tyrosine Kinases | 2 | INSR, KIT |
| High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells | 2 | FLT4, KDR |
| Signaling by ERBB2 | 1 | EGFR |
| Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants | 1 | EGFR |
| Signaling by ERBB4 | 1 | EGFR |
| SHC1 events in ERBB2 signaling | 1 | EGFR |
| PLCG1 events in ERBB2 signaling | 1 | EGFR |
| Developmental Biology | 1 | KIT |
| Signaling by SCF-KIT | 1 | KIT |
| Regulation of KIT signaling | 1 | KIT |
| Disease | 1 | KIT |
| Signaling by EGFR | 1 | EGFR |
| GRB2 events in EGFR signaling | 1 | EGFR |
| GAB1 signalosome | 1 | EGFR |
| SHC1 events in EGFR signaling | 1 | EGFR |
| EGFR downregulation | 1 | EGFR |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| positive regulation of cell population proliferation | 12 |
| protein phosphorylation | 12 |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 11 |
| cell surface receptor protein tyrosine kinase signaling pathway | 10 |
| protein autophosphorylation | 10 |
| positive regulation of cell migration | 9 |
| positive regulation of MAPK cascade | 9 |
| cell migration | 9 |
| peptidyl-tyrosine phosphorylation | 8 |
| positive regulation of ERK1 and ERK2 cascade | 7 |
| cell population proliferation | 5 |
| angiogenesis | 5 |
| positive regulation of protein phosphorylation | 4 |
| signal transduction | 4 |
| negative regulation of apoptotic process | 4 |
Indications & clinical
Indications
26 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 |
|---|---|---|---|
| renal cell carcinoma | 3 | MONDO:0005086 | EFO:0000681 |
| clear cell renal carcinoma | 3 | MONDO:0005005 | EFO:0000349 |
| plasma cell myeloma | 2 | MONDO:0009693 | EFO:0001378 |
| adenoid cystic carcinoma | 2 | MONDO:0004971 | EFO:0000231 |
| neoplasm | 2 | MONDO:0005070 | EFO:0000616 |
| malignant pleural mesothelioma | 2 | MONDO:0005112 | EFO:0000770 |
| hepatocellular carcinoma | 2 | MONDO:0007256 | EFO:0000182 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| glioblastoma | 2 | MONDO:0018177 | EFO:0000519 |
| gliosarcoma | 2 | MONDO:0016681 | EFO:1001465 |
| adrenal cortex carcinoma | 2 | MONDO:0006639 | EFO:1000796 |
| gastric neoplasm | 2 | MONDO:0021085 | MONDO:0001056 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| endometrium neoplasm | 2 | MONDO:0021251 | MONDO:0011962 |
| von Hippel-Lindau disease | 2 | MONDO:0008667 | MONDO:0008667 |
| gastrointestinal stromal tumor | 2 | MONDO:0011719 | MONDO:0011719 |
| adrenal gland pheochromocytoma | 2 | MONDO:0004974 | EFO:0000239 |
| brain neoplasm | 2 | MONDO:0021211 | EFO:0003833 |
| acute myeloid leukemia | 1 | MONDO:0018874 | EFO:0000222 |
| melanoma | 1 | MONDO:0005105 | EFO:0000756 |
6 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 34.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 22 |
| PHASE1 | 8 |
| PHASE1/PHASE2 | 2 |
| PHASE3 | 1 |
| PHASE2/PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01223027 | PHASE3 | COMPLETED | Study of Dovitinib Versus Sorafenib in Patients With Metastatic Renal Cell Carcinoma |
| NCT02116803 | PHASE2/PHASE3 | COMPLETED | An Open Label Multi-center Extension Study to Evaluate Long-term Safety/ Tolerability of Dovitinib in Patients With Solid Tumors Who Continue to Receive Treatment With Dovitinib (TKI258) in Novartis-sponsored Single Agent Dovitinib Studies Which Fulfilled the Requirements for the Primary Objective |
| NCT01232296 | PHASE2 | COMPLETED | A Study of Dovitinib Versus Sorafenib in Adult Patients With Hepatocellular Carcinoma (HCC) as a First Line Treatment |
| NCT01262027 | PHASE2 | COMPLETED | TKI258 for Metastatic Inflammatory Breast Cancer Patients |
| NCT01266070 | PHASE2 | TERMINATED | TKI 258 in Von Hippel-Lindau Syndrome (VHL) |
| NCT01440959 | PHASE2 | COMPLETED | Dovitinib for Imatinib/Sumitinib-failed Gastrointestinal Stromal Tumors (GIST): TKI258 |
| NCT01478373 | PHASE2 | COMPLETED | Efficacy and Safety of Dovitinib in Patients With Gastrointestinal Stromal Tumors Refractory and/or Intolerant to Imatinib |
| NCT01484041 | PHASE1/PHASE2 | TERMINATED | Dovitinib Plus an Aromatase Inhibitor for Metastatic Breast Cancer |
| NCT01514526 | PHASE2 | COMPLETED | Clinical Trial of Dovitinib in First-line Metastatic or Locally Advanced Non-resectable Adrenocortical Carcinoma |
| NCT01524692 | PHASE2 | COMPLETED | Study of Dovitinib (TKI258) in Adenoid Cystic Carcinoma |
| NCT01528345 | PHASE2 | TERMINATED | Trial Evaluating Dovitinib Combined With Fulvestrant, in Postmenopausal Patients With HER2- and HR+ Breast Cancer |
| NCT01635907 | PHASE2 | COMPLETED | Dovitinib in Neuroendocrine Tumors |
| NCT01676714 | PHASE2 | COMPLETED | Study of Dovitinib and Biomarkers in Advanced Non-Small Cell Lung Cancer or Advanced Colorectal Cancer |
| NCT01678105 | PHASE2 | COMPLETED | A Phase II Study of Dovitinib in Recurrent and/or Metastatic Adenoid Cystic Carcinoma of the Salivary Glands |
| NCT01719549 | PHASE2 | COMPLETED | Dovitinib for Gastric Cancer With FGFR2 Amplification: GASDOVI-1 |
| NCT01732107 | PHASE2 | TERMINATED | Dovitinib in BCG Refractory Urothelial Carcinoma With FGFR3 Mutations or Over-expression |
| NCT01753713 | PHASE2 | COMPLETED | Dovitinib in Treating Patients With Recurrent or Progressive Glioblastoma |
| NCT01769547 | PHASE2 | TERMINATED | A Phase II Study of Single-agent DOVitinib in Advanced Malignant PlEural Mesothelioma Which Has Progressed Following Prior Platinum-Antifolate Chemotherapy |
| NCT01791387 | PHASE2 | UNKNOWN | 1st-line Activity of Dovitinib and Correlation With Genetic Changes in RCC |
| NCT01831726 | PHASE2 | COMPLETED | Dovitinib for Patients With Tumor Pathway Activations Inhibited by Dovitinib |
| NCT01861197 | PHASE2 | UNKNOWN | Phase II Study of Dovitinib for FGFR1 Amplified Squamous Non-small Cell Lung Cancer |
| NCT01888965 | PHASE2 | TERMINATED | Maintenance Dovitinib for Colorectal and Pancreas Cancer |
| NCT01921673 | PHASE1/PHASE2 | COMPLETED | Dovitinib Plus Docetaxel in Gastric Cancer |
| NCT01964144 | PHASE2 | COMPLETED | An Open-label, Multicenter, Phase II Study of Dovitinib in Advanced Thyroid Cancer |
| NCT01994590 | PHASE2 | TERMINATED | Dovitinib (TKI258) and Abiraterone Acetate in Metastatic Castrate-Resistant Prostate Cancer (mCRPC) |
| NCT02065323 | PHASE2 | WITHDRAWN | A Study of Dovitinib With Androgen Deprivation Therapy (ADT) in Patients With Metastatic Prostate Cancer Receiving Primary ADT |
| NCT01270906 | PHASE1 | TERMINATED | Safety of CHIR-258 (TKI258) in Advanced Solid Tumors |
| NCT01443481 | PHASE1 | COMPLETED | Pharmacokinetics (PK) of TKI258 in Cancer Patients With Normal and Impaired Hepatic Function |
| NCT01548924 | PHASE1 | TERMINATED | Determination of Dose of Antiangiogenic Multitargeted DOVITINIB (TKI258) Plus Paclitaxel in Patients With Solid Tumors |
| NCT01680796 | PHASE1 | WITHDRAWN | Dovitinib Combined With Bortezomib and Dexamethasone for Relapsed/Refractory Multiple Myeloma |
| NCT01700270 | PHASE1 | COMPLETED | Pharmacokinetic Drug-drug Interaction Study of Dovitinib (TKI258) in Patients With Advanced Solid Tumors. |
| NCT01714765 | PHASE1 | COMPLETED | Dose Escalation Study Investigating Everolimus and Dovitinib in Metastatic Clear Cell Renal Cancer |
| NCT01972750 | PHASE1 | UNKNOWN | Dovitinib (TKI258) in the Treatment of Patients With Relapsed Glioblastoma |
| NCT05571969 | PHASE1 | SUSPENDED | Study to Determine the Maximum Tolerated Dose (MTD) of PARPi 2X-121 Monotherapy and the MTD of Dovitinib in Combination With 2X-121 in Patients With Advanced Solid Tumors |
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.
341 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| AFATINIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| Pazopanib | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| SELUMETINIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| SORAFENIB | ChEMBL | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| SUNITINIB | ChEMBL | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| LESTAURTINIB | ChEMBL | Phase 3 | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| LINIFANIB | ChEMBL | Phase 3 | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| CENISERTIB | ChEMBL | Phase 2 | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| FORETINIB | ChEMBL | Phase 2 | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| ILORASERTIB | ChEMBL | Phase 2 | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| R-406 | ChEMBL | Phase 2 | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| SU-014813 | ChEMBL | Phase 2 | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| TOZASERTIB | ChEMBL | Phase 2 | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| GEFITINIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA |
| AXITINIB | ChEMBL | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| VANDETANIB | ChEMBL | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| CEDIRANIB | ChEMBL | Phase 3 | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| TANDUTINIB | ChEMBL | Phase 2 | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FGFR1, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB |
| DASATINIB | ChEMBL | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, KDR, KIT, PDGFRA, PDGFRB |
| PONATINIB | ChEMBL | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, KDR, KIT, PDGFRA, PDGFRB |
| BRIVANIB | ChEMBL | Phase 3 | CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| MOTESANIB | ChEMBL | Phase 3 | CSF1R, EGFR, FGFR1, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| SEMAXANIB | ChEMBL | Phase 3 | CSF1R, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| DORAMAPIMOD | ChEMBL | Phase 2 | CSF1R, EGFR, FGFR1, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| OSI-632 | ChEMBL | Phase 2 | EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, PDGFRA, PDGFRB |
| Idelalisib | PubChem | Approved | CSF1R, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KIT, PDGFRA, PDGFRB |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | CSF1R, EGFR, FGFR1, FGFR3, FLT3, FLT4, INSR, KDR, KIT |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | CSF1R, EGFR, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| RAF-265 | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| REBASTINIB | ChEMBL | Phase 2 | CSF1R, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | EGFR, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| LENVATINIB | ChEMBL | Phase 4 (approved) | FGFR1, FGFR3, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| QUIZARTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| TIVOZANIB | ChEMBL | Phase 4 (approved) | FGFR1, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| VATALANIB | ChEMBL | Phase 3 | CSF1R, EGFR, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| IMATINIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, EGFR, FLT3, KDR, KIT, PDGFRA, PDGFRB |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | EGFR, FGFR1, FLT1, FLT3, FLT4, KDR, KIT |
| CERITINIB | ChEMBL | Phase 4 (approved) | EGFR, FGFR3, FLT3, INSR, KDR, KIT, PDGFRA |
| NINTEDANIB ESYLATE | ChEMBL | Phase 4 (approved) | FGFR1, FGFR3, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| PEXIDARTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, KDR, KIT, PDGFRA, PDGFRB |
| CANERTINIB | ChEMBL | Phase 3 | EGFR, FLT1, FLT3, KDR, KIT, PDGFRA, PDGFRB |
| AT-9283 | ChEMBL | Phase 2 | FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, PDGFRA |
| CEP-11981 | ChEMBL | Phase 2 | CSF1R, FGFR1, FGFR3, FLT1, FLT3, KDR, PDGFRA |
| CEP-32496 | ChEMBL | Phase 2 | CSF1R, EGFR, FLT1, FLT3, KDR, KIT, PDGFRB |
| MK-2461 | ChEMBL | Phase 2 | FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, PDGFRB |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | CSF1R, EGFR, FLT3, KIT, PDGFRA, PDGFRB |
| BARASERTIB | ChEMBL | Phase 3 | EGFR, FLT3, KDR, KIT, PDGFRA, PDGFRB |
| SARACATINIB | ChEMBL | Phase 3 | EGFR, FLT3, KDR, KIT, PDGFRA, PDGFRB |
| ENMD-2076 | ChEMBL | Phase 2 | CSF1R, FGFR1, FLT3, KDR, KIT, PDGFRA |
| LUCITANIB | ChEMBL | Phase 2 | FGFR1, FGFR3, FLT1, FLT4, KDR, PDGFRB |
| MILCICLIB | ChEMBL | Phase 2 | EGFR, FGFR1, FLT3, FLT4, KIT, PDGFRB |
| Binimetinib | PubChem | Approved | EGFR, FGFR1, FLT3, INSR, KDR, PDGFRB |
| DACOMITINIB | ChEMBL + PubChem | Phase 4 (approved) | EGFR, FGFR1, FLT3, INSR, PDGFRB |
Related Atlas pages
- Genes: EGFR, INSR, PDGFRA, PDGFRB, KIT, CSF1R, FLT3, FGFR1, FGFR3, FLT1, KDR, FLT4
- Diseases: renal cell carcinoma, clear cell renal carcinoma
- Drugs: Afatinib, Crizotinib, Pazopanib, Selumetinib, Fedratinib, Sorafenib, Sunitinib, Lestaurtinib, Linifanib, Gefitinib, Axitinib, Midostaurin, Nintedanib, Vandetanib, Cediranib, Regorafenib, Dasatinib, Ponatinib, Brivanib, Motesanib, Semaxanib, Idelalisib, Brigatinib, Entrectinib, Infigratinib, Erlotinib, Lenvatinib, Quizartinib, Tivozanib, Vatalanib, Imatinib, Cabozantinib, Ceritinib, Pexidartinib, Canertinib, Bosutinib, Barasertib, Saracatinib, Binimetinib, Dacomitinib
- Biomarker genes: FGF3, FGFR2