Cabozantinib

Summary

Cabozantinib (CHEMBL2105717) is an approved small-molecule tyrosine kinase inhibitor (ATC L01EX07) targeting KDR, MET, and RET; indicated across 57 conditions including neoplasm and renal cell carcinoma; with CIViC clinical evidence for 18 variant-indication associations (e.g. GNA11 Mutation in uveal melanoma).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01EX07
• Targets: 3 (KDR, MET, RET)
• Indications: 57 conditions
• Clinical trials: 254
• Precision-oncology evidence (CIViC): 18 variant–indication associations
• Chemistry: 501.5 Da · C28H24FN3O5

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2105717
Name	Cabozantinib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	25102847
ChEBI	CHEBI:72317
ATC	L01EX07
Molecular formula	C28H24FN3O5
Molecular weight	501.5
InChIKey	ONIQOQHATWINJY-UHFFFAOYSA-N

SMILES: COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F

IUPAC name: 1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N’-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

ChEBI definition: A dicarboxylic acid diamide that is N-phenyl-N’-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide in which the hydrogen at position 4 on the phenyl ring is substituted by a (6,7-dimethoxyquinolin-4-yl)oxy group. A multi-tyrosine kinase inhibitor, used (as its malate salt) for the treatment of progressive, metastatic, medullary thyroid cancer.

Pharmacological roles (ChEBI): tyrosine kinase inhibitor, antineoplastic agent.

Also known as: BMS-907351 FREE BASE, Cabozantinib, XL-184 FREE BASE, CABOZANTINIB, XL-184, XL 184, BMS-907351, XL184 FREE BASE, CABOZANTINIB S-MALATE, XL184, CABOZANTINIBCT-XL184COMETRIQXL184C3627, CABOMETYX

Parent form; salt/anhydrous children: CHEMBL2103868

Patent coverage: 4,816 distinct patent families (11,177 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 10,603 (95%) 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
KDR	kinase insert domain receptor	Inhibition	10.46	1.1%	P35968
MET	MET proto-oncogene, receptor tyrosine kinase	Inhibition	8.9	2.4%	P08581
RET	ret proto-oncogene	Inhibition	7.96	0.4%	P07949

Broader ChEMBL bioactivity targets: 55 (assay-derived). Sample: Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma, Receptor-interacting serine/threonine-protein kinase 3, Receptor tyrosine-protein kinase erbB-2, 5-hydroxytryptamine receptor 2B, Tyrosine-protein kinase ABL1, Alpha-2A adrenergic receptor, Vascular endothelial growth factor receptor 1, Alpha-2C adrenergic receptor, Mast/stem cell growth factor receptor Kit, Amine oxidase [flavin-containing] A.

Bioactivity

ChEMBL activities: 229 potent at pChembl ≥ 5 of 237 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
KDR	10.52	IC50	0.03	nM	CHEMBL_ACT_29065528
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_16465571
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_16617409
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_16742604
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_18096400
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_18260588
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_18309584
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_18772569
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_18854165
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_22809994
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_24672546
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_24867156
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_24867255
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_25952270
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_26137479
KDR	10.46	Ki	0.04	nM	CHEMBL_ACT_27790655
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_29212337
KDR	10.46	IC50	0.04	nM	CHEMBL_ACT_29252827
KDR	10.07	IC50	0.09	nM	CHEMBL_ACT_18096417
KDR	9.32	IC50	0.48	nM	CHEMBL_ACT_18390489
AXL	9.3	IC50	0.5	nM	CHEMBL_ACT_29320248
MERTK	9.3	IC50	0.5	nM	CHEMBL_ACT_29320252
KDR	9.3	IC50	0.5	nM	CHEMBL_ACT_29320256
FLT3	9.22	IC50	0.6	nM	CHEMBL_ACT_24862922
KDR	9.15	AC50	0.7	nM	CHEMBL_ACT_25167918
MET	8.89	IC50	1.3	nM	CHEMBL_ACT_16465572
MET	8.89	IC50	1.3	nM	CHEMBL_ACT_16617408
MET	8.89	IC50	1.3	nM	CHEMBL_ACT_16742603
MET	8.89	IC50	1.3	nM	CHEMBL_ACT_18096401
MET	8.89	IC50	1.3	nM	CHEMBL_ACT_18309583

Target pathways

Aggregated over 3 target gene(s): KDR, MET, RET.

Top Reactome pathways

55 total, by targets touching each:

Pathway	Targets	Genes
RAF/MAP kinase cascade	2	MET, RET
PIP3 activates AKT signaling	1	MET
Developmental Biology	1	MET
Signal Transduction	1	MET
Disease	1	MET
Neuropilin interactions with VEGF and VEGFR	1	KDR
VEGF binds to VEGFR leading to receptor dimerization	1	KDR
Negative regulation of the PI3K/AKT network	1	MET
Generic Transcription Pathway	1	MET
Integrin cell surface interactions	1	KDR
PI3K/AKT Signaling in Cancer	1	MET
Constitutive Signaling by Aberrant PI3K in Cancer	1	MET
Semaphorin interactions	1	MET
Sema4D in semaphorin signaling	1	MET
Sema4D mediated inhibition of cell attachment and migration	1	MET
Axon guidance	1	MET
VEGFA-VEGFR2 Pathway	1	KDR
VEGFR2 mediated cell proliferation	1	KDR
Diseases of signal transduction by growth factor receptors and second messengers	1	MET
Infectious disease	1	MET
MAPK family signaling cascades	1	MET
MAPK1/MAPK3 signaling	1	MET
Signaling by MET	1	MET
MET Receptor Activation	1	MET
Negative regulation of MET activity	1	MET
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	1	MET
RNA Polymerase II Transcription	1	MET
Gene expression (Transcription)	1	MET
MET activates RAS signaling	1	MET
MET activates PI3K/AKT signaling	1	MET

Dominant GO biological processes

GO term	Targets
cell surface receptor protein tyrosine kinase signaling pathway	3
protein phosphorylation	3
positive regulation of cell migration	2
positive regulation of MAPK cascade	2
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	2
semaphorin-plexin signaling pathway	2
positive regulation of endothelial cell chemotaxis	2
branching morphogenesis of an epithelial tube	2
neuron differentiation	2
signal transduction	2
angiogenesis	1
ovarian follicle development	1
branching involved in blood vessel morphogenesis	1
vasculogenesis	1
positive regulation of protein phosphorylation	1

Indications & clinical

Indications

57 indications (2 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
renal cell carcinoma	3	MONDO:0005086	EFO:0000681
non-small cell lung carcinoma	3	MONDO:0005233	EFO:0003060
hepatocellular carcinoma	3	MONDO:0007256	EFO:0000182
clear cell renal carcinoma	3	MONDO:0005005	EFO:0000349
chromophobe renal cell carcinoma	3	MONDO:0017885	EFO:0000335
papillary renal cell carcinoma	3	MONDO:0017884	EFO:0000640
thyroid gland papillary carcinoma	3	MONDO:0005075	EFO:0000641
collecting duct carcinoma	3	MONDO:0005220	EFO:0003016
renal carcinoma	3	MONDO:0005206	EFO:0002890
thyroid gland carcinoma	3	MONDO:0015075	EFO:0002892
renal cell adenocarcinoma	3	MONDO:0005549	EFO:0005708
prostate adenocarcinoma	2	MONDO:0005082	EFO:0000673
glioblastoma	2	MONDO:0018177	EFO:0000519
melanoma	2	MONDO:0005105	EFO:0000756
anaplastic astrocytoma	2	MONDO:0016684	EFO:0002499
exocrine pancreatic carcinoma	2	MONDO:0005192	EFO:0002618
thyroid gland follicular carcinoma	2	MONDO:0005034	EFO:0000501
metastatic melanoma	2	MONDO:0005191	EFO:0002617
urothelial carcinoma	2	MONDO:0040679	EFO:0008528
adrenal cortex carcinoma	2	MONDO:0006639	EFO:1000796
carcinoid tumor	2	MONDO:0005369	EFO:0004243
uterine carcinosarcoma	2	MONDO:0006485	EFO:1000613
intrahepatic cholangiocarcinoma	2	MONDO:0003210	EFO:1001961
soft tissue sarcoma	2	MONDO:0018078	EFO:1001968
salivary gland cancer	2	MONDO:0004669	MONDO:0004669
breast neoplasm	2	MONDO:0021100	MONDO:0007254
neuroendocrine neoplasm	2	MONDO:0019496	EFO:1001901
neuroendocrine carcinoma	2	MONDO:0002120	MONDO:0002120
lung neuroendocrine neoplasm	2	MONDO:0005454	EFO:0005220
rectal cancer	2	MONDO:0006519	EFO:1000657
colon adenocarcinoma	2	MONDO:0002271	EFO:1001949
carcinoma	2	MONDO:0004993	EFO:0000313
cutaneous melanoma	2	MONDO:0005012	EFO:0000389
osteosarcoma	2	MONDO:0009807	EFO:0000637
kidney cancer	2	MONDO:0002367	MONDO:0002367
gastrointestinal stromal tumor	2	MONDO:0011719	MONDO:0011719
meningioma	2	MONDO:0016642	MONDO:0016642
colorectal adenocarcinoma	2	MONDO:0005008	EFO:0000365
bile duct carcinoma	2	MONDO:0005496	EFO:0005540
malignant pancreatic neoplasm	2	MONDO:0009831	EFO:1000359
colorectal neoplasm	2	MONDO:0005335	MONDO:0005575
lung neoplasm	2	MONDO:0021117	MONDO:0008903
plasma cell myeloma	1	MONDO:0009693	EFO:0001378
liver disorder	1	MONDO:0005154	EFO:0001421
acute myeloid leukemia	1	MONDO:0018874	EFO:0000222
squamous cell carcinoma	1	MONDO:0005096	EFO:0000707
gliosarcoma	1	MONDO:0016681	EFO:1001465

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

Clinical trials

Total trials: 254.

Phase distribution

Phase	Trials
PHASE2	148
PHASE1	44
PHASE3	26
PHASE1/PHASE2	20
Not specified	9
PHASE4	5
PHASE2/PHASE3	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT01896479	PHASE4	ACTIVE_NOT_RECRUITING	A Study of Two Different Doses of Cabozantinib (XL184) in Progressive, Metastatic Medullary Thyroid Cancer
NCT06934057	PHASE4	RECRUITING	Cabozantinib and Nivolumab Among Older Patients With Renal Cell Carcinoma
NCT07010393	PHASE4	NOT_YET_RECRUITING	Genotype-Driven Neoadjuvant Therapy for Locally Advanced Thyroid Cancer: A Real-World Cohort Study
NCT07028125	PHASE4	RECRUITING	Digital Monitoring of Self-reported Symptoms by Patients Treated With Cabozantinib Plus Nivolumab for Advanced Clear-cell Renal Carcinoma
NCT03963206	PHASE4	COMPLETED	Cabozantinib toLERANCE Study in HepatoCellular Carcinoma (CLERANCE)
NCT03141177	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Nivolumab Combined With Cabozantinib Compared to Sunitinib in Previously Untreated Advanced or Metastatic Renal Cell Carcinoma
NCT03375320	PHASE3	ACTIVE_NOT_RECRUITING	Testing Cabozantinib in Patients With Advanced Pancreatic Neuroendocrine and Carcinoid Tumors
NCT03690388	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Cabozantinib Compared With Placebo in Subjects With Radioiodine-refractory Differentiated Thyroid Cancer Who Have Progressed After Prior Vascular Endothelial Growth Factor Receptor (VEGFR) -Targeted Therapy
NCT03755791	PHASE3	ACTIVE_NOT_RECRUITING	Study of Cabozantinib in Combination With Atezolizumab Versus Sorafenib in Participants With Advanced Hepatocellular Carcinoma (HCC) Who Have Not Received Previous Systemic Anticancer Therapy
NCT03768063	PHASE3	ACTIVE_NOT_RECRUITING	A Study in Patients Previously Enrolled in a Genentech and/or F. Hoffmann-La Roche Ltd Sponsored Atezolizumab Study
NCT03793166	PHASE3	ACTIVE_NOT_RECRUITING	Immunotherapy With Nivolumab and Ipilimumab Followed by Nivolumab or Nivolumab With Cabozantinib for Patients With Advanced Kidney Cancer, The PDIGREE Study
NCT03937219	PHASE3	ACTIVE_NOT_RECRUITING	Study of Cabozantinib in Combination With Nivolumab and Ipilimumab in Patients With Previously Untreated Advanced or Metastatic Renal Cell Carcinoma
NCT04211337	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Selpercatinib (LY3527723) in Participants With RET-Mutant Medullary Thyroid Cancer
NCT04446117	PHASE3	ACTIVE_NOT_RECRUITING	Study of Cabozantinib in Combination With Atezolizumab Versus Second NHT in Subjects With mCRPC
NCT04586231	PHASE3	ACTIVE_NOT_RECRUITING	A Study of Belzutifan (MK-6482) in Combination With Lenvatinib Versus Cabozantinib for Treatment of Renal Cell Carcinoma (MK-6482-011)
NCT05092958	PHASE3	ACTIVE_NOT_RECRUITING	Testing the Addition of the Anti-cancer Drug, Cabozantinib, to the Usual Immunotherapy Treatment, Avelumab, in Patients With Metastatic Urothelial Cancer, MAIN-CAV Study
NCT05691478	PHASE2/PHASE3	RECRUITING	A Study to Test the Addition of the Drug Cabozantinib to Chemotherapy in Patients With Newly Diagnosed Osteosarcoma
NCT06364631	PHASE3	RECRUITING	CARE1 Pragmatic Clinical Trial
NCT06475989	PHASE3	RECRUITING	Study of Targeted Therapy vs. Chemotherapy in Patients With Thyroid Cancer
NCT07011719	PHASE3	RECRUITING	Study of Casdatifan and Cabozantinib Versus Placebo and Cabozantinib in Patients With Advanced Clear Cell Renal Cell Carcinoma
NCT07227402	PHASE3	RECRUITING	A Clinical Study of Belzutifan and Zanzalintinib in People With Recurrent Kidney Cancer Following Adjuvant Therapy (MK-6482-033)
NCT07383441	PHASE3	NOT_YET_RECRUITING	Adding Biotherapy or Placebo to Standard Treatment for Advanced Kidney Cancer
NCT07405164	PHASE3	RECRUITING	Extension Study for Participants in Studies That Include Belzutifan (MK-6482-043/LITESPARK-043)
NCT00704730	PHASE3	COMPLETED	Efficacy of XL184 (Cabozantinib) in Advanced Medullary Thyroid Cancer
NCT01522443	PHASE3	TERMINATED	Study of Cabozantinib (XL184) Versus Mitoxantrone Plus Prednisone in Men With Previously Treated Symptomatic Castration-resistant Prostate Cancer
NCT01605227	PHASE3	COMPLETED	Study of Cabozantinib (XL184) Versus Prednisone in Men With Metastatic Castration-resistant Prostate Cancer Previously Treated With Docetaxel and Abiraterone or MDV3100
NCT01865747	PHASE3	COMPLETED	A Study of Cabozantinib (XL184) vs Everolimus in Subjects With Metastatic Renal Cell Carcinoma
NCT01908426	PHASE3	COMPLETED	Study of Cabozantinib (XL184) vs Placebo in Subjects With Hepatocellular Carcinoma Who Have Received Prior Sorafenib
NCT03729245	PHASE3	TERMINATED	A Study of Bempegaldesleukin (NKTR-214: BEMPEG) in Combination With Nivolumab Compared With the Investigator’s Choice of a Tyrosine Kinase Inhibitor (TKI) Therapy (Either Sunitinib or Cabozantinib Monotherapy) for Advanced Metastatic Renal Cell Carcinoma (RCC)
NCT04338269	PHASE3	TERMINATED	A Study of Atezolizumab in Combination With Cabozantinib Compared to Cabozantinib Alone in Participants With Advanced Renal Cell Carcinoma After Immune Checkpoint Inhibitor Treatment
NCT04471428	PHASE3	COMPLETED	Study of Atezolizumab in Combination With Cabozantinib Versus Docetaxel in Patients With Metastatic Non-Small Cell Lung Cancer Previously Treated With an Anti-PD-L1/PD-1 Antibody and Platinum-Containing Chemotherapy
NCT04760288	PHASE3	WITHDRAWN	A Study of Pralsetinib Versus Standard of Care (SOC) for Treatment of RET-Mutated Medullary Thyroid Cancer (MTC).
NCT01639508	PHASE2	RECRUITING	Cabozantinib in Patients With RET Fusion-Positive Advanced Non-Small Cell Lung Cancer and Those With Other Genotypes: ROS1 or NTRK Fusions or Increased MET or AXL Activity
NCT01708954	PHASE2	ACTIVE_NOT_RECRUITING	Erlotinib Hydrochloride and Cabozantinib-s-Malate Alone or in Combination as Second or Third Line Therapy in Treating Patients With Stage IV Non-small Cell Lung Cancer
NCT02243605	PHASE2	ACTIVE_NOT_RECRUITING	Cabozantinib S-malate in Treating Patients With Relapsed Osteosarcoma or Ewing Sarcoma
NCT02867592	PHASE2	ACTIVE_NOT_RECRUITING	Cabozantinib-S-Malate in Treating Younger Patients With Recurrent, Refractory, or Newly Diagnosed Sarcomas, Wilms Tumor, or Other Rare Tumors
NCT02925234	PHASE2	RECRUITING	The Drug Rediscovery Protocol (DRUP Trial)
NCT03367741	PHASE2	ACTIVE_NOT_RECRUITING	Cabozantinib S-malate and Nivolumab in Treating Patients With Advanced, Recurrent, or Metastatic Endometrial Cancer
NCT03468218	PHASE2	ACTIVE_NOT_RECRUITING	Pembrolizumab & Cabozantinib in Patients With Head and Neck Squamous Cell Cancer
NCT03539822	PHASE1/PHASE2	RECRUITING	Cabozantinib Plus Durvalumab With or Without Tremelimumab in Patients With Gastroesophageal Cancer and Other Gastrointestinal Malignancies

Clinical evidence (CIViC)

Variant × indication × effect (18 predictive associations from 18 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
GNA11 Mutation	Uveal Melanoma	Sensitivity/Response	Cabozantinib	CIViC B	EID3049
GNAQ Mutation	Uveal Melanoma	Sensitivity/Response	Cabozantinib	CIViC B	EID5068
RET Fusion	Lung Adenocarcinoma	Sensitivity/Response	Cabozantinib	CIViC B	EID4847
RET M918T	Medullary Thyroid Carcinoma	Sensitivity/Response	Cabozantinib	CIViC B	EID7710
RET Mutation	Medullary Thyroid Carcinoma	Sensitivity/Response	Cabozantinib	CIViC B	EID8984
MET D1228V	Lung Non-small Cell Carcinoma	Sensitivity/Response	Cabozantinib	CIViC C	EID1864
MET Exon 14 Skipping Mutation	Lung Adenocarcinoma	Sensitivity/Response	Cabozantinib	CIViC C	EID11400
MET Exon 14 Skipping Mutation	Lung Adenocarcinoma	Sensitivity/Response	Cabozantinib + Crizotinib	CIViC C	EID11410
NOT MET Amplification AND MET Exon 14 Skipping Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Cabozantinib + Crizotinib	CIViC C	EID11390
RBPMS::MET Fusion	Congenital Fibrosarcoma	Sensitivity/Response	Cabozantinib	CIViC C	EID8892
ROS1 D2033N	Lung Non-small Cell Carcinoma	Sensitivity/Response	Cabozantinib	CIViC C	EID7691
KDR R1032Q	Colorectal Cancer	Sensitivity/Response	Lenvatinib + Axitinib + Cabozantinib + Dovitinib	CIViC D	EID9339
MET Amplification	Gastric Adenocarcinoma	Sensitivity/Response	Cabozantinib	CIViC D	EID7873
MET Overexpression	Ovarian Clear Cell Carcinoma	Sensitivity/Response	Cabozantinib	CIViC D	EID7932
PIK3CA Mutation	Colorectal Cancer	Sensitivity/Response	Cabozantinib	CIViC D	EID771
ROS1 G2032R AND CD74::ROS1 Fusion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Cabozantinib	CIViC D	EID1101
ROS1 G2032R AND CD74::ROS1 Fusion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Foretinib + Cabozantinib	CIViC D	EID1249
KIF5B::RET Fusion AND RET V804L	Lung Non-small Cell Carcinoma	Resistance	Cabozantinib	CIViC D	EID4851

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline, but PharmGKB curates 0 clinical and 3 variant annotation(s) for this drug (gene-keyed; see PharmGKB).

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.

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

Molecule	Source	Status	Shared targets
Afatinib	ChEMBL + PubChem	Phase 4 (approved)	KDR, MET, RET
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	KDR, MET, RET
GEFITINIB	ChEMBL + PubChem	Phase 4 (approved)	KDR, MET, RET
PAZOPANIB	ChEMBL + PubChem	Phase 4 (approved)	KDR, MET, RET
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	KDR, MET, RET
AXITINIB	ChEMBL	Phase 4 (approved)	KDR, MET, RET
BRIGATINIB	ChEMBL	Phase 4 (approved)	KDR, MET, RET
CERITINIB	ChEMBL	Phase 4 (approved)	KDR, MET, RET
ENTRECTINIB	ChEMBL	Phase 4 (approved)	KDR, MET, RET
ERLOTINIB	ChEMBL	Phase 4 (approved)	KDR, MET, RET
FEDRATINIB	ChEMBL	Phase 4 (approved)	KDR, MET, RET
INFIGRATINIB	ChEMBL	Phase 4 (approved)	KDR, MET, RET
MIDOSTAURIN	ChEMBL	Phase 4 (approved)	KDR, MET, RET
NINTEDANIB	ChEMBL	Phase 4 (approved)	KDR, MET, RET
SORAFENIB	ChEMBL	Phase 4 (approved)	KDR, MET, RET
SUNITINIB	ChEMBL	Phase 4 (approved)	KDR, MET, RET
TIVOZANIB	ChEMBL	Phase 4 (approved)	KDR, MET, RET
VANDETANIB	ChEMBL	Phase 4 (approved)	KDR, MET, RET
CANERTINIB	ChEMBL	Phase 3	KDR, MET, RET
CEDIRANIB	ChEMBL	Phase 3	KDR, MET, RET
LESTAURTINIB	ChEMBL	Phase 3	KDR, MET, RET
LINIFANIB	ChEMBL	Phase 3	KDR, MET, RET
QUERCETIN	ChEMBL	Phase 3	KDR, MET, RET
AT-9283	ChEMBL	Phase 2	KDR, MET, RET
BEMCENTINIB	ChEMBL	Phase 2	KDR, MET, RET
BMS-777607	ChEMBL	Phase 2	KDR, MET, RET
CENISERTIB	ChEMBL	Phase 2	KDR, MET, RET
CEP-32496	ChEMBL	Phase 2	KDR, MET, RET
DEFOSBARASERTIB	ChEMBL	Phase 2	KDR, MET, RET
FORETINIB	ChEMBL	Phase 2	KDR, MET, RET
GOLVATINIB	ChEMBL	Phase 2	KDR, MET, RET
ILORASERTIB	ChEMBL	Phase 2	KDR, MET, RET
MERESTINIB	ChEMBL	Phase 2	KDR, MET, RET
MK-2461	ChEMBL	Phase 2	KDR, MET, RET
OSI-632	ChEMBL	Phase 2	KDR, MET, RET
R-406	ChEMBL	Phase 2	KDR, MET, RET
RAF-265	ChEMBL	Phase 2	KDR, MET, RET
REBASTINIB	ChEMBL	Phase 2	KDR, MET, RET
SU-014813	ChEMBL	Phase 2	KDR, MET, RET
TOZASERTIB	ChEMBL	Phase 2	KDR, MET, RET
Binimetinib	PubChem	Approved	KDR, MET, RET
Selumetinib	PubChem	Approved	KDR, MET, RET
Fostamatinib	ChEMBL + PubChem	Phase 4 (approved)	MET, RET
SELPERCATINIB	ChEMBL + PubChem	Phase 4 (approved)	KDR, RET
ALECTINIB	ChEMBL	Phase 4 (approved)	KDR, RET
BOSUTINIB	ChEMBL	Phase 4 (approved)	MET, RET
DASATINIB	ChEMBL	Phase 4 (approved)	KDR, RET
IBRUTINIB	ChEMBL	Phase 4 (approved)	KDR, RET
LENVATINIB	ChEMBL	Phase 4 (approved)	KDR, RET
NERATINIB	ChEMBL	Phase 4 (approved)	KDR, MET
PALBOCICLIB	ChEMBL	Phase 4 (approved)	MET, RET
PONATINIB	ChEMBL	Phase 4 (approved)	KDR, RET
QUIZARTINIB	ChEMBL	Phase 4 (approved)	KDR, RET
TOFACITINIB	ChEMBL	Phase 4 (approved)	KDR, RET
UPADACITINIB	ChEMBL	Phase 4 (approved)	KDR, RET
VEMURAFENIB	ChEMBL	Phase 4 (approved)	KDR, RET
ALISERTIB	ChEMBL	Phase 3	KDR, RET
BARASERTIB	ChEMBL	Phase 3	KDR, RET
BRIVANIB	ChEMBL	Phase 3	KDR, RET
DEFACTINIB	ChEMBL	Phase 3	KDR, RET