Ceritinib

Summary

Ceritinib (CHEMBL2403108) is an approved small-molecule antineoplastic agent (ATC L01ED02) targeting INSR, IGF1R, and FLT3; indicated across 13 conditions including non-small cell lung carcinoma and neoplasm; with CIViC clinical evidence for 33 variant-indication associations (e.g. ALK Fusion in lung non-small cell carcinoma).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: L01ED02
• Targets: 5 (INSR, IGF1R, FLT3…)
• Indications: 13 conditions
• Clinical trials: 45
• Precision-oncology evidence (CIViC): 33 variant–indication associations
• Chemistry: 558.1 Da · C28H36ClN5O3S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL2403108
Name	Ceritinib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	57379345
ChEBI	CHEBI:78432
ATC	L01ED02
Molecular formula	C28H36ClN5O3S
Molecular weight	558.1
InChIKey	VERWOWGGCGHDQE-UHFFFAOYSA-N

SMILES: CC1=CC(=C(C=C1C2CCNCC2)OC(C)C)NC3=NC=C(C(=N3)NC4=CC=CC=C4S(=O)(=O)C(C)C)Cl

IUPAC name: 5-chloro-2-N-(5-methyl-4-piperidin-4-yl-2-propan-2-yloxyphenyl)-4-N-(2-propan-2-ylsulfonylphenyl)pyrimidine-2,4-diamine

ChEBI definition: A member of the class of aminopyrimidines that is 2,6-diamino-5-chloropyrimidine in which the amino groups at positions 2 and 6 are respectively carrying 2-methoxy-4-(piperidin-4-yl)-5-methylphenyl and 2-(isopropylsulfonyl)phenyl substituents. Used for the treatment of ALK-positive metastatic non-small cell lung cancer.

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

Also known as: Ceritinib, Ceritinib[mi], LDK-378, LDK378, Zykadia, CERITINIB, 4MK, CPD 15, LDK 378, ZYKADIA, CERITINIB[MI], CERITINIB (LDK378)

Parent form; salt/anhydrous children: CHEMBL4468931, CHEMBL4476089, CHEMBL4542506

Patent coverage: 3,701 distinct patent families (8,551 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 8,010 (94%) 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
INSR	Insulin receptor	Inhibition	8.15	0.8%	P06213
IGF1R	Insulin-like growth factor I receptor	Inhibition	8.1	19%	P08069
FLT3	fms related receptor tyrosine kinase 3	Inhibition	7.22	0.9%	P36888
ALK	ALK receptor tyrosine kinase	Inhibition	9.7	0.8%	Q9UM73
TSSK1B	testis specific serine kinase 1B	Inhibition	7.64	0.3%	Q9BXA7

Broader ChEMBL bioactivity targets: 53 (assay-derived). Sample: Tyrosine-protein kinase ABL1, Mast/stem cell growth factor receptor Kit, Insulin-like growth factor 1 receptor, Receptor-type tyrosine-protein kinase FLT3, Insulin receptor, Platelet-derived growth factor receptor alpha, Epidermal growth factor receptor, Proto-oncogene tyrosine-protein kinase ROS, Proto-oncogene tyrosine-protein kinase receptor Ret, NPM/ALK (Nucleophosmin/ALK tyrosine kinase receptor).

Bioactivity

ChEMBL activities: 197 potent at pChembl ≥ 5 of 205 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ALK	9.7	IC50	0.2	nM	CHEMBL_ACT_13367230
ALK	9.7	IC50	0.2	nM	CHEMBL_ACT_13374067
ALK	9.7	IC50	0.2	nM	CHEMBL_ACT_24815754
ALK	9.6	IC50	0.25	nM	CHEMBL_ACT_23239917
ROS1	9.4	Ki	0.4	nM	CHEMBL_ACT_18761175
ROS1	9.4	Ki	0.4	nM	CHEMBL_ACT_26314130
ALK	9.21	IC50	0.61	nM	CHEMBL_ACT_22775264
ROS1	9.15	Ki	0.7	nM	CHEMBL_ACT_18761174
ROS1	9.15	Ki	0.7	nM	CHEMBL_ACT_26314019
ALK	9.08	IC50	0.83	nM	CHEMBL_ACT_24853442
ALK	9	IC50	1	nM	CHEMBL_ACT_26776982
ALK	8.96	IC50	1.1	nM	CHEMBL_ACT_22775388
ALK	8.92	IC50	1.2	nM	CHEMBL_ACT_24853429
ALK	8.89	Kd	1.3	nM	CHEMBL_ACT_18415018
ALK	8.85	IC50	1.4	nM	CHEMBL_ACT_17952575
ALK	8.82	IC50	1.5	nM	CHEMBL_ACT_17952579
ALK	8.8	IC50	1.6	nM	CHEMBL_ACT_22775392
EML4	8.75	IC50	1.79	nM	CHEMBL_ACT_29088286
ALK	8.72	IC50	1.9	nM	CHEMBL_ACT_22775384
ROS1	8.7	IC50	2	nM	CHEMBL_ACT_16808349
ALK	8.7	IC50	2	nM	CHEMBL_ACT_17952581
ROS1	8.7	IC50	2	nM	CHEMBL_ACT_18332200
ALK	8.7	IC50	2	nM	CHEMBL_ACT_19026264
ROS1	8.7	IC50	2	nM	CHEMBL_ACT_22416681
ALK	8.68	IC50	2.1	nM	CHEMBL_ACT_22820304
ALK	8.66	IC50	2.2	nM	CHEMBL_ACT_13367201
ROS1	8.66	IC50	2.2	nM	CHEMBL_ACT_22927955
ALK	8.64	IC50	2.3	nM	CHEMBL_ACT_16808329
ALK	8.64	IC50	2.3	nM	CHEMBL_ACT_19026255
ALK	8.62	IC50	2.4	nM	CHEMBL_ACT_22416952

Target pathways

Aggregated over 5 target gene(s): INSR, IGF1R, FLT3, ALK, TSSK1B.

Top Reactome pathways

56 total, by targets touching each:

Pathway	Targets	Genes
PIP3 activates AKT signaling	2	FLT3, INSR
Signal Transduction	2	ALK, INSR
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling	2	FLT3, INSR
Signaling by Receptor Tyrosine Kinases	2	ALK, INSR
PI3K Cascade	1	FLT3
Disease	1	ALK
Negative regulation of the PI3K/AKT network	1	INSR
Signaling by ALK	1	ALK
Constitutive Signaling by Aberrant PI3K in Cancer	1	FLT3
Signaling by Type 1 Insulin-like Growth Factor 1 Receptor (IGF1R)	1	IGF1R
IRS-related events triggered by IGF1R	1	IGF1R
SHC-related events triggered by IGF1R	1	IGF1R
Diseases of signal transduction by growth factor receptors and second messengers	1	ALK
RAF/MAP kinase cascade	1	FLT3
IRS activation	1	INSR
Signal attenuation	1	INSR
Insulin receptor signalling cascade	1	INSR
Signaling by Insulin receptor	1	INSR
Insulin receptor recycling	1	INSR
Intracellular signaling by second messengers	1	INSR
Extra-nuclear estrogen signaling	1	IGF1R
FLT3 Signaling	1	FLT3
STAT5 Activation	1	FLT3
Signaling by ALK in cancer	1	ALK
ALK mutants bind TKIs	1	ALK
Drug resistance of ALK mutants	1	ALK
FLT3 mutants bind TKIs	1	FLT3
STAT5 activation downstream of FLT3 ITD mutants	1	FLT3
KW2449-resistant FLT3 mutants	1	FLT3
semaxanib-resistant FLT3 mutants	1	FLT3

Dominant GO biological processes

GO term	Targets
protein phosphorylation	5
protein autophosphorylation	4
cell surface receptor protein tyrosine kinase signaling pathway	4
positive regulation of cell population proliferation	3
positive regulation of MAPK cascade	3
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	3
insulin receptor signaling pathway	2
positive regulation of cell migration	2
positive regulation of protein-containing complex disassembly	2
dendritic spine maintenance	2
amyloid-beta clearance	2
signal transduction	2
peptidyl-tyrosine autophosphorylation	2
regulation of apoptotic process	2
positive regulation of receptor internalization	1

Indications & clinical

Indications

13 indications (3 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
non-small cell lung carcinoma	4	MONDO:0005233	EFO:0003060
neoplasm	4	MONDO:0005070	EFO:0000616
soft tissue sarcoma	3	MONDO:0018078	EFO:1001968
anaplastic large cell lymphoma	2	MONDO:0020325	EFO:0003032
cutaneous melanoma	2	MONDO:0005012	EFO:0000389
glioblastoma	2	MONDO:0018177	EFO:0000519
neuroblastoma	2	MONDO:0005072	EFO:0000621
melanoma	2	MONDO:0005105	EFO:0000756
cholangiocarcinoma	2	MONDO:0019087	EFO:0005221
inflammatory myofibroblastic tumor	2	MONDO:0015798	MONDO:0015798
liver disorder	1	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: 45.

Phase distribution

Phase	Trials
PHASE2	17
PHASE1	15
Not specified	6
PHASE3	3
PHASE1/PHASE2	2
PHASE4	1
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02584933	PHASE4	ACTIVE_NOT_RECRUITING	Roll-over Study to Allow Access to Certinib (LDK378) for Patients Who Are on Ceritinib Treatment in a Novartis-sponsored Study
NCT01828099	PHASE3	COMPLETED	LDK378 Versus Chemotherapy in Previously Untreated Patients With ALK Rearranged Non-small Cell Lung Cancer
NCT01828112	PHASE3	COMPLETED	LDK378 Versus Chemotherapy in ALK Rearranged (ALK Positive) Patients Previously Treated With Chemotherapy (Platinum Doublet) and Crizotinib
NCT03784014	PHASE3	COMPLETED	Molecular Profiling of Advanced Soft-tissue Sarcomas
NCT02559778	PHASE2	RECRUITING	Pediatric Precision Laboratory Advanced Neuroblastoma Therapy
NCT06813079	PHASE2	NOT_YET_RECRUITING	Using Tumor Models to Determine Treatments
NCT01685060	PHASE2	COMPLETED	LDK378 in Adult Patients With ALK-activated NSCLC Previously Treated With Chemotherapy and Crizotinib
NCT01685138	PHASE2	COMPLETED	LDK378 in Crizotinib naïve Adult Patients With ALK-activated Non-small Cell Lung Cancer
NCT01964157	PHASE2	UNKNOWN	An Open-label, Multicenter, Phase II Study of LDK378 in Patients With Non-small Cell Lung Cancer Harboring ROS1 Rearrangement
NCT02040870	PHASE1/PHASE2	COMPLETED	LDK378 in Adult Chinese Patients With ALK-rearranged (ALK-positive) Advanced Non-small Cell Lung Cancer (NSCLC) Previously Treated With Crizotinib
NCT02186821	PHASE2	TERMINATED	Ceritinib (LDK378) for Patients Whose Tumors Have Aberrations in ALK or ROS1 (SIGNATURE)
NCT02276027	PHASE2	COMPLETED	A Phase II, Open Label, Multiple Arm Study of AUY922, BYL719, INC280, LDK378 and MEK162 in Chinese Patients With Advanced Non-small Cell Lung Cancer
NCT02289144	PHASE2	WITHDRAWN	Ceritinib in Mutation and Oncogene Directed Therapy in Thyroid Cancer
NCT02336451	PHASE2	COMPLETED	A Phase II Study to Evaluate the Efficacy and Safety of Oral Ceritinib in Patients With ALK-positive NSCLC Metastatic to the Brain and/or to Leptomeninges
NCT02343679	PHASE2	WITHDRAWN	Novartis PhII Ceritinib (LDK378) in R/R ALK+ Hem Malignancies
NCT02374489	PHASE2	TERMINATED	A Phase II Trial of LDK378 in ROS1 and /or ALK Over-expressed Advanced Intrahepatic or Hilar Cholangiocarcinoma
NCT02450903	PHASE2	COMPLETED	LDK378 in Patients With ALK Positive NSCLC Previously Treated With Alectinib.
NCT02465528	PHASE2	TERMINATED	Ceritinib Rare Indications Study in ALK+ Tumors
NCT02513667	PHASE2	TERMINATED	Ceritinib in Combination With Stereotactic Ablative Radiation Metastatic Lung Adenocarcinoma
NCT02587650	PHASE2	TERMINATED	Capmatinib, Ceritinib, Regorafenib, or Entrectinib in Treating Patients With BRAF/NRAS Wild-Type Stage III-IV Melanoma
NCT02638909	PHASE2	TERMINATED	Study of Oral Ceritinib in Patients With ALK and ROS1 Activated Gastrointestinal Malignancies
NCT02729961	PHASE1/PHASE2	WITHDRAWN	Ceritinib With Brentuximab Vedotin in Treating Patients With ALK-Positive Anaplastic Large Cell Lymphoma
NCT03737994	PHASE2	TERMINATED	Targeted Treatment for ALK Positive Patients Who Have Previously Been Treated for Non-squamous Non-small Cell Lung Cancer
NCT02321501	PHASE1	ACTIVE_NOT_RECRUITING	Ceritinib and Everolimus in Treating Patients With Locally Advanced or Metastatic Solid Tumors or Stage IIIB-IV Non-small Cell Lung Cancer
NCT02393625	PHASE1	ACTIVE_NOT_RECRUITING	Study of Safety and Efficacy of Ceritinib in Combination With Nivolumab in Patients With ALK-positive Non-small Cell Lung Cancer
NCT03611738	PHASE1	ACTIVE_NOT_RECRUITING	Ceritinib Plus Docetaxel in ALK-Negative, EGFR WT Advanced NSCLC
NCT01283516	PHASE1	COMPLETED	A Dose Escalation/Expansion Study of LDK378 in Patients With Tumors Characterized by Genetic Abnormalities in Anaplastic Lymphoma Kinase
NCT01634763	PHASE1	COMPLETED	Study of Safety and Preliminary Efficacy for LDK378 in Japanese Patients With Genetic Alterations in Anaplastic Lymphoma Kinase (ALK)
NCT01742286	PHASE1	COMPLETED	Phase I Study of LDK378 in Pediatric, Malignancies With a Genetic Alteration in Anaplastic Lymphoma Kinase (ALK)
NCT01772797	PHASE1	COMPLETED	Phase Ib Study of LDK378 and AUY922 in ALK-rearranged Non-small Cell Lung Cancer
NCT01950481	PHASE1	COMPLETED	Effect of Hepatic Impairment on LDK378 Pharmacokinetics
NCT02227940	PHASE1	COMPLETED	Ceritinib and Combination Chemotherapy in Treating Patients With Advanced Solid Tumors or Locally Advanced or Metastatic Pancreatic Cancer
NCT02292550	PHASE1	COMPLETED	Study of Safety and Efficacy of LEE011 and Ceritinib in Patients With ALK-positive Non-small Cell Lung Cancer.
NCT02299505	PHASE1	COMPLETED	Pharmacokinetic and Safety Study of Lower Doses of Ceritinib Taken With a Low-fat Meal Versus 750 mg of Ceritinib in the Fasted State in Adult Patients With (ALK-positive) Metastatic Non-small Cell Lung Cancer (NSCLC)
NCT02422589	PHASE1	COMPLETED	A Phase I, Multi-center, Open Label, Drug-drug Interaction Study to Assess the Effect of Ceritinib on the Pharmacokinetics of Warfarin and Midazolam in Patients With ALK-positive Advanced Tumors
NCT02780128	PHASE1	TERMINATED	Next Generation Personalized Neuroblastoma Therapy
NCT03087448	PHASE1	TERMINATED	Ceritinib + Trametinib in Patients With Advanced ALK-Positive Non-Small Cell Lung Cancer (NSCLC)
NCT03501368	PHASE1	COMPLETED	Study of Trametinib + Ceritinib in Patients With Unresectable Melanoma
NCT02605746	EARLY_PHASE1	COMPLETED	Preoperative Ceritinib (LDK378) in Glioblastoma Multiforme and CNS Metastasis
NCT05467189	Not specified	RECRUITING	Antineoplastic Drugs in Elderly Patients

Clinical evidence (CIViC)

Variant × indication × effect (33 predictive associations from 40 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
ALK Fusion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Ceritinib	CIViC A	EID11190 +3
ALK Fusion	Inflammatory Myofibroblastic Tumor	Sensitivity/Response	Ceritinib	CIViC B	EID11291 +1
ALK Mutation	Lung Non-small Cell Carcinoma	Sensitivity/Response	Ceritinib	CIViC B	EID1237
ROS1 Fusion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Ceritinib	CIViC B	EID11334
ALK I1171	Lung Non-small Cell Carcinoma	Sensitivity/Response	Ceritinib	CIViC C	EID1284 +2
ALK Fusion AND ALK L1196M	Lung Non-small Cell Carcinoma	Sensitivity/Response	Ceritinib	CIViC C	EID2343 +1
ALK Fusion	Anaplastic Large Cell Lymphoma	Sensitivity/Response	Ceritinib	CIViC C	EID7546
ALK I1171T	Neuroblastoma	Sensitivity/Response	Ceritinib	CIViC C	EID9404
ALK S1206Y AND v::ALK Fusion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Ceritinib	CIViC C	EID2865
CD72::ROS1 Fusion	Lung Adenocarcinoma	Sensitivity/Response	Ceritinib	CIViC C	EID1248
EML4::ALK Fusion AND ALK F1245C	Lung Non-small Cell Carcinoma	Sensitivity/Response	Ceritinib	CIViC C	EID1338
STRN::ALK Fusion	Colon Adenocarcinoma	Sensitivity/Response	Ceritinib	CIViC C	EID5952
EML4::ALK Fusion AND ALK C1156Y	Lung Non-small Cell Carcinoma	Resistance	Ceritinib + Luminespib + Crizotinib	CIViC C	EID841
EML4::ALK Fusion AND ALK G1202del	Lung Non-small Cell Carcinoma	Resistance	Ceritinib	CIViC C	EID7599
ALK Alternative Transcript (ATI)	Melanoma	Sensitivity/Response	Ceritinib + Crizotinib + Alectinib + ALK Inhibitor ASP3026 + Entrectinib	CIViC D	EID7484
ALK G1269A AND v::ALK Fusion	Lung Non-small Cell Carcinoma	Sensitivity/Response	Ceritinib	CIViC D	EID1342
ALK G1269A AND v::ALK Fusion	Cancer	Sensitivity/Response	Ceritinib	CIViC D	EID1355
EML4::ALK Fusion AND ALK L1196M	Lung Non-small Cell Carcinoma	Sensitivity/Response	Ceritinib	CIViC D	EID1341
EML4::ALK Fusion AND ALK L1196M	Cancer	Sensitivity/Response	Brigatinib + Lorlatinib + Alectinib + Ceritinib	CIViC D	EID7597
EML4::ALK Fusion AND ALK S1206Y	Cancer	Sensitivity/Response	Ceritinib	CIViC D	EID1343
EML4::ALK Fusion AND ALK V1180L	Lung Non-small Cell Carcinoma	Sensitivity/Response	Ceritinib	CIViC D	EID1289
EML4::ALK e6::e20	Lung Non-small Cell Carcinoma	Sensitivity/Response	Ceritinib	CIViC D	EID1340
ALK F1174L AND NPM1::ALK Fusion	Anaplastic Large Cell Lymphoma	Resistance	Ceritinib	CIViC D	EID12658
EML4::ALK Fusion AND ABCB1 Overexpression	Lung Adenocarcinoma	Resistance	Ceritinib + Crizotinib	CIViC D	EID7869
EML4::ALK Fusion AND ALK C1156Y	Cancer	Resistance	Lorlatinib + Alectinib + Ceritinib + Brigatinib	CIViC D	EID7609
EML4::ALK Fusion AND ALK G1202R	Lung Non-small Cell Carcinoma	Resistance	Ceritinib	CIViC D	EID1345
EML4::ALK Fusion AND ALK G1202R AND ALK L1196M	Cancer	Resistance	Brigatinib + Crizotinib + Lorlatinib + Alectinib + Ceritinib	CIViC D	EID7592
EML4::ALK Fusion AND ALK G1202R AND ALK L1198F	Cancer	Resistance	Alectinib + Lorlatinib + Brigatinib + Ceritinib	CIViC D	EID7595
EML4::ALK Fusion AND ALK I1171S	Cancer	Resistance	Ceritinib	CIViC D	EID12657
NPM1::ALK Fusion AND ALK I1171S	Cancer	Resistance	Ceritinib	CIViC D	EID12660

+3 more predictive associations (showing top 30 by level).

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.

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

Molecule	Source	Status	Shared targets
Afatinib	ChEMBL + PubChem	Phase 4 (approved)	ALK, FLT3, IGF1R, INSR, TSSK1B
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	ALK, FLT3, IGF1R, INSR, TSSK1B
FEDRATINIB	ChEMBL + PubChem	Phase 4 (approved)	ALK, FLT3, IGF1R, INSR, TSSK1B
Gefitinib	ChEMBL + PubChem	Phase 4 (approved)	ALK, FLT3, IGF1R, INSR, TSSK1B
Pazopanib	ChEMBL + PubChem	Phase 4 (approved)	ALK, FLT3, IGF1R, INSR, TSSK1B
BRIGATINIB	ChEMBL	Phase 4 (approved)	ALK, FLT3, IGF1R, INSR, TSSK1B
NINTEDANIB	ChEMBL	Phase 4 (approved)	ALK, FLT3, IGF1R, INSR, TSSK1B
SUNITINIB	ChEMBL	Phase 4 (approved)	ALK, FLT3, IGF1R, INSR, TSSK1B
LESTAURTINIB	ChEMBL	Phase 3	ALK, FLT3, IGF1R, INSR, TSSK1B
CENISERTIB	ChEMBL	Phase 2	ALK, FLT3, IGF1R, INSR, TSSK1B
R-406	ChEMBL	Phase 2	ALK, FLT3, IGF1R, INSR, TSSK1B
Idelalisib	PubChem	Approved	ALK, FLT3, IGF1R, INSR, TSSK1B
Selumetinib	PubChem	Approved	ALK, FLT3, IGF1R, INSR, TSSK1B
ENTRECTINIB	ChEMBL	Phase 4 (approved)	ALK, FLT3, IGF1R, INSR
DOVITINIB	ChEMBL	Phase 3	ALK, FLT3, INSR, TSSK1B
BMS-754807	ChEMBL	Phase 2	ALK, FLT3, IGF1R, INSR
FORETINIB	ChEMBL	Phase 2	ALK, FLT3, IGF1R, INSR
ILORASERTIB	ChEMBL	Phase 2	ALK, FLT3, IGF1R, INSR
TOZASERTIB	ChEMBL	Phase 2	ALK, FLT3, IGF1R, INSR
belumosudil	PubChem	Approved	ALK, IGF1R, INSR, TSSK1B
ERLOTINIB	ChEMBL + PubChem	Phase 4 (approved)	ALK, FLT3, TSSK1B
Fostamatinib	ChEMBL + PubChem	Phase 4 (approved)	FLT3, IGF1R, INSR
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	FLT3, IGF1R, INSR
SORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	FLT3, INSR, TSSK1B
VANDETANIB	ChEMBL + PubChem	Phase 4 (approved)	ALK, FLT3, TSSK1B
BOSUTINIB	ChEMBL	Phase 4 (approved)	ALK, FLT3, TSSK1B
INFIGRATINIB	ChEMBL	Phase 4 (approved)	ALK, FLT3, INSR
MIDOSTAURIN	ChEMBL	Phase 4 (approved)	ALK, FLT3, TSSK1B
LINIFANIB	ChEMBL	Phase 3	ALK, FLT3, INSR
LINSITINIB	ChEMBL	Phase 3	FLT3, IGF1R, INSR
QUERCETIN	ChEMBL	Phase 3	ALK, FLT3, IGF1R
OSI-632	ChEMBL	Phase 2	ALK, FLT3, INSR
SU-014813	ChEMBL	Phase 2	ALK, FLT3, INSR
Binimetinib	PubChem	Approved	FLT3, IGF1R, INSR
dacomitinib	PubChem	Approved	FLT3, IGF1R, INSR
Trametinib	PubChem	Approved	FLT3, IGF1R, INSR
ABEMACICLIB	ChEMBL + PubChem	Phase 4 (approved)	FLT3, TSSK1B
DASATINIB	ChEMBL + PubChem	Phase 4 (approved)	FLT3, TSSK1B
LAPATINIB	ChEMBL + PubChem	Phase 4 (approved)	INSR, TSSK1B
QUIZARTINIB	ChEMBL + PubChem	Phase 4 (approved)	FLT3, TSSK1B
RUXOLITINIB	ChEMBL + PubChem	Phase 4 (approved)	ALK, TSSK1B
GILTERITINIB	ChEMBL	Phase 4 (approved)	ALK, FLT3
NERATINIB	ChEMBL	Phase 4 (approved)	FLT3, INSR
OSIMERTINIB	ChEMBL	Phase 4 (approved)	ALK, INSR
PALBOCICLIB	ChEMBL	Phase 4 (approved)	ALK, FLT3
ALVOCIDIB	ChEMBL	Phase 3	ALK, FLT3
CANERTINIB	ChEMBL	Phase 3	ALK, FLT3
CEDIRANIB	ChEMBL	Phase 3	ALK, FLT3
SEMAXANIB	ChEMBL	Phase 3	ALK, FLT3
BEMCENTINIB	ChEMBL	Phase 2	ALK, FLT3
BI-2536	ChEMBL	Phase 2	ALK, FLT3
CEP-11981	ChEMBL	Phase 2	ALK, FLT3
ELLAGIC ACID	ChEMBL	Phase 2	IGF1R, INSR
PELITINIB	ChEMBL	Phase 2	ALK, FLT3
Belzutifan	PubChem	Approved	FLT3, INSR
ALECTINIB	ChEMBL	Phase 4 (approved)	ALK
AXITINIB	ChEMBL	Phase 4 (approved)	FLT3
CABOZANTINIB	ChEMBL	Phase 4 (approved)	FLT3
FILGOTINIB	ChEMBL	Phase 4 (approved)	FLT3
IBRUTINIB	ChEMBL	Phase 4 (approved)	FLT3