Pexidartinib

Summary

Pexidartinib (CHEMBL3813873) is an approved small-molecule EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor (ATC L01EX15) targeting KIT, CSF1R, and FLT3; indicated across 16 conditions including neoplasm and tenosynovial giant cell tumor, diffuse type; with CIViC clinical evidence for 12 variant-indication associations (e.g. FLT3 F691L in acute myeloid leukemia).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01EX15
• Targets: 8 (KIT, CSF1R, FLT3…)
• Indications: 16 conditions
• Clinical trials: 26
• Precision-oncology evidence (CIViC): 12 variant–indication associations
• Chemistry: 417.8 Da · C20H15ClF3N5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3813873
Name	Pexidartinib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	25151352
ChEBI	CHEBI:145373
ATC	L01EX15
Molecular formula	C20H15ClF3N5
Molecular weight	417.8
InChIKey	JGWRKYUXBBNENE-UHFFFAOYSA-N

SMILES: C1=CC(=NC=C1CC2=CNC3=C2C=C(C=N3)Cl)NCC4=CN=C(C=C4)C(F)(F)F

IUPAC name: 5-[(5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl)methyl]-N-[[6-(trifluoromethyl)-3-pyridinyl]methyl]pyridin-2-amine

ChEBI definition: A pyrrolopyridine that is 5-chloro-1H-pyrrolo[2,3-b]pyridine which is substituted by a [6-({[6-(trifluoromethyl)pyridin-3-yl]methyl}amino)pyridin-3-yl]methyl group at position 3. It is a potent multi-targeted receptor tyrosine kinase inhibitor of CSF-1R, KIT, and FLT3 (IC50 of 20 nM, 10 nM and 160 nM, respectively). Approved by the FDA for the treatment of adult patients with symptomatic tenosynovial giant cell tumor (TGCT).

Pharmacological roles (ChEBI): EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, antineoplastic agent.

Also known as: CML-261, Pexidartinib, Plx-3397, PLX-3397, PLX3397, PEXIDARTINIB, PEXIDARTINIBPLX-3397, PEXIDARTINIB (PLX3397), pexidartinib

Parent form; salt/anhydrous children: CHEMBL3989973

Patent coverage: 1,475 distinct patent families (3,586 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 3,028 (84%) 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
KIT	KIT proto-oncogene, receptor tyrosine kinase	Inhibition	7.57	0.5%	P10721
CSF1R	colony stimulating factor 1 receptor	Inhibition	7.89	0%	P07333
FLT3	fms related receptor tyrosine kinase 3	Inhibition	6.8	0.9%	P36888
FLT1	fms related receptor tyrosine kinase 1	Inhibition	6.06	0.1%	P17948
KDR	kinase insert domain receptor	Inhibition	6.36	1.1%	P35968
NTRK3	neurotrophic receptor tyrosine kinase 3	Inhibition	6.05	0%	Q16288
CDK19	cyclin dependent kinase 19	Inhibition	6.85	0.1%	Q9BWU1
LCK	LCK proto-oncogene, Src family tyrosine kinase	Inhibition	6.07	0.1%	P06239

Broader ChEMBL bioactivity targets: 30 (assay-derived). Sample: Macrophage colony-stimulating factor 1 receptor, Alpha-2A adrenergic receptor, Vascular endothelial growth factor receptor 1, Platelet-derived growth factor receptor beta, Mast/stem cell growth factor receptor Kit, Receptor-type tyrosine-protein kinase FLT3, Platelet-derived growth factor receptor alpha, D(1A) dopamine receptor, Thromboxane A2 receptor, Progesterone receptor.

Bioactivity

ChEMBL activities: 104 potent at pChembl ≥ 5 of 110 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CSF1R	8.77	IC50	1.7	nM	CHEMBL_ACT_24693942
CSF1R	8.77	IC50	1.7	nM	CHEMBL_ACT_24694186
CSF1R	8.66	IC50	2.2	nM	CHEMBL_ACT_29025737
CSF1R	8.33	IC50	4.7	nM	CHEMBL_ACT_25922565
FLT3	8.3	IC50	5	nM	CHEMBL_ACT_16609130
CSF1R	8.3	IC50	5	nM	CHEMBL_ACT_25536023
CSF1R	8.25	IC50	5.61	nM	CHEMBL_ACT_25585245
CSF1R	8.24	Kd	5.8	nM	CHEMBL_ACT_25465441
CSF1R	8.24	Kd	5.8	nM	CHEMBL_ACT_25535943
PRKCQ	8.22	Kd	6	nM	CHEMBL_ACT_17930841
KIT	8.16	IC50	6.9	nM	CHEMBL_ACT_29025740
FLT3	8.15	IC50	7.1	nM	CHEMBL_ACT_24693962
FLT3	8.15	IC50	7.1	nM	CHEMBL_ACT_24694211
FLT3	8.15	IC50	7.1	nM	CHEMBL_ACT_29025746
FLT3	8.05	IC50	9	nM	CHEMBL_ACT_26132408
PDGFRA	8.02	IC50	9.6	nM	CHEMBL_ACT_24693982
PDGFRA	8.02	IC50	9.6	nM	CHEMBL_ACT_24694236
PDGFRA	8.02	IC50	9.6	nM	CHEMBL_ACT_29025743
CSF1R	8.01	IC50	9.8	nM	CHEMBL_ACT_25465322
CSF1R	8.01	IC50	9.7	nM	CHEMBL_ACT_25535963
KIT	8	IC50	10	nM	CHEMBL_ACT_25500506
KIT	8	IC50	10	nM	CHEMBL_ACT_26186115
KIT	8	IC50	10	nM	CHEMBL_ACT_26187727
KIT	8	IC50	10	nM	CHEMBL_ACT_29055505
CSF1R	7.97	IC50	10.8	nM	CHEMBL_ACT_18172205
FLT3	7.96	IC50	11	nM	CHEMBL_ACT_18893336
FLT3	7.96	IC50	11	nM	CHEMBL_ACT_24862906
FLT3	7.96	IC50	11	nM	CHEMBL_ACT_25016248
FLT3	7.96	IC50	11	nM	CHEMBL_ACT_25839758
CSF1R	7.92	IC50	12	nM	CHEMBL_ACT_18930902

Target pathways

Aggregated over 8 target gene(s): KIT, CSF1R, FLT3, FLT1, KDR, NTRK3, CDK19, LCK.

Top Reactome pathways

124 total, by targets touching each:

Pathway	Targets	Genes
PIP3 activates AKT signaling	4	FLT3, KIT, LCK, NTRK3
Constitutive Signaling by Aberrant PI3K in Cancer	4	FLT3, KIT, LCK, NTRK3
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	4	FLT3, KIT, LCK, NTRK3
Disease	3	CDK19, KIT, LCK
Developmental Biology	2	CDK19, KIT
Signaling by SCF-KIT	2	KIT, LCK
Regulation of KIT signaling	2	KIT, LCK
Signal Transduction	2	KIT, LCK
Neuropilin interactions with VEGF and VEGFR	2	FLT1, KDR
VEGF binds to VEGFR leading to receptor dimerization	2	FLT1, KDR
Negative regulation of the PI3K/AKT network	2	KIT, LCK
PI3K/AKT Signaling in Cancer	2	KIT, LCK
Diseases of signal transduction by growth factor receptors and second messengers	2	KIT, LCK
Infectious disease	2	CDK19, LCK
RAF/MAP kinase cascade	2	FLT3, KIT
Intracellular signaling by second messengers	2	KIT, LCK
Signaling by Receptor Tyrosine Kinases	2	KIT, LCK
FLT3 Signaling	2	FLT3, LCK
Signaling by KIT in disease	2	KIT, LCK
Signaling by phosphorylated juxtamembrane, extracellular and kinase domain KIT mutants	2	KIT, LCK
FLT3 signaling through SRC family kinases	2	FLT3, LCK
Viral Infection Pathways	2	CDK19, LCK
Hemostasis	1	LCK
PI3K Cascade	1	FLT3
GPVI-mediated activation cascade	1	LCK
Cytokine Signaling in Immune system	1	LCK
Adaptive Immune System	1	LCK
Metabolism	1	CDK19
HIV Infection	1	LCK
Host Interactions of HIV factors	1	LCK

Dominant GO biological processes

GO term	Targets
protein phosphorylation	8
cell surface receptor protein tyrosine kinase signaling pathway	7
positive regulation of cell population proliferation	6
positive regulation of MAPK cascade	6
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	6
cell migration	5
hemopoiesis	5
positive regulation of cell migration	5
protein autophosphorylation	5
peptidyl-tyrosine phosphorylation	5
regulation of cell shape	3
cytokine-mediated signaling pathway	3
regulation of cell population proliferation	3
positive regulation of tyrosine phosphorylation of STAT protein	3
positive regulation of gene expression	3

Indications & clinical

Indications

16 indications (1 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	4	MONDO:0005070	EFO:0000616
tenosynovial giant cell tumor, diffuse type	3	MONDO:0024686	MONDO:0024686
glioblastoma	2	MONDO:0018177	EFO:0000519
Hodgkins lymphoma	2	MONDO:0004952	EFO:0000183
melanoma	2	MONDO:0005105	EFO:0000756
metastatic melanoma	2	MONDO:0005191	EFO:0002617
angiosarcoma	2	MONDO:0016982	EFO:0003968
breast neoplasm	2	MONDO:0021100	MONDO:0007254
rheumatoid arthritis	1	MONDO:0008383	EFO:0000685
acute myeloid leukemia	1	MONDO:0018874	EFO:0000222
prostate adenocarcinoma	1	MONDO:0005082	EFO:0000673
malignant peripheral nerve sheath tumor	1	MONDO:0017827	EFO:0000760
gastrointestinal stromal tumor	1	MONDO:0011719	MONDO:0011719
liver disorder	0	MONDO:0005154	EFO:0001421

2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 26.

Phase distribution

Phase	Trials
PHASE1	9
PHASE2	6
PHASE1/PHASE2	6
PHASE3	2
PHASE4	1
EARLY_PHASE1	1
Not specified	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT04526704	PHASE4	COMPLETED	Study to Evaluate Discontinuation and Re-Treatment in Participants With Tenosynovial Giant Cell Tumor (TGCT) Previously Treated With Pexidartinib
NCT04488822	PHASE3	ACTIVE_NOT_RECRUITING	A Study of the Efficacy and Safety of Pexidartinib in Adult Subjects With TGCT
NCT02371369	PHASE3	COMPLETED	Phase 3 Study of Pexidartinib for Pigmented Villonodular Synovitis (PVNS) or Giant Cell Tumor of the Tendon Sheath (GCT-TS)
NCT01042379	PHASE2	RECRUITING	I-SPY TRIAL: Neoadjuvant and Personalized Adaptive Novel Agents to Treat Breast Cancer
NCT04703322	PHASE2	ACTIVE_NOT_RECRUITING	A Study of Pexidartinib in Tenosynovial Giant Cell Tumor in Japan
NCT01217229	PHASE2	COMPLETED	Safety and Efficacy Study of PLX3397 in Adults With Relapsed or Refractory Hodgkin Lymphoma
NCT01349036	PHASE2	TERMINATED	A Phase 2 Study of PLX3397 in Patients With Recurrent Glioblastoma
NCT01349049	PHASE1/PHASE2	COMPLETED	Phase 1/2 Safety and Efficacy of PLX3397 in Adults With Relapsed or Refractory Acute Myeloid Leukemia (AML)
NCT01499043	PHASE2	TERMINATED	Pilot Study of PLX3397 in Patients With Advanced Castration-Resistant Prostate Cancer (CRPC)
NCT01596751	PHASE1/PHASE2	COMPLETED	Phase Ib/II Study of PLX 3397 and Eribulin in Patients With Metastatic Breast Cancer
NCT01790503	PHASE1/PHASE2	COMPLETED	A Phase 1b/2 Study of PLX3397 + Radiation Therapy + Temozolomide in Patients With Newly Diagnosed Glioblastoma
NCT02071940	PHASE2	COMPLETED	PLX3397 KIT in Acral aNd mucOsal Melanoma
NCT02401815	PHASE1/PHASE2	COMPLETED	CGT9486 (Formerly Known as PLX9486) as a Single Agent and in Combination With PLX3397 (Pexidartinib) or Sunitinib in Participants With Advanced Solid Tumors
NCT02452424	PHASE1/PHASE2	TERMINATED	A Combination Clinical Study of PLX3397 and Pembrolizumab To Treat Advanced Melanoma and Other Solid Tumors
NCT02584647	PHASE1/PHASE2	TERMINATED	PLX3397 Plus Sirolimus in Unresectable Sarcoma and Malignant Peripheral Nerve Sheath Tumors
NCT01004861	PHASE1	COMPLETED	Safety Study of PLX108-01 in Patients With Solid Tumors
NCT01090570	PHASE1	WITHDRAWN	Safety, Pharmacokinetic (PK), Pharmcodynamic (PD), and Drug-Drug Interaction of PLX3397 in Patients With Rheumatoid Arthritis Who Are Receiving Methotrexate
NCT01525602	PHASE1	COMPLETED	Safety Study of PLX3397 and Paclitaxel in Patients With Advanced Solid Tumors
NCT01826448	PHASE1	TERMINATED	A Phase 1b Open Label, Dose Escalation Study of PLX3397 in Combination With Vemurafenib in V600-mutated BRAF Melanoma
NCT02734433	PHASE1	COMPLETED	Study of Pexidartinib in Asian Subjects With Advanced Solid Tumors
NCT02777710	PHASE1	COMPLETED	Evaluation of Safety and Activity of an Anti-PDL1 Antibody (DURVALUMAB) Combined With CSF-1R TKI (PEXIDARTINIB) in Patients With Metastatic/Advanced Pancreatic or Colorectal Cancers
NCT03138759	PHASE1	COMPLETED	Effect of Probenecid on Pexidartinib Pharmacokinetics
NCT03158103	PHASE1	COMPLETED	A Study of MEK162 (Binimetinib) in Combination With Pexidartinib in Patients With Advanced Gastrointestinal Stromal Tumor (GIST)
NCT03291288	PHASE1	COMPLETED	Effect of Pexidartinib on the Way the Body Processes CYP3A4 and CYP2C9 Substrates (Pharmacokinetics)
NCT04223635	EARLY_PHASE1	COMPLETED	Study of Pexidartinib in Participants With Moderate Hepatic Impairment Compared With Healthy Participants
NCT02975700	Not specified	COMPLETED	A Study of PLX3397 in Patients With Unresectable or Metastatic KIT-mutated Melanoma

Clinical evidence (CIViC)

Variant × indication × effect (12 predictive associations from 13 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
FLT3 F691L	Acute Myeloid Leukemia	Sensitivity/Response	Pexidartinib	CIViC B	EID8674 +1
CSF1 Overexpression	Tenosynovial Giant Cell Tumor	Sensitivity/Response	Pexidartinib	CIViC B	EID1969
FLT3 F691L	Acute Myeloid Leukemia	Resistance	Pexidartinib	CIViC B	EID9717
CSF1R Expression	Glioblastoma	Sensitivity/Response	Pexidartinib	CIViC D	EID8132
CSF1R Expression	Glioblastoma	Sensitivity/Response	Vatalanib + Pexidartinib	CIViC D	EID8133
CSF1R Expression	Glioblastoma	Sensitivity/Response	Pexidartinib + Dovitinib	CIViC D	EID8134
FLT3 D839A	Acute Myeloid Leukemia	Resistance	Pexidartinib	CIViC D	EID8671
FLT3 D839H	Acute Myeloid Leukemia	Resistance	Pexidartinib	CIViC D	EID8673
FLT3 D839N	Acute Myeloid Leukemia	Resistance	Pexidartinib	CIViC D	EID8672
FLT3 ITD & D839G	Acute Myeloid Leukemia	Resistance	Pexidartinib	CIViC D	EID8669
FLT3 ITD & N841K	Acute Myeloid Leukemia	Resistance	Pexidartinib	CIViC D	EID9936
FLT3 M664I	Acute Myeloid Leukemia	Resistance	Pexidartinib	CIViC D	EID8667

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

278 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
Afatinib	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
FEDRATINIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
GEFITINIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
MIDOSTAURIN	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
PAZOPANIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
QUIZARTINIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
SORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
SUNITINIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
DORAMAPIMOD	ChEMBL	Phase 2	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
FORETINIB	ChEMBL	Phase 2	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
TOZASERTIB	ChEMBL	Phase 2	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
Selumetinib	PubChem	Approved	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
AXITINIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK
PONATINIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
VANDETANIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK
ENTRECTINIB	ChEMBL	Phase 4 (approved)	CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
NINTEDANIB	ChEMBL	Phase 4 (approved)	CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
DOVITINIB	ChEMBL	Phase 3	CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
LESTAURTINIB	ChEMBL	Phase 3	CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
LINIFANIB	ChEMBL	Phase 3	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, NTRK3
ILORASERTIB	ChEMBL	Phase 2	CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
R-406	ChEMBL	Phase 2	CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
RAF-265	ChEMBL	Phase 2	CDK19, CSF1R, FLT1, FLT3, KDR, KIT, LCK
REBASTINIB	ChEMBL	Phase 2	CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
SU-014813	ChEMBL	Phase 2	CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
TANDUTINIB	ChEMBL	Phase 2	CSF1R, FLT1, FLT3, KDR, KIT, LCK, NTRK3
BOSUTINIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT3, KIT, LCK, NTRK3
ERLOTINIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, FLT1, FLT3, KDR, KIT, LCK
IMATINIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT3, KDR, KIT, LCK
NILOTINIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT3, KIT, LCK, NTRK3
DASATINIB	ChEMBL	Phase 4 (approved)	CSF1R, FLT1, FLT3, KDR, KIT, LCK
CEDIRANIB	ChEMBL	Phase 3	CSF1R, FLT1, FLT3, KDR, KIT, LCK
MOTESANIB	ChEMBL	Phase 3	CSF1R, FLT1, FLT3, KDR, KIT, LCK
CENISERTIB	ChEMBL	Phase 2	CSF1R, FLT1, FLT3, KDR, KIT, LCK
CEP-32496	ChEMBL	Phase 2	CSF1R, FLT1, FLT3, KDR, KIT, LCK
DEFOSBARASERTIB	ChEMBL	Phase 2	CSF1R, FLT1, FLT3, KDR, KIT, LCK
Idelalisib	PubChem	Approved	CSF1R, FLT1, FLT3, KIT, LCK, NTRK3
NERATINIB	ChEMBL + PubChem	Phase 4 (approved)	CDK19, CSF1R, FLT3, KDR, LCK
BRIGATINIB	ChEMBL	Phase 4 (approved)	CSF1R, FLT3, KDR, KIT, LCK
CABOZANTINIB	ChEMBL	Phase 4 (approved)	FLT1, FLT3, KDR, KIT, LCK
INFIGRATINIB	ChEMBL	Phase 4 (approved)	FLT1, FLT3, KDR, KIT, LCK
TIVOZANIB	ChEMBL	Phase 4 (approved)	FLT1, FLT3, KDR, KIT, LCK
ALVOCIDIB	ChEMBL	Phase 3	CDK19, CSF1R, FLT3, KIT, LCK
BRIVANIB	ChEMBL	Phase 3	CSF1R, FLT1, KDR, KIT, LCK
CANERTINIB	ChEMBL	Phase 3	FLT1, FLT3, KDR, KIT, LCK
SEMAXANIB	ChEMBL	Phase 3	CSF1R, FLT1, FLT3, KDR, KIT
VATALANIB	ChEMBL	Phase 3	CDK19, CSF1R, FLT1, KDR, KIT
ENMD-2076	ChEMBL	Phase 2	CSF1R, FLT3, KDR, KIT, LCK
CERITINIB	ChEMBL	Phase 4 (approved)	FLT3, KDR, KIT, LCK
IBRUTINIB	ChEMBL	Phase 4 (approved)	CSF1R, FLT3, KDR, LCK
ALISERTIB	ChEMBL	Phase 3	FLT1, KDR, LCK, NTRK3
BARASERTIB	ChEMBL	Phase 3	FLT3, KDR, KIT, LCK
DEFACTINIB	ChEMBL	Phase 3	FLT1, FLT3, KDR, NTRK3
SARACATINIB	ChEMBL	Phase 3	FLT3, KDR, KIT, LCK
VIMSELTINIB	ChEMBL	Phase 3	CSF1R, FLT3, KIT, LCK
AT-9283	ChEMBL	Phase 2	FLT1, FLT3, KDR, LCK
BMS-754807	ChEMBL	Phase 2	CSF1R, FLT3, LCK, NTRK3
BMS-777607	ChEMBL	Phase 2	FLT3, KDR, KIT, LCK