Dovitinib

drug
On this page

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

FieldValue
ChEMBL IDCHEMBL522892
NameDovitinib
TypeSmall molecule
Max phase3
FDA approvedno
PubChem CID135398510
Molecular formulaC21H21FN6O
Molecular weight392.4
InChIKeyPIQCTGMSNWUMAF-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).

GeneTargetActionpAffinityCancer dependencyUniProt
EGFRepidermal growth factor receptorInhibition5.717.5%P00533
INSRInsulin receptorInhibition5.70.8%P06213
PDGFRAplatelet derived growth factor receptor alphaInhibition6.686.2%P16234
PDGFRBplatelet derived growth factor receptor betaInhibition8.32.3%P09619
KITKIT proto-oncogene, receptor tyrosine kinaseInhibition8.70.5%P10721
CSF1Rcolony stimulating factor 1 receptorInhibition8.520%P07333
FLT3fms related receptor tyrosine kinase 3Inhibition90.9%P36888
FGFR1fibroblast growth factor receptor 1Inhibition8.111.5%P11362
FGFR3fibroblast growth factor receptor 3Inhibition8.520.5%P22607
FLT1fms related receptor tyrosine kinase 1Inhibition8.520.1%P17948
KDRkinase insert domain receptorInhibition1.1%P35968
FLT4fms related receptor tyrosine kinase 4Inhibition8.520.2%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):

TargetpChemblTypeValueUnitActivity ID
FLT39.52Kd0.3nMCHEMBL_ACT_17903640
FLT39.19Kd0.64nMCHEMBL_ACT_2907383
FLT39.19Kd0.64nMCHEMBL_ACT_7591693
CAMK1G9Kd1nMCHEMBL_ACT_17886447
PDGFRB9IC501nMCHEMBL_ACT_17979951
KIT9IC501nMCHEMBL_ACT_17979952
FLT39IC501nMCHEMBL_ACT_17979953
CSF1R9IC501nMCHEMBL_ACT_17979967
KIT8.96IC501.1nMCHEMBL_ACT_13370872
FLT38.96Kd1.1nMCHEMBL_ACT_7591697
YES18.85IC501.4nMCHEMBL_ACT_13395969
KIT8.8Kd1.6nMCHEMBL_ACT_7590016
TNIK8.7IC502nMCHEMBL_ACT_16433822
P117998.7Kd2nMCHEMBL_ACT_2901473
MYLK38.7Kd2nMCHEMBL_ACT_7591947
FLT48.6IC502.51nMCHEMBL_ACT_13418834
FLT18.52IC503nMCHEMBL_ACT_2250295
FLT48.52IC503nMCHEMBL_ACT_2250296
FGFR38.52IC503nMCHEMBL_ACT_2250297
KIT8.52IC503nMCHEMBL_ACT_2250298
CSF1R8.52IC503nMCHEMBL_ACT_2250299
FLT38.52IC503nMCHEMBL_ACT_2250300
KIT8.51Kd3.1nMCHEMBL_ACT_2896989
KIT8.51Kd3.1nMCHEMBL_ACT_7590019
FLT38.5Ki3.16nMCHEMBL_ACT_9599368
FLT38.44Kd3.6nMCHEMBL_ACT_2890811
FLT38.44Kd3.6nMCHEMBL_ACT_7591696
PDGFRB8.42Kd3.8nMCHEMBL_ACT_2899069
PDGFRB8.42Kd3.8nMCHEMBL_ACT_7591631
FLT38.32Kd4.8nMCHEMBL_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:

PathwayTargetsGenes
PIP3 activates AKT signaling8EGFR, FGFR1, FGFR3, FLT3, INSR, KIT, PDGFRA, PDGFRB
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling8EGFR, FGFR1, FGFR3, FLT3, INSR, KIT, PDGFRA, PDGFRB
Constitutive Signaling by Aberrant PI3K in Cancer7EGFR, FGFR1, FGFR3, FLT3, KIT, PDGFRA, PDGFRB
RAF/MAP kinase cascade7EGFR, FGFR1, FGFR3, FLT3, KIT, PDGFRA, PDGFRB
PI3K Cascade3FGFR1, FGFR3, FLT3
VEGF binds to VEGFR leading to receptor dimerization3FLT1, FLT4, KDR
Signal Transduction2INSR, KIT
Downstream signal transduction2PDGFRA, PDGFRB
Signaling by PDGF2PDGFRA, PDGFRB
Neuropilin interactions with VEGF and VEGFR2FLT1, KDR
Negative regulation of the PI3K/AKT network2INSR, KIT
Signal transduction by L12EGFR, FGFR1
TFAP2 (AP-2) family regulates transcription of growth factors and their receptors2EGFR, KIT
Intracellular signaling by second messengers2INSR, KIT
Signaling by Receptor Tyrosine Kinases2INSR, KIT
High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells2FLT4, KDR
Signaling by ERBB21EGFR
Constitutive Signaling by Ligand-Responsive EGFR Cancer Variants1EGFR
Signaling by ERBB41EGFR
SHC1 events in ERBB2 signaling1EGFR
PLCG1 events in ERBB2 signaling1EGFR
Developmental Biology1KIT
Signaling by SCF-KIT1KIT
Regulation of KIT signaling1KIT
Disease1KIT
Signaling by EGFR1EGFR
GRB2 events in EGFR signaling1EGFR
GAB1 signalosome1EGFR
SHC1 events in EGFR signaling1EGFR
EGFR downregulation1EGFR

Dominant GO biological processes

GO termTargets
positive regulation of cell population proliferation12
protein phosphorylation12
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction11
cell surface receptor protein tyrosine kinase signaling pathway10
protein autophosphorylation10
positive regulation of cell migration9
positive regulation of MAPK cascade9
cell migration9
peptidyl-tyrosine phosphorylation8
positive regulation of ERK1 and ERK2 cascade7
cell population proliferation5
angiogenesis5
positive regulation of protein phosphorylation4
signal transduction4
negative regulation of apoptotic process4

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).

IndicationTrial phaseMONDOEFO
renal cell carcinoma3MONDO:0005086EFO:0000681
clear cell renal carcinoma3MONDO:0005005EFO:0000349
plasma cell myeloma2MONDO:0009693EFO:0001378
adenoid cystic carcinoma2MONDO:0004971EFO:0000231
neoplasm2MONDO:0005070EFO:0000616
malignant pleural mesothelioma2MONDO:0005112EFO:0000770
hepatocellular carcinoma2MONDO:0007256EFO:0000182
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
glioblastoma2MONDO:0018177EFO:0000519
gliosarcoma2MONDO:0016681EFO:1001465
adrenal cortex carcinoma2MONDO:0006639EFO:1000796
gastric neoplasm2MONDO:0021085MONDO:0001056
breast neoplasm2MONDO:0021100MONDO:0007254
endometrium neoplasm2MONDO:0021251MONDO:0011962
von Hippel-Lindau disease2MONDO:0008667MONDO:0008667
gastrointestinal stromal tumor2MONDO:0011719MONDO:0011719
adrenal gland pheochromocytoma2MONDO:0004974EFO:0000239
brain neoplasm2MONDO:0021211EFO:0003833
acute myeloid leukemia1MONDO:0018874EFO:0000222
melanoma1MONDO:0005105EFO: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

PhaseTrials
PHASE222
PHASE18
PHASE1/PHASE22
PHASE31
PHASE2/PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT01223027PHASE3COMPLETEDStudy of Dovitinib Versus Sorafenib in Patients With Metastatic Renal Cell Carcinoma
NCT02116803PHASE2/PHASE3COMPLETEDAn 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
NCT01232296PHASE2COMPLETEDA Study of Dovitinib Versus Sorafenib in Adult Patients With Hepatocellular Carcinoma (HCC) as a First Line Treatment
NCT01262027PHASE2COMPLETEDTKI258 for Metastatic Inflammatory Breast Cancer Patients
NCT01266070PHASE2TERMINATEDTKI 258 in Von Hippel-Lindau Syndrome (VHL)
NCT01440959PHASE2COMPLETEDDovitinib for Imatinib/Sumitinib-failed Gastrointestinal Stromal Tumors (GIST): TKI258
NCT01478373PHASE2COMPLETEDEfficacy and Safety of Dovitinib in Patients With Gastrointestinal Stromal Tumors Refractory and/or Intolerant to Imatinib
NCT01484041PHASE1/PHASE2TERMINATEDDovitinib Plus an Aromatase Inhibitor for Metastatic Breast Cancer
NCT01514526PHASE2COMPLETEDClinical Trial of Dovitinib in First-line Metastatic or Locally Advanced Non-resectable Adrenocortical Carcinoma
NCT01524692PHASE2COMPLETEDStudy of Dovitinib (TKI258) in Adenoid Cystic Carcinoma
NCT01528345PHASE2TERMINATEDTrial Evaluating Dovitinib Combined With Fulvestrant, in Postmenopausal Patients With HER2- and HR+ Breast Cancer
NCT01635907PHASE2COMPLETEDDovitinib in Neuroendocrine Tumors
NCT01676714PHASE2COMPLETEDStudy of Dovitinib and Biomarkers in Advanced Non-Small Cell Lung Cancer or Advanced Colorectal Cancer
NCT01678105PHASE2COMPLETEDA Phase II Study of Dovitinib in Recurrent and/or Metastatic Adenoid Cystic Carcinoma of the Salivary Glands
NCT01719549PHASE2COMPLETEDDovitinib for Gastric Cancer With FGFR2 Amplification: GASDOVI-1
NCT01732107PHASE2TERMINATEDDovitinib in BCG Refractory Urothelial Carcinoma With FGFR3 Mutations or Over-expression
NCT01753713PHASE2COMPLETEDDovitinib in Treating Patients With Recurrent or Progressive Glioblastoma
NCT01769547PHASE2TERMINATEDA Phase II Study of Single-agent DOVitinib in Advanced Malignant PlEural Mesothelioma Which Has Progressed Following Prior Platinum-Antifolate Chemotherapy
NCT01791387PHASE2UNKNOWN1st-line Activity of Dovitinib and Correlation With Genetic Changes in RCC
NCT01831726PHASE2COMPLETEDDovitinib for Patients With Tumor Pathway Activations Inhibited by Dovitinib
NCT01861197PHASE2UNKNOWNPhase II Study of Dovitinib for FGFR1 Amplified Squamous Non-small Cell Lung Cancer
NCT01888965PHASE2TERMINATEDMaintenance Dovitinib for Colorectal and Pancreas Cancer
NCT01921673PHASE1/PHASE2COMPLETEDDovitinib Plus Docetaxel in Gastric Cancer
NCT01964144PHASE2COMPLETEDAn Open-label, Multicenter, Phase II Study of Dovitinib in Advanced Thyroid Cancer
NCT01994590PHASE2TERMINATEDDovitinib (TKI258) and Abiraterone Acetate in Metastatic Castrate-Resistant Prostate Cancer (mCRPC)
NCT02065323PHASE2WITHDRAWNA Study of Dovitinib With Androgen Deprivation Therapy (ADT) in Patients With Metastatic Prostate Cancer Receiving Primary ADT
NCT01270906PHASE1TERMINATEDSafety of CHIR-258 (TKI258) in Advanced Solid Tumors
NCT01443481PHASE1COMPLETEDPharmacokinetics (PK) of TKI258 in Cancer Patients With Normal and Impaired Hepatic Function
NCT01548924PHASE1TERMINATEDDetermination of Dose of Antiangiogenic Multitargeted DOVITINIB (TKI258) Plus Paclitaxel in Patients With Solid Tumors
NCT01680796PHASE1WITHDRAWNDovitinib Combined With Bortezomib and Dexamethasone for Relapsed/Refractory Multiple Myeloma
NCT01700270PHASE1COMPLETEDPharmacokinetic Drug-drug Interaction Study of Dovitinib (TKI258) in Patients With Advanced Solid Tumors.
NCT01714765PHASE1COMPLETEDDose Escalation Study Investigating Everolimus and Dovitinib in Metastatic Clear Cell Renal Cancer
NCT01972750PHASE1UNKNOWNDovitinib (TKI258) in the Treatment of Patients With Relapsed Glioblastoma
NCT05571969PHASE1SUSPENDEDStudy 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.

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:

MoleculeSourceStatusShared targets
AFATINIBChEMBL + PubChemPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
CRIZOTINIBChEMBL + PubChemPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
PazopanibChEMBL + PubChemPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
SELUMETINIBChEMBL + PubChemPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
FEDRATINIBChEMBLPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
SORAFENIBChEMBLPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
SUNITINIBChEMBLPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
LESTAURTINIBChEMBLPhase 3CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
LINIFANIBChEMBLPhase 3CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
CENISERTIBChEMBLPhase 2CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
FORETINIBChEMBLPhase 2CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
ILORASERTIBChEMBLPhase 2CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
R-406ChEMBLPhase 2CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
SU-014813ChEMBLPhase 2CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
TOZASERTIBChEMBLPhase 2CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
GEFITINIBChEMBL + PubChemPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA
AXITINIBChEMBLPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
MIDOSTAURINChEMBLPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
NINTEDANIBChEMBLPhase 4 (approved)CSF1R, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
VANDETANIBChEMBLPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
CEDIRANIBChEMBLPhase 3CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
TANDUTINIBChEMBLPhase 2CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
REGORAFENIBChEMBL + PubChemPhase 4 (approved)CSF1R, FGFR1, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA, PDGFRB
DASATINIBChEMBLPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, KDR, KIT, PDGFRA, PDGFRB
PONATINIBChEMBLPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT3, KDR, KIT, PDGFRA, PDGFRB
BRIVANIBChEMBLPhase 3CSF1R, EGFR, FGFR1, FGFR3, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
MOTESANIBChEMBLPhase 3CSF1R, EGFR, FGFR1, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
SEMAXANIBChEMBLPhase 3CSF1R, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
DORAMAPIMODChEMBLPhase 2CSF1R, EGFR, FGFR1, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
OSI-632ChEMBLPhase 2EGFR, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, PDGFRA, PDGFRB
IdelalisibPubChemApprovedCSF1R, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KIT, PDGFRA, PDGFRB
BRIGATINIBChEMBLPhase 4 (approved)CSF1R, EGFR, FGFR1, FGFR3, FLT3, FLT4, INSR, KDR, KIT
ENTRECTINIBChEMBLPhase 4 (approved)CSF1R, FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT
INFIGRATINIBChEMBLPhase 4 (approved)FGFR1, FGFR3, FLT1, FLT3, FLT4, INSR, KDR, KIT, PDGFRA
DEFOSBARASERTIBChEMBLPhase 2CSF1R, EGFR, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
RAF-265ChEMBLPhase 2CSF1R, FGFR1, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
REBASTINIBChEMBLPhase 2CSF1R, FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA
ERLOTINIBChEMBLPhase 4 (approved)EGFR, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
LENVATINIBChEMBLPhase 4 (approved)FGFR1, FGFR3, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
QUIZARTINIBChEMBLPhase 4 (approved)CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
TIVOZANIBChEMBLPhase 4 (approved)FGFR1, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB
VATALANIBChEMBLPhase 3CSF1R, EGFR, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB
IMATINIBChEMBL + PubChemPhase 4 (approved)CSF1R, EGFR, FLT3, KDR, KIT, PDGFRA, PDGFRB
CABOZANTINIBChEMBLPhase 4 (approved)EGFR, FGFR1, FLT1, FLT3, FLT4, KDR, KIT
CERITINIBChEMBLPhase 4 (approved)EGFR, FGFR3, FLT3, INSR, KDR, KIT, PDGFRA
NINTEDANIB ESYLATEChEMBLPhase 4 (approved)FGFR1, FGFR3, FLT1, FLT4, KDR, PDGFRA, PDGFRB
PEXIDARTINIBChEMBLPhase 4 (approved)CSF1R, FLT1, FLT3, KDR, KIT, PDGFRA, PDGFRB
CANERTINIBChEMBLPhase 3EGFR, FLT1, FLT3, KDR, KIT, PDGFRA, PDGFRB
AT-9283ChEMBLPhase 2FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, PDGFRA
CEP-11981ChEMBLPhase 2CSF1R, FGFR1, FGFR3, FLT1, FLT3, KDR, PDGFRA
CEP-32496ChEMBLPhase 2CSF1R, EGFR, FLT1, FLT3, KDR, KIT, PDGFRB
MK-2461ChEMBLPhase 2FGFR1, FGFR3, FLT1, FLT3, FLT4, KDR, PDGFRB
BOSUTINIBChEMBLPhase 4 (approved)CSF1R, EGFR, FLT3, KIT, PDGFRA, PDGFRB
BARASERTIBChEMBLPhase 3EGFR, FLT3, KDR, KIT, PDGFRA, PDGFRB
SARACATINIBChEMBLPhase 3EGFR, FLT3, KDR, KIT, PDGFRA, PDGFRB
ENMD-2076ChEMBLPhase 2CSF1R, FGFR1, FLT3, KDR, KIT, PDGFRA
LUCITANIBChEMBLPhase 2FGFR1, FGFR3, FLT1, FLT4, KDR, PDGFRB
MILCICLIBChEMBLPhase 2EGFR, FGFR1, FLT3, FLT4, KIT, PDGFRB
BinimetinibPubChemApprovedEGFR, FGFR1, FLT3, INSR, KDR, PDGFRB
DACOMITINIBChEMBL + PubChemPhase 4 (approved)EGFR, FGFR1, FLT3, INSR, PDGFRB