Imatinib

Summary

Imatinib (CHEMBL941) is an approved small-molecule tyrosine kinase inhibitor (ATC L01EA01) that acts as a tyrosine-protein kinase ABL inhibitor and platelet-derived growth factor receptor beta inhibitor (+2 more curated mechanisms), targeting ABL1, PDGFRB, and KIT; approved for 7 indications including acute lymphoblastic leukemia and chronic myeloid leukemia, and in clinical trials for 27 other conditions; with CIViC clinical evidence for 206 variant-indication associations (e.g. FIP1L1::PDGFRA Fusion in myeloid and lymphoid neoplasms with eosinophilia and abnormalities of pdgfra, pdgfrb, and fgfr1).

At a glance

• Status: FDA-approved (also EMA)
• Modality: Small molecule
• ATC class: L01EA01
• Targets: 5 (ABL1, PDGFRB, KIT…) (top 1% of drugs corpus-wide)
• Indications: 52 conditions (top 3% of drugs corpus-wide)
• Clinical trials: 470
• Precision-oncology evidence (CIViC): 206 variant–indication associations
• Chemistry: 493.6 Da · C29H31N7O
• Target biology: 5 curated targets implicated as cohort genes in 76 diseases corpus-wide; indicated or in trials for 48 (7 on both)
• Competitive landscape: target KIT is also targeted by 30 other curated drugs in the corpus (PDGFRB: 22; ABL1: 11; DDR2: 5 others)

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL941
Name	Imatinib
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	5291
ChEBI	CHEBI:45783
ATC	L01EA01
Molecular formula	C29H31N7O
Molecular weight	493.6
InChIKey	KTUFNOKKBVMGRW-UHFFFAOYSA-N

SMILES: CC1=C(C=C(C=C1)NC(=O)C2=CC=C(C=C2)CN3CCN(CC3)C)NC4=NC=CC(=N4)C5=CN=CC=C5

IUPAC name: 4-[(4-methylpiperazin-1-yl)methyl]-N-[4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]phenyl]benzamide

ChEBI definition: A benzamide obtained by formal condensation of the carboxy group of 4-[(4-methylpiperazin-1-yl)methyl]benzoic acid with the primary aromatic amino group of 4-methyl-N3-[4-(pyridin-3-yl)pyrimidin-2-yl]benzene-1,3-diamine. Used (as its mesylate salt) for treatment of chronic myelogenous leukemia and gastrointestinal stromal tumours.

Pharmacological roles (ChEBI): tyrosine kinase inhibitor, apoptosis inducer.

Also known as: Glamox, Imatinib, NSC-743414, NSC-759854, IMATINIB, GLEEVEC, STI-571, IMATINIB MESYLATE, GLIVEC, CGP-57148B, GLAMOX, STI571

Parent form; salt/anhydrous children: CHEMBL1642, CHEMBL2386595

Patent coverage: ubiquitous in the patent literature (a reference / commodity compound named in millions of filings — the raw count carries no drug-specific signal).

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
DDR1	discoidin domain receptor tyrosine kinase 1	Inhibition	6.47	0.1%	Q08345
DDR2	discoidin domain receptor tyrosine kinase 2	Inhibition	6.17	0%	Q16832
ABL1	ABL proto-oncogene 1, non-receptor tyrosine kinase	Inhibition	6.7	1.2%	P00519

Mechanism of action (ChEMBL curated)

Target genes: ABL1, PDGFRB, KIT

Mechanism of action	Action type	Target	Target type
Tyrosine-protein kinase ABL inhibitor	INHIBITOR	Tyrosine-protein kinase ABL1	SINGLE PROTEIN
Platelet-derived growth factor receptor beta inhibitor	INHIBITOR	Platelet-derived growth factor receptor beta	SINGLE PROTEIN
Stem cell growth factor receptor inhibitor	INHIBITOR	Mast/stem cell growth factor receptor Kit	SINGLE PROTEIN
Bcr/Abl fusion protein inhibitor	INHIBITOR	Bcr/Abl fusion protein	CHIMERIC PROTEIN

Broader ChEMBL bioactivity targets: 85 (assay-derived screening hits — not curated targets; per-target potencies are in the ChEMBL bioactivities table below).

Bioactivity

ChEMBL activities: 407 potent at pChembl ≥ 5 of 430 total. Top 100 distinct by potency (10 = 0.1 nM, 6 = 1 µM):

Protein	UniProt	Gene	pChembl	Type	Value	Activity ID
Receptor tyrosine-protein kinase erbB-2	P04626	ERBB2	10.22	IC50	0.06 nM	CHEMBL_ACT_24962908
Epidermal growth factor receptor	P00533	EGFR	9.96	IC50	0.11 nM	CHEMBL_ACT_24962906
Epithelial discoidin domain-containing receptor 1	Q08345	DDR1	9.15	Kd	0.7 nM	CHEMBL_ACT_2903445
Epithelial discoidin domain-containing receptor 1	Q08345	DDR1	9.1	Kd	0.79 nM	CHEMBL_ACT_18910095
Tyrosine-protein kinase ABL1	P00519	ABL1	9	Kd	1 nM	CHEMBL_ACT_18910094
Tyrosine-protein kinase ABL1	P00519	ABL1	8.96	IC50	1.1 nM	CHEMBL_ACT_3186208
Tyrosine-protein kinase ABL1	P00519	ABL1	8.96	Kd	1.1 nM	CHEMBL_ACT_7569852
Tyrosine-protein kinase ABL1	P00519	ABL1	8.74	Kd	1.8 nM	CHEMBL_ACT_7569847
Platelet-derived growth factor receptor alpha	P16234	PDGFRA	8.7	IC50	2 nM	CHEMBL_ACT_13418824
Tyrosine-protein kinase ABL1	P00519	ABL1	8.66	Kd	2.2 nM	CHEMBL_ACT_1651429
Tyrosine-protein kinase ABL1	P00519	ABL1	8.6	Kd	2.5 nM	CHEMBL_ACT_7569842
Tyrosine-protein kinase ABL1	P00519	ABL1	8.55	IC50	2.79 nM	CHEMBL_ACT_24729011
Platelet-derived growth factor receptor alpha	P16234	PDGFRA	8.55	IC50	2.8 nM	CHEMBL_ACT_29279125
Platelet-derived growth factor receptor alpha	P16234	PDGFRA	8.34	IC50	4.6 nM	CHEMBL_ACT_18057971
Tyrosine-protein kinase ABL1	P00519	ABL1	8.34	IC50	4.6 nM	CHEMBL_ACT_29094610
Tyrosine-protein kinase ABL1	P00519	ABL1	8.23	Kd	5.9 nM	CHEMBL_ACT_7569844
Tyrosine-protein kinase ABL2	P42684	ABL2	8.22	Kd	6 nM	CHEMBL_ACT_6174264
Breakpoint cluster region protein	P11274	BCR	8.15	Kd	7 nM	CHEMBL_ACT_17884711
Tyrosine-protein kinase ABL1	P00519	ABL1	8.08	Kd	8.3 nM	CHEMBL_ACT_7569840
Tyrosine-protein kinase ABL1	P00519	ABL1	8.07	Kd	8.5 nM	CHEMBL_ACT_2895371
Macrophage colony-stimulating factor 1 receptor	P07333	CSF1R	8	Kd	10 nM	CHEMBL_ACT_18910092
Tyrosine-protein kinase ABL2	P42684	ABL2	8	Kd	10 nM	CHEMBL_ACT_18910093
Tyrosine-protein kinase ABL1 (house mouse)	P00520		7.97	IC50	10.8 nM	CHEMBL_ACT_3397785
Macrophage colony-stimulating factor 1 receptor	P07333	CSF1R	7.96	Kd	11 nM	CHEMBL_ACT_7569856
Tyrosine-protein kinase ABL1	P00519	ABL1	7.92	Kd	12 nM	CHEMBL_ACT_2894829
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.9	Kd	12.59 nM	CHEMBL_ACT_18910091
Tyrosine-protein kinase ABL1	P00519	ABL1	7.89	IC50	13 nM	CHEMBL_ACT_15769243
Tyrosine-protein kinase ABL2	P42684	ABL2	7.89	Kd	13 nM	CHEMBL_ACT_1651264
Tyrosine-protein kinase ABL1	P00519	ABL1	7.89	Ki	13 nM	CHEMBL_ACT_2095593
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.89	Kd	13 nM	CHEMBL_ACT_7568110
Tyrosine-protein kinase ABL1	P00519	ABL1	7.85	IC50	14 nM	CHEMBL_ACT_14986740
Tyrosine-protein kinase ABL1	P00519	ABL1	7.85	Kd	14 nM	CHEMBL_ACT_1651363
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.85	Kd	14 nM	CHEMBL_ACT_2895939
Platelet-derived growth factor receptor beta	P09619	PDGFRB	7.85	Kd	14 nM	CHEMBL_ACT_2899081
Tyrosine-protein kinase ABL1	P00519	ABL1	7.85	Ki	14 nM	CHEMBL_ACT_3447716
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.82	Kd	15 nM	CHEMBL_ACT_2897039
Discoidin domain-containing receptor 2	Q16832	DDR2	7.82	Kd	15 nM	CHEMBL_ACT_2897557
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.79	IC50	16.4 nM	CHEMBL_ACT_18093797
Platelet-derived growth factor receptor alpha	P16234	PDGFRA	7.75	IC50	18 nM	CHEMBL_ACT_2356931
Macrophage colony-stimulating factor 1 receptor	P07333	CSF1R	7.72	Kd	19 nM	CHEMBL_ACT_2902388
Tyrosine-protein kinase ABL1	P00519	ABL1	7.7	IC50	19.9 nM	CHEMBL_ACT_13370906
Macrophage colony-stimulating factor 1 receptor	P07333	CSF1R	7.68	IC50	21 nM	CHEMBL_ACT_26198613
Tyrosine-protein kinase ABL1	P00519	ABL1	7.68	Kd	21 nM	CHEMBL_ACT_2895409
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.67	IC50	21.6 nM	CHEMBL_ACT_13370875
Epithelial discoidin domain-containing receptor 1	Q08345	DDR1	7.66	Kd	22 nM	CHEMBL_ACT_17896054
Tyrosine-protein kinase ABL1	P00519	ABL1	7.62	Kd	24 nM	CHEMBL_ACT_1651385
Tyrosine-protein kinase ABL1	P00519	ABL1	7.6	IC50	25 nM	CHEMBL_ACT_14545491
Platelet-derived growth factor receptor beta	P09619	PDGFRB	7.55	Kd	28 nM	CHEMBL_ACT_1651704
Carbonic anhydrase 2	P00918	CA2	7.52	Ki	30.2 nM	CHEMBL_ACT_2692377
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.51	Ki	30.7 nM	CHEMBL_ACT_28237853
Platelet-derived growth factor receptor alpha	P16234	PDGFRA	7.51	Kd	31 nM	CHEMBL_ACT_2899043
Carbonic anhydrase 1	P00915	CA1	7.5	Ki	31.9 nM	CHEMBL_ACT_2692376
Tyrosine-protein kinase ABL1	P00519	ABL1	7.47	EC50	34 nM	CHEMBL_ACT_16593632
Tyrosine-protein kinase ABL1	P00519	ABL1	7.46	Kd	35 nM	CHEMBL_ACT_2895333
Tyrosine-protein kinase ABL1	P00519	ABL1	7.43	Ki	37 nM	CHEMBL_ACT_3447169
Tyrosine-protein kinase ABL1	P00519	ABL1	7.42	IC50	38.02 nM	CHEMBL_ACT_13293007
Tyrosine-protein kinase ABL1	P00519	ABL1	7.42	IC50	38 nM	CHEMBL_ACT_1614497
Tyrosine-protein kinase ABL1 (house mouse)	P00520		7.42	IC50	38 nM	CHEMBL_ACT_25041343
Ribosyldihydronicotinamide dehydrogenase [quinone]	P16083	NQO2	7.41	Ki	39 nM	CHEMBL_ACT_16844188
Multidrug and toxin extrusion protein 1	Q96FL8	SLC47A1	7.4	IC50	40 nM	CHEMBL_ACT_12636125
Tyrosine-protein kinase Lck	P06239	LCK	7.4	Kd	39.81 nM	CHEMBL_ACT_18910090
Tyrosine-protein kinase ABL1	P00519	ABL1	7.4	IC50	40 nM	CHEMBL_ACT_1907590
Tyrosine-protein kinase Lck	P06239	LCK	7.4	Kd	40 nM	CHEMBL_ACT_2897928
Ribosyldihydronicotinamide dehydrogenase [quinone]	P16083	NQO2	7.39	Kd	41 nM	CHEMBL_ACT_17922216
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.39	IC50	41 nM	CHEMBL_ACT_18057752
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.39	IC50	40.8 nM	CHEMBL_ACT_29279023
Ribosyldihydronicotinamide dehydrogenase [quinone]	P16083	NQO2	7.37	IC50	43 nM	CHEMBL_ACT_16844186
Tyrosine-protein kinase ABL1	P00519	ABL1	7.37	IC50	43 nM	CHEMBL_ACT_19161692
Epithelial discoidin domain-containing receptor 1	Q08345	DDR1	7.37	IC50	43 nM	CHEMBL_ACT_3471361
Tyrosine-protein kinase ABL1	P00519	ABL1	7.36	Kd	44 nM	CHEMBL_ACT_1651418
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.34	IC50	46 nM	CHEMBL_ACT_2356925
Multidrug and toxin extrusion protein 1	Q96FL8	SLC47A1	7.3	IC50	50 nM	CHEMBL_ACT_12636134
Platelet-derived growth factor receptor beta	P09619	PDGFRB	7.3	IC50	50 nM	CHEMBL_ACT_1614495
Platelet-derived growth factor receptor beta (house mouse)	P05622		7.3	IC50	50 nM	CHEMBL_ACT_25041345
Platelet-derived growth factor receptor beta	P09619	PDGFRB	7.3	Ki	50.12 nM	CHEMBL_ACT_9588176
Tyrosine-protein kinase ABL1	P00519	ABL1	7.3	Ki	50.12 nM	CHEMBL_ACT_9599655
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.28	IC50	53 nM	CHEMBL_ACT_19148206
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.28	IC50	52 nM	CHEMBL_ACT_2356924
Tyrosine-protein kinase ABL1	P00519	ABL1	7.27	IC50	54 nM	CHEMBL_ACT_19087793
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.24	IC50	58 nM	CHEMBL_ACT_2371993
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.23	IC50	59 nM	CHEMBL_ACT_25688582
Tyrosine-protein kinase Lck	P06239	LCK	7.21	Kd	62 nM	CHEMBL_ACT_1651374
Tyrosine-protein kinase ABL1	P00519	ABL1	7.21	Kd	62 nM	CHEMBL_ACT_1651451
Tyrosine-protein kinase ABL2	P42684	ABL2	7.19	Kd	64 nM	CHEMBL_ACT_17878769
Tyrosine-protein kinase ABL1	P00519	ABL1	7.19	Kd	65 nM	CHEMBL_ACT_7569845
Platelet-derived growth factor receptor alpha	P16234	PDGFRA	7.15	IC50	71 nM	CHEMBL_ACT_24900277
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.15	Kd	71 nM	CHEMBL_ACT_2897001
Platelet-derived growth factor receptor alpha	P16234	PDGFRA	7.14	IC50	72 nM	CHEMBL_ACT_3471358
Platelet-derived growth factor receptor beta	P09619	PDGFRB	7.14	IC50	72 nM	CHEMBL_ACT_3471359
Tyrosine-protein kinase ABL1	P00519	ABL1	7.13	IC50	74 nM	CHEMBL_ACT_15718780
Tyrosine-protein kinase ABL1	P00519	ABL1	7.12	IC50	75 nM	CHEMBL_ACT_26276615
Carbonic anhydrase 9	Q16790	CA9	7.12	Ki	75.7 nM	CHEMBL_ACT_2692384
Carbonic anhydrase 15 (house mouse)	Q99N23		7.11	Ki	78 nM	CHEMBL_ACT_2692388
Tyrosine-protein kinase ABL1	P00519	ABL1	7.11	Kd	77 nM	CHEMBL_ACT_2894867
Ribosyldihydronicotinamide dehydrogenase [quinone]	P16083	NQO2	7.09	IC50	82 nM	CHEMBL_ACT_16857702
Epithelial discoidin domain-containing receptor 1	Q08345	DDR1	7.05	IC50	90 nM	CHEMBL_ACT_16844184
Platelet-derived growth factor receptor alpha	P16234	PDGFRA	7.05	EC50	90 nM	CHEMBL_ACT_2206925
Mast/stem cell growth factor receptor Kit	P10721	KIT	7.04	Kd	91 nM	CHEMBL_ACT_7568117
Tyrosine-protein kinase ABL1	P00519	ABL1	7.04	Kd	92 nM	CHEMBL_ACT_7569848
Platelet-derived growth factor receptor alpha	P16234	PDGFRA	7.02	IC50	96 nM	CHEMBL_ACT_1699240

Target pathways

Aggregated over 3 target gene(s): DDR1, DDR2, ABL1.

Top Reactome pathways

55 total, by targets touching each:

Pathway	Targets	Genes
Extracellular matrix organization	2	DDR1, DDR2
Non-integrin membrane-ECM interactions	2	DDR1, DDR2
Hemostasis	1	ABL1
Developmental Biology	1	ABL1
Signal Transduction	1	ABL1
Cell Cycle	1	ABL1
Disease	1	ABL1
Innate Immune System	1	ABL1
Immune System	1	ABL1
Signaling by Rho GTPases	1	ABL1
RHO GTPase Effectors	1	ABL1
Fcgamma receptor (FCGR) dependent phagocytosis	1	ABL1
Regulation of actin dynamics for phagocytic cup formation	1	ABL1
Epigenetic regulation of gene expression	1	ABL1
Generic Transcription Pathway	1	ABL1
Signaling by ROBO receptors	1	ABL1
Axon guidance	1	ABL1
Role of ABL in ROBO-SLIT signaling	1	ABL1
Mitotic G1 phase and G1/S transition	1	ABL1
Myogenesis	1	ABL1
Infectious disease	1	ABL1
RHO GTPases Activate WASPs and WAVEs	1	ABL1
HDR through Single Strand Annealing (SSA)	1	ABL1
DNA Double-Strand Break Repair	1	ABL1
Homology Directed Repair	1	ABL1
Recruitment and ATM-mediated phosphorylation of repair and signaling proteins at DNA double strand breaks	1	ABL1
HDR through Homologous Recombination (HRR) or Single Strand Annealing (SSA)	1	ABL1
DNA Double Strand Break Response	1	ABL1
Cyclin D associated events in G1	1	ABL1
G1 Phase	1	ABL1
Cell Cycle, Mitotic	1	ABL1
RNA Polymerase II Transcription	1	ABL1
DNA Repair	1	ABL1
Gene expression (Transcription)	1	ABL1
Transcriptional regulation by RUNX2	1	ABL1
Transcriptional regulation by RUNX1	1	ABL1
RUNX1 regulates transcription of genes involved in differentiation of HSCs	1	ABL1
RUNX2 regulates osteoblast differentiation	1	ABL1
RUNX2 regulates bone development	1	ABL1
Cellular responses to stimuli	1	ABL1
Leishmania infection	1	ABL1
Parasite infection	1	ABL1
Leishmania phagocytosis	1	ABL1
FCGR3A-mediated phagocytosis	1	ABL1
Nervous system development	1	ABL1
Signaling by Rho GTPases, Miro GTPases and RHOBTB3	1	ABL1
Epigenetic regulation of gene expression by MLL3 and MLL4 complexes	1	ABL1
Parasitic Infection Pathways	1	ABL1
Factors involved in megakaryocyte development and platelet production	1	ABL1
MLL4 and MLL3 complexes regulate expression of PPARG target genes in adipogenesis and hepatic steatosis	1	ABL1

Dominant GO biological processes

GO term	Targets
cell adhesion	3
protein phosphorylation	3
cell surface receptor protein tyrosine kinase signaling pathway	2
regulation of extracellular matrix disassembly	2
positive regulation of neuron projection development	2
collagen-activated tyrosine kinase receptor signaling pathway	2
protein autophosphorylation	2
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction	2
positive regulation of fibroblast proliferation	2
cellular response to transforming growth factor beta stimulus	2
female pregnancy	1
lactation	1
smooth muscle cell migration	1
peptidyl-tyrosine autophosphorylation	1
wound healing, spreading of cells	1

Predicted targets — Sugi Predict

This molecule is SureChEMBL compound SCHEMBL29355523 — see its predicted protein targets + similar patent compounds on Sugi Predict.

Indications & clinical

Indications

7 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
acute lymphoblastic leukemia	3	MONDO:0004967	EFO:0000220
chronic myeloid leukemia	3	MONDO:0011996	EFO:0000339
leukemia	3	MONDO:0005059	EFO:0000565
neoplasm	3	MONDO:0005070	EFO:0000616
sarcoma	3	MONDO:0005089	EFO:0000691
myeloid leukemia	3	MONDO:0004643
gastrointestinal stromal tumor	3	MONDO:0011719

27 diseases in clinical trials (phase 2–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
pulmonary arterial hypertension	3	MONDO:0015924	EFO:0001361
stroke disorder	3	MONDO:0005098	EFO:0000712
pulmonary hypertension	3	MONDO:0005149
graft versus host disease	3	MONDO:0013730
severe acute respiratory syndrome	3	MONDO:0005091
pneumonia	3	MONDO:0005249	EFO:0003106
influenza	3	MONDO:0005812	EFO:0007328
acute myeloid leukemia	2	MONDO:0018874	EFO:0000222
fibromatosis	2	MONDO:0005031	EFO:0000497
gastric adenocarcinoma	2	MONDO:0005036	EFO:0000503
glioblastoma	2	MONDO:0018177	EFO:0000519
rheumatoid arthritis	2	MONDO:0008383	EFO:0000685
systemic sclerosis	2	MONDO:0005100	EFO:0000717
melanoma	2	MONDO:0005105	EFO:0000756
metastatic melanoma	2	MONDO:0005191	EFO:0002617
gastric neoplasm	2	MONDO:0021085	EFO:0003897
colonic neoplasm	2	MONDO:0005401	EFO:0004288
Plasmodium falciparum malaria	2	MONDO:0005920	EFO:0007444
thyroid gland papillary carcinoma	2	MONDO:0005075	EFO:0000641
hypereosinophilic syndrome	2	MONDO:0015691	EFO:1001467
breast neoplasm	2	MONDO:0021100
lung neoplasm	2	MONDO:0021117
spinal cord injury	2	MONDO:0043797	EFO:1001919
desmoid tumor	2	MONDO:0007608	EFO:0009907
chordoma	2	MONDO:0008978
tuberculosis	2	MONDO:0018076
lymphoid leukemia	2	MONDO:0005402	EFO:0004289

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

Regulatory approval & mechanism (DrugCentral)

Approved: FDA, EMA. Curated mechanism: AGONIST/INHIBITOR · 3 MOA targets of 71 total (P00519, P09619, P10721).

DrugCentral (CC BY-SA): authoritative regulatory-approval status + curated mechanism. The drug’s full target set is in Targets above.

Clinical trials

Total trials: 470.

Phase distribution

Phase	Trials
Phase 2	240
Phase 3	72
Phase 1	61
Phase 1/2	44
Not specified	29
Phase 4	18
Phase 2/3	3
Early Phase 1	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT03844360	Phase 4	RECRUITING	Dose Individualization of Antineoplastic Drugs and Anti-Infective Drug in Children With Hematoplastic Disease
NCT04877522	Phase 4	RECRUITING	Asciminib Roll-over Study
NCT05367765	Phase 4	NOT_YET_RECRUITING	A Real World Study of the Efficacy and Safety of Flumatinib Versus Imatinib in Patients With Newly Diagnosed Chronic Myeloid Leukemia in Chronic Phase
NCT00081926	Phase 4	COMPLETED	Gleevec Trial in Patients With Newly Diagnosed Chronic Phase Chronic Myelogenous Leukemia
NCT00171899	Phase 4	COMPLETED	Study Comparing Standard Dose and High-dose Imatinib Mesylate in Patients With Chronic Phase Philadelphia Chromosome Positive (Ph+) Chronic Myelogenous Leukemia (CML)
NCT00171977	Phase 4	COMPLETED	Post-Marketing Clinical Study of Postoperative Adjuvant Therapy With Imatinib Mesylate in Patients With Gastrointestinal Stromal Tumors (GIST)
NCT00372476	Phase 4	COMPLETED	Efficacy and Safety of Imatinib and Vinorelbine in Patients With Advanced Breast Cancer
NCT00390897	Phase 4	COMPLETED	Glivec® (Imatinib Mesylate, STI571) in Monotherapy Versus Glivec®-Interferon Alpha in the Treatment of Chronic-Phase Chronic Myeloid Leukaemia
NCT00510354	Phase 4	COMPLETED	Treatment of Patients With Everolimus and Imatinib Mesylate Who Have Progressive Gastro Intestinal Stromal Tumors (GIST) and Are Resistant to Imatinib Mesylate
NCT01297777	Phase 4	COMPLETED	Imatinib in KIT-negative Systemic Mastocytosis
NCT01491763	Phase 4	UNKNOWN	Chemotherapy and Imatinib in Young Adults With Acute Lymphoblastic Leukemia Ph (BCR-ABL) POSITIVE
NCT01578213	Phase 4	COMPLETED	Validation of Digital-PCR Analysis Through Programmed Imatinib Interruption in PCR Negative CML Patients
NCT01742299	Phase 4	COMPLETED	Study to Allow Access to Imatinib for Patients Who Are on Imatinib Treatment in a Novartis-sponsored Study and Are Benefiting From the Treatment as Judged by the Investigator
NCT02317159	Phase 4	UNKNOWN	Efficacy and Safety of Imatinib Mesylate as First-line Treatment for the Patients With Chronic Phase of Chronic Myeloid Leukemia
NCT02602314	Phase 4	UNKNOWN	Sustained Treatment-free Remission in BCR-ABL+ Chronic Myeloid Leukemia
NCT02894645	Phase 4	UNKNOWN	Malaysia-Singapore Acute Lymphoblastic Leukemia 2010 Study
NCT05071482	Phase 4	TERMINATED	Flumatinib Versus Imatinib Combined With Chemotherapy for de Novo Ph+ ALL
NCT05220280	Phase 4	UNKNOWN	SOLIDARITY Finland Plus Long-COVID
NCT02413736	Phase 3	ACTIVE_NOT_RECRUITING	Three Versus Five Years of Adjuvant Imatinib as Treatment of Patients With Operable GIST
NCT02735707	Phase 3	RECRUITING	Randomized, Embedded, Multifactorial Adaptive Platform Trial for Community- Acquired Pneumonia
NCT03007147	Phase 3	ACTIVE_NOT_RECRUITING	Imatinib Mesylate and Combination Chemotherapy in Treating Patients With Newly Diagnosed Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia
NCT03589326	Phase 3	ACTIVE_NOT_RECRUITING	A Study of Ponatinib Versus Imatinib in Adults With Acute Lymphoblastic Leukemia
NCT03722420	Phase 3	ACTIVE_NOT_RECRUITING	Randomized Evaluation of Radotinib Versus Imatinib in Phase III Study for Efficacy With Chinese Patients (RERISE China)
NCT04307576	Phase 3	RECRUITING	A Treatment Study Protocol for Participants 0-45 Years With Acute Lymphoblastic Leukaemia
NCT04722848	Phase 3	ACTIVE_NOT_RECRUITING	Sequential Treatment With Ponatinib and Blinatumomab vs Chemotherapy and Imatinib in Newly Diagnosed Adult Ph+ ALL
NCT04971226	Phase 3	ACTIVE_NOT_RECRUITING	A Study of Oral Asciminib Versus Other TKIs in Adult Patients With Newly Diagnosed Ph+ CML-CP
NCT05970900	Phase 3	NOT_YET_RECRUITING	Preoperative Imatinib Mesylate Combined With Rectal-sparing Surgery in Patients With c-KIT Gene-mutant Rectal GIST
NCT06682169	Phase 3	RECRUITING	Evaluation of Rovadicitinib Compared to the Protocol Selected by Researchers in Third Line and Subsequent Studies of Moderate to Severe Chronic Graft-versus-host Disease
NCT07530367	Phase 3	NOT_YET_RECRUITING	Tofacitinib Plus Imatinib in Moderate-to-Severe Palmoplantar Pustulosis
NCT07585266	Phase 3	RECRUITING	A Study to Investigate Velzatinib Compared With Imatinib in Adult Participants With Previously Untreated Metastatic and/or Unresectable Gastrointestinal Stromal Tumors (StrateGIST Frontline)
NCT00002514	Phase 3	COMPLETED	Stem Cell Transplantation Compared With Standard Chemotherapy in Treating Patients With Acute Lymphoblastic Leukemia in First Remission
NCT00006343	Phase 3	COMPLETED	STI571 Compared With Interferon Alfa Plus Cytarabine in Treating Patients With Newly Diagnosed Chronic Myelogenous Leukemia
NCT00009906	Phase 3	TERMINATED	Comparison of Two Different Doses of STI571 in Treating Patients With Metastatic or Unresectable Gastrointestinal Stromal Tumor
NCT00022737	Phase 3	COMPLETED	Combination Chemotherapy With or Without Peripheral Stem Cell Transplant in Treating Children With Acute Lymphoblastic Leukemia
NCT00041197	Phase 3	COMPLETED	Imatinib Mesylate in Treating Patients With Primary Gastrointestinal Stromal Tumor That Has Been Completely Removed By Surgery
NCT00050531	Phase 3	COMPLETED	High-Dose Gleevec Alone or in Combination With Peg-Intron and GM-CSF in Early Phase Chronic Myelogenous Leukemia (CML)
NCT00055874	Phase 3	COMPLETED	Imatinib Mesylate With or Without Interferon Alfa or Cytarabine Compared With Interferon Alfa Followed by Donor Stem Cell Transplant in Treating Patients With Newly Diagnosed Chronic Phase Chronic Myelogenous Leukemia
NCT00103168	Phase 3	COMPLETED	Imatinib Mesylate or Observation Only in Treating Patients Who Have Undergone Surgery for Localized Gastrointestinal Stromal Tumor
NCT00116935	Phase 3	COMPLETED	Study Comparing 12 Months Versus 36 Months of Imatinib in the Treatment of Gastrointestinal Stromal Tumor (GIST)
NCT00124748	Phase 3	TERMINATED	Efficacy of 400 Mg Versus 800 Mg Imatinib in Chronic Myeloid Leukemia in Chronic Phase Patients - TOPS (Tyrosine Kinase Inhibitor Optimization and Selectivity)
NCT00137111	Phase 3	COMPLETED	Therapy for Newly Diagnosed Patients With Acute Lymphoblastic Leukemia
NCT00154375	Phase 3	COMPLETED	Study of Imatinib Mesylate in Combination With Hydroxyurea Versus Hydroxyurea Alone as an Oral Therapy in Patients With Temozolomide Resistant Progressive Glioblastoma
NCT00219739	Phase 3	COMPLETED	STI571 ProspectIve RandomIzed Trial: SPIRIT
NCT00237120	Phase 3	COMPLETED	Efficacy, Safety and Long-term Prognosis of Imatinib in Patients Newly Diagnosed With Chronic Myelogenous Leukemia (Chronic Phase)
NCT00293124	Phase 3	COMPLETED	Open-label Trial of GlivecWith Unresectable or Metastatic Malignant Gastrointestinal Stromal Tumors
NCT00297570	Phase 3	UNKNOWN	Imatinib Versus Imatinib and Peg-Interferon in Patients With Ph+ CML and Complete Cytogenetic Response After Imatinib Therapy
NCT00324987	Phase 3	TERMINATED	Imatinib Mesylate With or Without Bevacizumab in Treating Patients With Metastatic or Unresectable Gastrointestinal Stromal Tumor
NCT00327262	Phase 3	UNKNOWN	Comparing Imatinib Standard Dose With Imatinib High Dose Induction in Pretreated Chronic Myeloid Leukemia (CML) Patients in Chronic Phase
NCT00327678	Phase 3	COMPLETED	Treatment of Acute Lymphoblastic Leukemia (ALL) in Younger Adults
NCT00362466	Phase 3	TERMINATED	A Study of Dasatinib vs. High-Dose Imatinib (600 mg) in Patients With Chronic Phase Chronic Myeloid Leukemia (CML) Who Failed to Achieve Complete Cytogenetic Response After 3-18 Months of Imatinib Therapy
NCT00372567	Phase 3	TERMINATED	Safety And Effectiveness Of Daily Dosing With Sunitinib Or Imatinib In Patients With Gastrointestinal Stromal Tumors
NCT00427583	Phase 2/3	TERMINATED	Imatinib Mesylate Treatment of Patients With Malignant Peripheral Nerve Sheath Tumors
NCT00471497	Phase 3	COMPLETED	A Study of Imatinib Versus Nilotinib in Adult Patients With Newly Diagnosed Philadelphia Chromosome Positive (Ph+) Chronic Myelogenous Leukemia in Chronic Phase (CML-CP)
NCT00477269	Phase 2/3	COMPLETED	Safety and Efficacy of Imatinib Mesylate in Patients With Pulmonary Arterial Hypertension
NCT00481247	Phase 3	COMPLETED	A Phase III Study of Dasatinib vs Imatinib in Patients With Newly Diagnosed Chronic Phase Chronic Myeloid Leukemia
NCT00514488	Phase 3	COMPLETED	Imatinib Standard Dose (400 mg/Day) Versus Imatinib High Dose (800 mg/Day)
NCT00519090	Phase 3	TERMINATED	Nilotinib vs Imatinib in Adult Patients With Philadelphia (Ph+) Chronic Myelogenous Leukemia in Chronic Phase (CML-CP)
NCT00574873	Phase 3	COMPLETED	Compare Bosutinib To Imatinib In Subjects With Newly Diagnosed Chronic Phase Philadelphia Chromosome Positive CML
NCT00685828	Phase 3	UNKNOWN	Imatinib Mesylate in Treating Patients With Unresectable or Metastatic Gastrointestinal Stromal Tumor
NCT00751036	Phase 3	TERMINATED	Nilotinib 800 Mg And Imatinib 800 Mg For The Treatment Of Patients With Gastrointestinal Stromal Tumors (Gist) Refractory To Imatinib 400 Mg
NCT00760877	Phase 3	COMPLETED	Nilotinib Versus Standard Imatinib (400/600 mg Every Day (QD)) Comparing the Kinetics of Complete Molecular Response for Chronic Myelogenous Leukemia in Chronic Phase (CML-CP) Pts With Evidence of Persistent Leukemia by Real-time Quantitative Polymerase Chain Reaction (RQ-PCR)
NCT00785785	Phase 3	COMPLETED	A Study of Nilotinib Versus Imatinib in GIST Patients
NCT00802841	Phase 3	COMPLETED	Randomized Phase Lll Study of Imatinib Dose Optimization vs Nilotinib in CML Patients With Suboptimal Response to Imatinib
NCT00812240	Phase 3	TERMINATED	Masitinib in First Line Treatment of Gastro-Intestinal Stromal Tumor (GIST)
NCT00902174	Phase 3	COMPLETED	Imatinib (QTI571) in Pulmonary Arterial Hypertension
NCT00956072	Phase 3	TERMINATED	Imatinib Mesylate With or Without Surgery in Treating Patients With Metastatic Gastrointestinal Stromal Tumor That is Responding to Imatinib Mesylate
NCT01031628	Phase 3	TERMINATED	Study of Dose Escalation Versus no Dose Escalation of Imatinib in Metastatic Gastrointestinal Stromal Tumors (GIST) Patients
NCT01117987	Phase 3	TERMINATED	Extension to QTI571A2301 to Evaluate the Long-term Safety, Tolerability and Efficacy of Imatinib in Severe Pulmonary Arterial Hypertension (PAH)
NCT01151852	Phase 3	COMPLETED	Rechallenge of Imatinib in GIST Having no Effective Treatment: RIGHT
NCT01275196	Phase 3	COMPLETED	Safety and Efficacy of Nilotinib vs. Imatinib in the Treatment of Newly Diagnosed Chinese Ph+ CML-CP Patients
NCT01392469	Phase 3	COMPLETED	Pharmacokinetic Effects of QTI571 on Sildenafil and Bosentan in Pulmonary Arterial Hypertension Participants
NCT01392495	Phase 3	TERMINATED	Extension to CQTI571A2102 to Evaluate Long-term Safety, Tolerability and Efficacy of Imatinib in Severe Pulmonary Arterial Hypertension (PAH)
NCT01400074	Phase 3	UNKNOWN	Efficacy of Nilotinib Versus Imatinib in Ph+ CML in Early CP Who Have a Suboptimal Molecular Response to Imatinib
NCT01460693	Phase 3	COMPLETED	Comparison of Imatinib Versus Dasatinib in Patients With Newly-diagnosed Chronic Phase Chronic Myeloid Leukaemia
NCT01511289	Phase 3	COMPLETED	Radotinib Versus Imatinib in Newly Diagnosed Philadelphia Chromosome and Chronic Myeloid Leukemia Chronic Phase Patients
NCT01819389	Phase 3	COMPLETED	Low-dose Nilotinib and Imatinib Combination in Chronic Myeloid Leukemia Patients, With Failure, Suboptimal Response or Treatment Intolerance
NCT01827930	Phase 3	TERMINATED	Phase III Trial Evaluating the Effectiveness of a Dose Adjustment of Imatinib Mesylate on the Molecular Response
NCT02103322	Phase 2/3	COMPLETED	Comparative Bioequivalence Study in Adult Patients Suffering From Chronic Myeloid Leukemia & Gastrointestinal Stromal Tumor Under Fed Conditions
NCT02130557	Phase 3	COMPLETED	A Multicenter Phase 3, Open-Label Study of Bosutinib Versus Imatinib in Adult Patients With Newly Diagnosed Chronic Phase Chronic Myelogenous Leukemia
NCT02174445	Phase 3	TERMINATED	An Open-label, Randomised Multicenter Phase 3b Study to Determine the Confirmed Rate of Molecular Response ≥ 4 Log (MR4) at Two Years
NCT02260505	Phase 3	COMPLETED	Efficiency of Imatinib Treatment Maintenance or Interruption After 3 Years of Adjuvant Treatment in Patients With Gastrointestinal Stromal Tumours (GIST)
NCT02272777	Phase 3	COMPLETED	A Study of Imatinib and Nilotinib in Patients With Chronic Myelogenous Leukemia in Chronic Phase
NCT02326311	Phase 3	COMPLETED	Optimization of TKIs Treatment and Quality of Life in Ph+ CML Patients ≥60 Years in Deep Molecular Response
NCT02576080	Phase 3	UNKNOWN	Efficacy of Imatinib in Patients With Intermediate-risk Gastrointestinal Stromal Tumor With a High-risk Genomic Grade Index
NCT02611492	Phase 3	UNKNOWN	A Phase III Randomized Trial of the Reduction of Chemotherapy in Philadelphia Chromosome-positive ALL of Young Adults
NCT02881086	Phase 3	COMPLETED	Optimization of Therapy in Adult Patients With Newly Diagnosed Acute Lymphoblastic Leukemia or Lymphoblastic Lymphoma by Individualised, Targeted and Intensified Treatment
NCT03112603	Phase 3	COMPLETED	A Study of Ruxolitinib vs Best Available Therapy (BAT) in Patients With Steroid-refractory Chronic Graft vs. Host Disease (GvHD) After Bone Marrow Transplantation (REACH3)
NCT03515018	Phase 3	UNKNOWN	Evaluation of the Therapeutic Effect of HU Pulse Therapy for CML Patients
NCT03639922	Phase 3	UNKNOWN	Imatinib in Acute Ischaemic Stroke
NCT04330690	Phase 3	UNKNOWN	Treatments for COVID-19: Canadian Arm of the SOLIDARITY Trial
NCT04394416	Phase 3	TERMINATED	Trial of Imatinib for Hospitalized Adults With COVID-19
NCT04422678	Phase 3	UNKNOWN	The Safety & Efficacy of Imatinib for the Treatment of SARS-COV-2 Induced Pneumonia
NCT05413915	Phase 3	TERMINATED	Asciminib Used in Consolidation With Imatinib vs. Imatinib to Achieve TFR in CP-CML
NCT00044304	Phase 2	ACTIVE_NOT_RECRUITING	Tyrosine Kinase Inhibition to Treat Myeloid Hypereosinophilic Syndrome
NCT00070499	Phase 2	ACTIVE_NOT_RECRUITING	Imatinib Mesylate or Dasatinib in Treating Patients With Previously Untreated Chronic Phase Chronic Myelogenous Leukemia
NCT03516279	Phase 2	ACTIVE_NOT_RECRUITING	Pembrolizumab and Dasatinib, Imatinib Mesylate, or Nilotinib in Treating Patients With Chronic Myeloid Leukemia and Persistently Detectable Minimal Residual Disease
NCT03654768	Phase 2	ACTIVE_NOT_RECRUITING	Testing the Addition of Ruxolitinib to the Usual Treatment (Tyrosine Kinase Inhibitors) for Chronic Myeloid Leukemia
NCT03906292	Phase 2	ACTIVE_NOT_RECRUITING	Frontline Asciminib Combination in Chronic Phase CML
NCT04070443	Phase 2	ACTIVE_NOT_RECRUITING	Safety and Efficacy of Ponatinib Followed by Imatinib in Patients With Chronic Myelogenous Leukemia in Chronic Phase
NCT04147533	Phase 2	ACTIVE_NOT_RECRUITING	Efficacy and Safety of TKIs’ Withdrawal After a Two-step Dose Reduction in Patients with Chronic Myeloid Leukemia

Clinical evidence (CIViC)

Variant × therapy × indication — from 266 curated evidence items. CIViC evidence level: A (validated) → B (clinical) → C (case study) → D (preclinical) → E (inferential).

showing 30 of 206 predictive associations by evidence level:

Variant	Therapy	Indication	Effect	Level	CIViC
FIP1L1::PDGFRA Fusion	Imatinib	Myeloid And Lymphoid Neoplasms With Eosinophilia And Abnormalities Of PDGFRA, PDGFRB, And FGFR1	Sensitivity/Response	CIViC A	EID1445 +2
KIT Exon 11 Mutation	Imatinib	Gastrointestinal Stromal Tumor	Sensitivity/Response	CIViC A	EID654 +2
BCR::ABL1 Fusion	Imatinib	Chronic Myeloid Leukemia	Sensitivity/Response	CIViC A	EID260 +1
KIT Exon 9 Mutation	Imatinib	Gastrointestinal Stromal Tumor	Sensitivity/Response	CIViC A	EID1221 +1
PDGFRB Fusion	Imatinib	Myeloproliferative Neoplasm	Sensitivity/Response	CIViC A	EID11272 +1
BCR::ABL1 Fusion	Imatinib	Acute Myeloid Leukemia	Sensitivity/Response	CIViC A	EID259
COL1A1::PDGFB Fusion	Imatinib	Dermatofibrosarcoma Protuberans	Sensitivity/Response	CIViC A	EID11271
FIP1L1::PDGFRA Fusion	Imatinib	Myeloproliferative Neoplasm	Sensitivity/Response	CIViC A	EID11273
KIT Mutation	Imatinib	Gastrointestinal Stromal Tumor	Sensitivity/Response	CIViC A	EID11282
PDGFRA D842V	Imatinib	Gastrointestinal Stromal Tumor	Sensitivity/Response	CIViC A	EID11545
PDGFRA Mutation	Imatinib	Gastrointestinal Stromal Tumor	Sensitivity/Response	CIViC B	EID11331 +1
BCL2L11 Deletion Polymorphism	Imatinib	Chronic Myeloid Leukemia	Sensitivity/Response	CIViC B	EID9701
CTNNB1 S45F	Imatinib	Desmoid Tumor	Sensitivity/Response	CIViC B	EID11018
ETV6::ABL1 Fusion	Nilotinib + Dasatinib + Imatinib	Myeloid Neoplasm	Sensitivity/Response	CIViC B	EID11326
IKZF1 Deletion	Methotrexate + Daunorubicin + Cytarabine + Fludarabine + Imatinib	B-lymphoblastic Leukemia/lymphoma	Sensitivity/Response	CIViC B	EID7366
KIT EXPRESSION	Imatinib	Gastrointestinal Stromal Tumor	Sensitivity/Response	CIViC B	EID2480
KIT Exon 11 Mutation	Imatinib	Melanoma	Sensitivity/Response	CIViC B	EID58
KIT Mutation	Imatinib	Melanoma	Sensitivity/Response	CIViC B	EID1222
KIT Y503_F504insAY	Imatinib	Gastrointestinal Stromal Tumor	Sensitivity/Response	CIViC B	EID2394
NOT KIT D816V	Imatinib	Systemic Mastocytosis	Sensitivity/Response	CIViC B	EID11158
KIT 557/558 in-frame deletion/delins	Imatinib	Gastrointestinal Stromal Tumor	Reduced Sensitivity	CIViC B	EID12935
KIT Exon 9 Mutation	Imatinib	Gastrointestinal Stromal Tumor	Reduced Sensitivity	CIViC B	EID2477
BCR::ABL1 Fusion AND ABL1 T315I	Imatinib	Chronic Myeloid Leukemia	Resistance	CIViC B	EID234 +4
KIT Q694K	Imatinib	Gastrointestinal Stromal Tumor	Resistance	CIViC B	EID2498 +4
KIT S692L	Imatinib	Gastrointestinal Stromal Tumor	Resistance	CIViC B	EID2493 +4
PDGFRA D842V	Imatinib	Gastrointestinal Stromal Tumor	Resistance	CIViC B	EID15 +4
KIT S501_A502INSAY	Imatinib	Gastrointestinal Stromal Tumor	Resistance	CIViC B	EID2855 +3
KIT T661I	Imatinib	Gastrointestinal Stromal Tumor	Resistance	CIViC B	EID2491 +3
BCL2L11 Deletion Polymorphism	Imatinib	Chronic Myeloid Leukemia	Resistance	CIViC B	EID1280
KIT Amplification	Imatinib	Mucosal Melanoma	Resistance	CIViC B	EID1466

CIViC column: a representative evidence item (EID); +N = additional CIViC items supporting the same association.

Pharmacology

MeSH pharmacological classification

Definition (MeSH): A tyrosine kinase inhibitor and ANTINEOPLASTIC AGENT that inhibits the BCR-ABL kinase created by chromosome rearrangements in CHRONIC MYELOID LEUKEMIA and ACUTE LYMPHOBLASTIC LEUKEMIA, as well as PDG-derived tyrosine kinases that are overexpressed in gastrointestinal stromal tumors.

Pharmacological action: Antineoplastic Agents; Tyrosine Kinase Inhibitors.

Broader MeSH headings: Benzamides; Piperazines; Pyrimidines.

MeSH descriptor D000068877 “Imatinib Mesylate” — exact-name match on this drug’s salt/hydrate form CHEMBL1642.

Pharmacogenomics

PGx drug labels — PharmGKB annotations of regulatory drug labels (FDA / EMA / PMDA / Health Canada (HCSC) / Swissmedic) that carry pharmacogenomic information, ordered by the label’s PGx level (Testing Required strongest → No Clinical PGx; — = no level recorded). Label guidance = the label gives PGx prescribing / dosing / alternate-drug information.

4 label annotations:

Agency	PGx level	Gene(s)	Label guidance	PharmGKB
FDA	Testing Required	ABL1, BCR, FIP1L1, KIT, PDGFRA, PDGFRB		PA166104790
EMA	Testing Required	ABL1, BCR, FIP1L1, KIT, PDGFRA, PDGFRB		PA166104926
PMDA	Testing Required	ABL1, BCR		PA166123542
HCSC	Testing Required	ABL1, BCR, FIP1L1, KIT, PDGFRA, PDGFRB		PA166127682

Pharmacogenomic clinical annotations (35) — variant × gene × association × phenotype, ranked by PharmGKB evidence level (1 strongest → 4):

Gene	Variant	Association	Phenotype	Level
ABCB1	rs1045642	Efficacy	Chronic myelogenous leukemia;BCR-ABL1 positive	3
ABCB1	rs1128503	Efficacy	Chronic myelogenous leukemia;BCR-ABL1 positive	3
ABCB1	rs2235040	Toxicity	Gastrointestinal Stromal Tumors	3
ABCB1	rs28656907	Dosage	Drug Toxicity;Gastrointestinal Stromal Tumors	3
ABCB4	rs1202283	Efficacy	Gastrointestinal Stromal Tumors	3
ABCC2	rs2273697	Efficacy	Gastrointestinal Stromal Tumors	3
ABCC4	rs9561765	Efficacy	Gastrointestinal Stromal Tumors	3
ABCG2	rs1061018	Other		3
ABCG2	rs12505410	Efficacy	Chronic myelogenous leukemia;BCR-ABL1 positive	3
ABCG2	rs13120400	Efficacy	Chronic myelogenous leukemia;BCR-ABL1 positive	3
ABCG2	rs2231137	Other		3
ABCG2	rs2231137	Dosage	Drug Toxicity;Gastrointestinal Stromal Tumors	3
ABCG2	rs2231142	Metabolism/PK		3
ABCG2	rs2725252	Efficacy	Chronic myelogenous leukemia;BCR-ABL1 positive	3
ABCG2	rs41282401	Other		3
ABCG2	rs45605536	Other		3
ABCG2	rs58818712	Other		3
BCL2L11	rs724710	Efficacy	Neoplasms	3
CHST1	rs9787901	Toxicity	Gastrointestinal Stromal Tumors	3
CYP1A2	rs762551	Dosage	Gastrointestinal Stromal Tumors	3
CYP2B6	rs3745274	Efficacy,Toxicity	Chronic myelogenous leukemia;BCR-ABL1 positive	3
CYP2F1	rs305968	Toxicity	Gastrointestinal Stromal Tumors	3
CYP3A4	CYP3A4*1, CYP3A4*3, CYP3A4*20, CYP3A4*22	Metabolism/PK		3
CYP3A5	rs776746	Metabolism/PK	Chronic myelogenous leukemia;BCR-ABL1 positive	3
EGFR	rs10258429	Toxicity	Gastrointestinal Stromal Tumors	3
GSTT1	GSTT1 non-null, GSTT1 null	Efficacy	Chronic myelogenous leukemia;BCR-ABL1 positive	3
NQO1	rs10517	Efficacy	Gastrointestinal Stromal Tumors	3
RUNDC3B	rs28656907	Dosage	Drug Toxicity;Gastrointestinal Stromal Tumors	3
SLC19A1	rs1051266	Toxicity	Gastrointestinal Stromal Tumors	3
SLC19A1	rs12659	Toxicity	Gastrointestinal Stromal Tumors	3
SLC22A1	rs628031	Efficacy,Toxicity,Metabolism/PK	Neoplasms	3
SLC22A1	rs683369	Efficacy,Metabolism/PK	Chronic myelogenous leukemia;BCR-ABL1 positive	3
SLC22A1	rs683369	Toxicity	Gastrointestinal Stromal Tumors	3
SLCO1A2	rs3764043	Metabolism/PK	Chronic myelogenous leukemia;BCR-ABL1 positive	3
ULK3	rs2290573	Efficacy	Chronic myelogenous leukemia;BCR-ABL1 positive	3

Published variant annotations — per-publication pharmacogenomic findings for this drug (significant associations only), each from a curated PharmGKB literature annotation:

showing 60 of 70 published findings:

Gene	Variant	Category	Finding	PMID
ABCA3	rs150929	Efficacy	Genotypes GG + GT is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotype TT.	PMID:25056761
ABCB1	rs1045642	Efficacy	Genotypes AA + AG is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotype GG.	PMID:22875622
ABCB1	rs1045642	Efficacy	Genotype GG is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AA + AG.	PMID:25245580
ABCB1	rs1045642	Metabolism/PK	Genotype AG is associated with decreased trough concentration of imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AA + GG.	PMID:27426203
ABCB1	rs1045642	Efficacy	Genotype AA is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AG + GG.	PMID:28367681
ABCB1	rs1045642	Metabolism/PK	Genotype AA is associated with increased concentrations of imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AG + GG.	PMID:28330783
ABCB1	rs1045642	Efficacy	Genotype GG is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AA + AG.	PMID:28289867
ABCB1	rs1045642	Efficacy	Allele A is associated with increased clinical benefit to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele G.	PMID:38640718
ABCB1	rs1045642	Metabolism/PK	Genotypes AG + GG is associated with increased trough concentration of imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype AA.	PMID:38756645
ABCB1	rs1045642	Toxicity	Allele A is associated with increased severity of Myelosuppression when treated with imatinib in people with Chronic myelomonocytic leukemia as compared to allele G.	PMID:40326103
ABCB1	rs1128503	Efficacy	Genotype GG is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AA + AG.	PMID:25245580
ABCB1	rs1128503	Efficacy	Genotype GG is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AA + AG.	PMID:28367681
ABCB1	rs1128503	Efficacy	Allele A is associated with increased clinical benefit to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele G.	PMID:38640718
ABCB1	rs2032582	Efficacy	Allele C is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive.	PMID:25245580
ABCB1	rs2032582	Efficacy	Genotypes AT + TT is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes CC + CT.	PMID:27991849
ABCB1	rs2032582	Efficacy	Allele A is associated with increased clinical benefit to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele C.	PMID:38640718
ABCB1	rs2235040	Toxicity	Genotype CT is associated with decreased risk of Drug Toxicity and Eye Disorder when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype CC.	PMID:28762371
ABCB4	rs1202283	Efficacy	Genotypes AA + AG is associated with increased progression-free survival when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype GG.	PMID:30237583
ABCC2	rs2273697	Efficacy	Genotype GG is associated with decreased progression-free survival when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes AA + AG.	PMID:30237583
ABCC4	rs9561765	Efficacy	Genotype AG is associated with increased response to imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype AA.	PMID:23127916
ABCG2	rs12505410	Efficacy	Allele G is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele T.	PMID:24123600
ABCG2	rs13120400	Efficacy	Genotypes CC + CT is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotype TT.	PMID:24123600
ABCG2	rs2231137	Dosage	Genotypes CT + TT are associated with decreased dose of imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype CC.	PMID:30713339
ABCG2	rs2231142	Efficacy	Genotype TT is associated with increased progression-free survival when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes GG + GT.	PMID:25417047
ABCG2	rs2231142	Efficacy	Allele T is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele G.	PMID:27991849
ABCG2	rs2231142	Toxicity	Allele T is associated with increased severity of Exanthema when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to allele G.	PMID:35144161
ABCG2	rs2231142	Metabolism/PK	Genotypes GT + TT is associated with increased dose-adjusted trough concentrations of imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype GG.	PMID:37212851
ABCG2	rs2231142	Efficacy	Allele T is associated with increased clinical benefit to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele G.	PMID:38640718
ABCG2	rs2231142	Efficacy	Genotype GT is associated with increased clinical benefit to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotype GG.	PMID:39714624
ABCG2	rs2231142	Other, Metabolism/PK	Genotype GT is associated with decreased metabolism of imatinib in people with Neoplasms as compared to genotype GG.	PMID:18981009
ABCG2	rs2725252	Efficacy	Genotypes AC + CC is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotype AA.	PMID:24123600
ARID5B	rs10821936	Efficacy	Genotype TT is associated with increased likelihood of treatment failure when treated with imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes CC + CT.	PMID:35205374
ATIC	rs2372536	Efficacy	Allele G is associated with increased likelihood of treatment failure when treated with imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes CC + CG.	PMID:35205374
BCL2L11	rs724710	Efficacy	Allele T is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele C.	PMID:24223824
CCL5	rs4796120	Toxicity	Genotypes AG + GG is associated with increased likelihood of Hypersensitivity when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype AA.	PMID:41193444
CHST1	rs9787901	Toxicity	Genotypes AA + AG is associated with increased risk of Drug Toxicity when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype GG.	PMID:30237583
CYP1A2	rs11636419	Toxicity	Genotype AA is associated with increased likelihood of periorbital edema when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes AG + GG.	PMID:37212851
CYP1A2	rs762551	Dosage	Genotype CC is associated with decreased dose of imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes AA + AC.	PMID:30713339
CYP2B6	rs3745274	Efficacy	Genotypes GG + GT is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotype TT.	PMID:24293093
CYP2F1	rs305968	Toxicity	Genotype AA is associated with increased risk of Drug Toxicity when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes AG + GG.	PMID:30237583
CYP3A4	rs2242480	Efficacy	Allele C is associated with increased clinical benefit to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele T.	PMID:38640718
CYP3A4	rs28371759	Efficacy	Genotype AG is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotype AA.	PMID:37706370
CYP3A5	rs776746	Metabolism/PK	Genotype CC is associated with increased trough concentration of imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes CT + TT.	PMID:27426203
CYP3A5	rs776746	Metabolism/PK	Genotype CC is associated with increased concentrations of imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes CT + TT.	PMID:28330783
CYP3A5	rs776746	Efficacy	Allele C is associated with increased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele T.	PMID:29427770
CYP3A5	rs776746	Efficacy	Allele C is associated with increased clinical benefit to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to allele T.	PMID:38640718
EGFR	rs10228436	Toxicity	Genotypes AG + GG is associated with decreased likelihood of Hypersensitivity when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype AA.	PMID:41193444
EGFR	rs10258429	Toxicity	Genotypes CT + TT is associated with increased risk of Drug Toxicity and Eye Disorder when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype CC.	PMID:28762371
EGFR	rs2072454	Toxicity	Genotype CC is associated with increased likelihood of periorbital edema when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes CT + TT.	PMID:37212851
FLT1	rs9551465	Toxicity	Genotype CC is associated with decreased likelihood of Myelosuppression when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes AA + AC.	PMID:41193444
FLT1	rs966	Toxicity	Genotype AA is associated with increased likelihood of Myelosuppression when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes AC + CC.	PMID:41193444
GSTT1	GSTT1 non-null, GSTT1 null	Efficacy	GSTT1 null/null is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to GSTT1 non-null/non-null + non-null/null.	PMID:25188725
NQO1	rs10517	Efficacy	Genotype GG is associated with decreased progression-free survival when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes AA + AG.	PMID:30237583
NR1I2	rs3814055	Toxicity	Genotype TT is associated with increased severity of Myelosuppression when treated with imatinib in people with Chronic myelomonocytic leukemia as compared to genotypes CC + CT.	PMID:40326103
SLC19A1	rs1051266	Toxicity	Genotype TT is associated with increased risk of Drug Toxicity when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes CC + CT.	PMID:30237583
SLC19A1	rs12659	Toxicity	Genotypes AG + GG is associated with decreased risk of Drug Toxicity when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotype AA.	PMID:30237583
SLC22A1	rs1867351	Toxicity	Genotype TT is associated with increased likelihood of periorbital edema when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes CC + CT.	PMID:37212851
SLC22A1	rs628031	Efficacy	Genotypes AA + AG is associated with decreased response to imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotype GG.	PMID:29427770
SLC22A1	rs628031	Toxicity	Genotype GG is associated with increased risk of Drug Toxicity when treated with imatinib in people with Gastrointestinal Stromal Tumors as compared to genotypes AA + AG.	PMID:30237583
SLC22A1	rs628031	Metabolism/PK	Genotype GG is associated with decreased clearance of imatinib in people with Leukemia, Myelogenous, Chronic, BCR-ABL Positive as compared to genotypes AA + AG.	PMID:23272163

PharmGKB pathway — curated pharmacokinetic / pharmacodynamic pathway diagrams for this drug:

• Imatinib Pathway, Pharmacokinetics/Pharmacodynamics — pharmacokinetic/pharmacodynamic

Adverse-event reports (FAERS)

63,262 reports across 4 FAERS drug-name records; 4,311 distinct MedDRA reactions.

openFDA FAERS — spontaneous post-marketing reports. Co-occurrence, not causation: reports are voluntary, unverified, and confounded by indication and reporting bias (the drug’s own indication often appears as a ‘reaction’). PRR is a disproportionality heuristic (reaction rate for this drug vs the FAERS background), NOT a risk estimate. Counts are pooled across the drug’s name records.

Most-reported events

Serious = reports flagged serious (death / life-threatening / hospitalisation / disability / other medically important).

50 reactions by report volume:

Reaction (MedDRA PT)	Reports	Serious	PRR
death	16,580	16,562 (100%)	10.2×
nausea	3,417	2,561 (75%)	1.7×
drug ineffective	3,238	2,418 (75%)	1.1×
diarrhoea	3,079	2,436 (79%)	1.8×
fatigue	2,556	1,964 (77%)	1.3×
malignant neoplasm progression	2,463	2,453 (100%)	9.0×
vomiting	2,374	1,983 (84%)	1.8×
dyspnoea	1,974	1,824 (92%)	1.2×
pyrexia	1,948	1,886 (97%)	1.9×
malaise	1,837	1,325 (72%)	1.5×
anaemia	1,788	1,724 (96%)	3.1×
rash	1,748	1,307 (75%)	1.5×
chronic myeloid leukaemia	1,563	1,558 (100%)	140.3×
drug intolerance	1,560	1,319 (85%)	8.4×
asthenia	1,557	1,400 (90%)	1.5×
drug resistance	1,515	1,408 (93%)	40.4×
headache	1,354	1,114 (82%)	0.8×
muscle spasms	1,344	991 (74%)	2.9×
gastrointestinal stromal tumour	1,327	1,316 (99%)	208.0×
pleural effusion	1,307	1,231 (94%)	8.4×
arthralgia	1,260	1,062 (84%)	1.1×
abdominal pain	1,254	1,169 (93%)	2.0×
pain	1,155	930 (81%)	0.7×
pneumonia	1,148	1,135 (99%)	1.2×
haemoglobin decreased	1,126	1,095 (97%)	3.9×
thrombocytopenia	1,126	1,119 (99%)	3.9×
dizziness	1,088	927 (85%)	0.8×
oedema peripheral	1,016	951 (94%)	3.1×
decreased appetite	1,010	900 (89%)	1.6×
disease progression	1,007	941 (93%)	5.2×
myalgia	1,007	867 (86%)	2.5×
off label use	1,000	867 (87%)	0.8×
second primary malignancy	979	979 (100%)	59.4×
pruritus	978	819 (84%)	1.0×
fall	972	903 (93%)	1.1×
platelet count decreased	965	907 (94%)	3.2×
abdominal pain upper	936	797 (85%)	1.6×
neoplasm malignant	929	925 (100%)	8.9×
sepsis	896	892 (100%)	3.0×
neutropenia	883	870 (99%)	2.6×
cough	882	798 (90%)	1.1×
oedema	866	763 (88%)	5.3×
pain in extremity	808	674 (83%)	1.0×
blast crisis in myelogenous leukaemia	804	804 (100%)	358.6×
white blood cell count increased	804	747 (93%)	7.8×
drug interaction	803	767 (96%)	2.7×
weight decreased	797	705 (88%)	1.0×
pancytopenia	754	746 (99%)	4.7×
white blood cell count decreased	737	667 (91%)	2.4×
fluid retention	701	580 (83%)	5.6×

Strongest disproportionality

Reactions over-reported for this drug vs the FAERS background (PRR), among those with ≥ 10 reports (a high PRR off a few reports is noise, not signal).

50 reactions by disproportionality:

Reaction (MedDRA PT)	Reports	Serious	PRR
ankle brachial index decreased	10	10 (100%)	926.1×
carotid intima-media thickness increased	12	12 (100%)	538.8×
chordoma	39	39 (100%)	537.5×
oral pigmentation	18	14 (78%)	523.0×
chronic myeloid leukaemia (in remission)	12	11 (92%)	485.5×
philadelphia chromosome positive	305	300 (98%)	427.2×
necrotising panniculitis	17	17 (100%)	424.8×
transdifferentiation of neoplasm	11	11 (100%)	388.1×
blast crisis in myelogenous leukaemia	804	804 (100%)	358.6×
cytogenetic analysis abnormal	589	525 (89%)	342.7×
chronic myeloid leukaemia recurrent	245	245 (100%)	337.6×
chronic myeloid leukaemia transformation	206	206 (100%)	254.8×
amaurosis fugax	258	258 (100%)	236.0×
chromosome analysis abnormal	128	125 (98%)	210.0×
polymerase chain reaction positive	93	90 (97%)	208.9×
gastrointestinal stromal tumour	1,327	1,316 (99%)	208.0×
clonal evolution	22	20 (91%)	185.8×
leukaemic infiltration brain	14	14 (100%)	167.1×
pancreatic toxicity	15	15 (100%)	161.2×
oncologic complication	163	163 (100%)	153.3×
gene mutation identification test positive	146	137 (94%)	149.5×
lactobacillus infection	14	14 (100%)	141.1×
chronic myeloid leukaemia	1,563	1,558 (100%)	140.3×
desmoid tumour	33	33 (100%)	138.4×
drug resistance mutation	18	17 (94%)	134.6×
pseudoporphyria	44	43 (98%)	133.7×
central nervous system neoplasm	22	22 (100%)	125.1×
endocarditis noninfective	11	11 (100%)	120.7×
trisomy 8	14	13 (93%)	115.4×
chest expansion decreased	10	10 (100%)	114.8×
philadelphia positive chronic myeloid leukaemia	22	22 (100%)	113.2×
philadelphia positive acute lymphocytic leukaemia	26	26 (100%)	110.5×
pituitary apoplexy	15	15 (100%)	109.6×
polymerase chain reaction	20	19 (95%)	109.2×
gastric antral vascular ectasia	94	94 (100%)	105.7×
osteonecrosis of external auditory canal	19	19 (100%)	104.0×
blast cell crisis	78	78 (100%)	100.4×
hepatic calcification	10	10 (100%)	96.8×
typhoid fever	33	33 (100%)	94.4×
chronic graft versus host disease in lung	10	10 (100%)	94.4×
malignant tumour excision	14	14 (100%)	91.5×
leukostasis syndrome	11	11 (100%)	90.8×
adenovirus reactivation	11	11 (100%)	87.2×
acute lymphocytic leukaemia recurrent	295	294 (100%)	86.0×
graft versus host disease in lung	40	40 (100%)	83.0×
chronic graft versus host disease in skin	73	73 (100%)	82.6×
graft versus host disease in eye	21	21 (100%)	81.6×
metamyelocyte count increased	14	14 (100%)	79.5×
adrenomegaly	10	10 (100%)	74.8×
myelocyte count increased	12	12 (100%)	71.1×

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.

129 molecules share ≥1 primary target. Top 100 by shared-target count:

Molecule	Source	Status	Shared targets
Afatinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
CABOZANTINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
CRIZOTINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
DASATINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
ENTRECTINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
ERLOTINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
FEDRATINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
Gefitinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
Ibrutinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
Lapatinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
PAZOPANIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
PONATINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
QUIZARTINIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
REGORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
Ruxolitinib	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
SORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
Tirbanibulin	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
TOVORAFENIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
VANDETANIB	ChEMBL + PubChem	Phase 4 (approved)	ABL1, DDR1, DDR2
AXITINIB	ChEMBL	Phase 4 (approved)	ABL1, DDR1, DDR2
BOSUTINIB	ChEMBL	Phase 4 (approved)	ABL1, DDR1, DDR2
LENVATINIB	ChEMBL	Phase 4 (approved)	ABL1, DDR1, DDR2
NILOTINIB	ChEMBL	Phase 4 (approved)	ABL1, DDR1, DDR2
NINTEDANIB	ChEMBL	Phase 4 (approved)	ABL1, DDR1, DDR2
SUNITINIB	ChEMBL	Phase 4 (approved)	ABL1, DDR1, DDR2
TIVOZANIB	ChEMBL	Phase 4 (approved)	ABL1, DDR1, DDR2
CEDIRANIB	ChEMBL	Phase 3	ABL1, DDR1, DDR2
DOVITINIB	ChEMBL	Phase 3	ABL1, DDR1, DDR2
LESTAURTINIB	ChEMBL	Phase 3	ABL1, DDR1, DDR2
LINIFANIB	ChEMBL	Phase 3	ABL1, DDR1, DDR2
MASITINIB	ChEMBL	Phase 3	ABL1, DDR1, DDR2
SARACATINIB	ChEMBL	Phase 3	ABL1, DDR1, DDR2
TESEVATINIB	ChEMBL	Phase 3	ABL1, DDR1, DDR2
AEE-788	ChEMBL	Phase 2	ABL1, DDR1, DDR2
BAFETINIB	ChEMBL	Phase 2	ABL1, DDR1, DDR2
BMS-777607	ChEMBL	Phase 2	ABL1, DDR1, DDR2
CEP-32496	ChEMBL	Phase 2	ABL1, DDR1, DDR2
DANUSERTIB	ChEMBL	Phase 2	ABL1, DDR1, DDR2
DEFOSBARASERTIB	ChEMBL	Phase 2	ABL1, DDR1, DDR2
DORAMAPIMOD	ChEMBL	Phase 2	ABL1, DDR1, DDR2
ENMD-2076	ChEMBL	Phase 2	ABL1, DDR1, DDR2
FORETINIB	ChEMBL	Phase 2	ABL1, DDR1, DDR2
GLESATINIB	ChEMBL	Phase 2	ABL1, DDR1, DDR2
GOLVATINIB	ChEMBL	Phase 2	ABL1, DDR1, DDR2
MILCICLIB	ChEMBL	Phase 2	ABL1, DDR1, DDR2
OSI-632	ChEMBL	Phase 2	ABL1, DDR1, DDR2
PEXMETINIB	ChEMBL	Phase 2	ABL1, DDR1, DDR2
R-406	ChEMBL	Phase 2	ABL1, DDR1, DDR2
RAF-265	ChEMBL	Phase 2	ABL1, DDR1, DDR2
REBASTINIB	ChEMBL	Phase 2	ABL1, DDR1, DDR2
TOZASERTIB	ChEMBL	Phase 2	ABL1, DDR1, DDR2
Binimetinib	PubChem	Approved	ABL1, DDR1, DDR2
dacomitinib	PubChem	Approved	ABL1, DDR1, DDR2
Fostamatinib	PubChem	Approved	ABL1, DDR1, DDR2
Idelalisib	PubChem	Approved	ABL1, DDR1, DDR2
Selumetinib	PubChem	Approved	ABL1, DDR1, DDR2
Trametinib	PubChem	Approved	ABL1, DDR1, DDR2
MIDOSTAURIN	ChEMBL	Phase 4 (approved)	ABL1, DDR1
BRIVANIB	ChEMBL	Phase 3	ABL1, DDR1
CANERTINIB	ChEMBL	Phase 3	ABL1, DDR1
MOTESANIB	ChEMBL	Phase 3	ABL1, DDR1
NAPORAFENIB	ChEMBL	Phase 3	DDR1, DDR2
BELVARAFENIB	ChEMBL	Phase 2	DDR1, DDR2
BMS-754807	ChEMBL	Phase 2	ABL1, DDR1
LUCITANIB	ChEMBL	Phase 2	DDR1, DDR2
MERESTINIB	ChEMBL	Phase 2	DDR1, DDR2
NEFLAMAPIMOD	ChEMBL	Phase 2	ABL1, DDR1
SU-014813	ChEMBL	Phase 2	ABL1, DDR2
TANDUTINIB	ChEMBL	Phase 2	DDR1, DDR2
TG100-801	ChEMBL	Phase 2	ABL1, DDR1
Capivasertib	PubChem	Approved	DDR1, DDR2
Capmatinib	PubChem	Approved	DDR1, DDR2
Cobimetinib	PubChem	Approved	DDR1, DDR2
Momelotinib	PubChem	Approved	DDR1, DDR2
Pexidartinib	PubChem	Approved	DDR1, DDR2
Tepotinib	PubChem	Approved	DDR1, DDR2
AFATINIB DIMALEATE	ChEMBL	Phase 4 (approved)	ABL1
ASCIMINIB	ChEMBL	Phase 4 (approved)	ABL1
BIOTIN	ChEMBL	Phase 4 (approved)	ABL1
BRIGATINIB	ChEMBL	Phase 4 (approved)	ABL1
CERITINIB	ChEMBL	Phase 4 (approved)	ABL1
DABRAFENIB	ChEMBL	Phase 4 (approved)	ABL1
DACTINOMYCIN	ChEMBL	Phase 4 (approved)	DDR2
FILGOTINIB	ChEMBL	Phase 4 (approved)	ABL1
INFIGRATINIB	ChEMBL	Phase 4 (approved)	ABL1
MEBENDAZOLE	ChEMBL	Phase 4 (approved)	ABL1
NERATINIB	ChEMBL	Phase 4 (approved)	ABL1
PACRITINIB	ChEMBL	Phase 4 (approved)	DDR1
TOFACITINIB	ChEMBL	Phase 4 (approved)	ABL1
ALISERTIB	ChEMBL	Phase 3	ABL1
ALVOCIDIB	ChEMBL	Phase 3	ABL1
BRIVANIB ALANINATE	ChEMBL	Phase 3	DDR1
DEFACTINIB	ChEMBL	Phase 3	ABL1
FLUMATINIB	ChEMBL	Phase 3	ABL1
OLVEREMBATINIB	ChEMBL	Phase 3	ABL1
RADOTINIB	ChEMBL	Phase 3	ABL1
RESVERATROL	ChEMBL	Phase 3	ABL1
SEMAXANIB	ChEMBL	Phase 3	ABL1
TANESPIMYCIN	ChEMBL	Phase 3	ABL1
VATALANIB	ChEMBL	Phase 3	DDR1