Imatinib
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Also known as GlamoxNSC-743414NSC-759854GLEEVECSTI-571IMATINIB MESYLATEGLIVECCGP-57148BSTI571CGP057148BST-1571IMATINIB (STI571)SID26755316SID29215405SID124892207SID124892208SID103905596Imatinib (STI-571)SID124892209
Summary
Imatinib (CHEMBL941) is an approved small-molecule tyrosine kinase inhibitor (ATC L01EA01) targeting DDR1, DDR2, and ABL1; indicated across 52 conditions including acute lymphoblastic leukemia and chronic myeloid leukemia; with CIViC clinical evidence for 203 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: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EA01
- Targets: 3 (DDR1, DDR2, ABL1)
- Indications: 52 conditions
- Clinical trials: 469
- Precision-oncology evidence (CIViC): 203 variant–indication associations
- Chemistry: 493.6 Da · C29H31N7O
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, antineoplastic agent, 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: 28,675 distinct patent families (111,611 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 109,700 (98%) 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 |
|---|---|---|---|---|---|
| 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 |
Broader ChEMBL bioactivity targets: 85 (assay-derived). Sample: Homeodomain-interacting protein kinase 4, Nuclear receptor ROR-gamma, Prelamin-A/C, Solute carrier family 22 member 2, Multidrug and toxin extrusion protein 1, Multidrug and toxin extrusion protein 2, Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma, Receptor tyrosine-protein kinase erbB-2, Thromboxane-A synthase, Tyrosine-protein kinase Fyn.
Bioactivity
ChEMBL activities: 407 potent at pChembl ≥ 5 of 430 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| ERBB2 | 10.22 | IC50 | 0.06 | nM | CHEMBL_ACT_24962908 |
| EGFR | 9.96 | IC50 | 0.11 | nM | CHEMBL_ACT_24962906 |
| DDR1 | 9.15 | Kd | 0.7 | nM | CHEMBL_ACT_2903445 |
| DDR1 | 9.15 | Kd | 0.7 | nM | CHEMBL_ACT_7568175 |
| DDR1 | 9.1 | Kd | 0.79 | nM | CHEMBL_ACT_18910095 |
| ABL1 | 9 | Kd | 1 | nM | CHEMBL_ACT_18910094 |
| ABL1 | 8.96 | IC50 | 1.1 | nM | CHEMBL_ACT_3186208 |
| ABL1 | 8.96 | Kd | 1.1 | nM | CHEMBL_ACT_7569852 |
| ABL1 | 8.74 | Kd | 1.8 | nM | CHEMBL_ACT_7569847 |
| PDGFRA | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_13418824 |
| ABL1 | 8.66 | Kd | 2.2 | nM | CHEMBL_ACT_1651429 |
| ABL1 | 8.6 | Kd | 2.5 | nM | CHEMBL_ACT_7569842 |
| ABL1 | 8.55 | IC50 | 2.79 | nM | CHEMBL_ACT_24729011 |
| PDGFRA | 8.55 | IC50 | 2.8 | nM | CHEMBL_ACT_29279125 |
| PDGFRA | 8.34 | IC50 | 4.6 | nM | CHEMBL_ACT_18057971 |
| ABL1 | 8.34 | IC50 | 4.6 | nM | CHEMBL_ACT_29094610 |
| ABL1 | 8.23 | Kd | 5.9 | nM | CHEMBL_ACT_7569844 |
| ABL2 | 8.22 | Kd | 6 | nM | CHEMBL_ACT_6174264 |
| BCR | 8.15 | Kd | 7 | nM | CHEMBL_ACT_17884711 |
| ABL1 | 8.08 | Kd | 8.3 | nM | CHEMBL_ACT_7569840 |
| ABL1 | 8.07 | Kd | 8.5 | nM | CHEMBL_ACT_2895371 |
| CSF1R | 8 | Kd | 10 | nM | CHEMBL_ACT_18910092 |
| ABL2 | 8 | Kd | 10 | nM | CHEMBL_ACT_18910093 |
| ABL2 | 8 | Kd | 10 | nM | CHEMBL_ACT_22969941 |
| ABL2 | 8 | Kd | 10 | nM | CHEMBL_ACT_2895523 |
| ABL2 | 8 | Kd | 10 | nM | CHEMBL_ACT_7569854 |
| P00520 | 7.97 | IC50 | 10.8 | nM | CHEMBL_ACT_3397785 |
| CSF1R | 7.96 | Kd | 11 | nM | CHEMBL_ACT_7569856 |
| ABL1 | 7.92 | Kd | 12 | nM | CHEMBL_ACT_2894829 |
| KIT | 7.9 | Kd | 12.59 | nM | CHEMBL_ACT_18910091 |
Target pathways
Aggregated over 3 target gene(s): DDR1, DDR2, ABL1.
Top Reactome pathways
54 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| 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 |
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 |
| positive regulation of ERK1 and ERK2 cascade | 2 |
| cellular response to transforming growth factor beta stimulus | 2 |
| regulation of cell growth | 1 |
| regulation of cell-matrix adhesion | 1 |
| embryo implantation | 1 |
| lactation | 1 |
Indications & clinical
Indications
52 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial 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 |
| pulmonary arterial hypertension | 3 | MONDO:0015924 | EFO:0001361 |
| stroke disorder | 3 | MONDO:0005098 | EFO:0000712 |
| myeloid leukemia | 3 | MONDO:0004643 | MONDO:0004643 |
| pulmonary hypertension | 3 | MONDO:0005149 | MONDO:0005149 |
| graft versus host disease | 3 | MONDO:0013730 | MONDO:0013730 |
| severe acute respiratory syndrome | 3 | MONDO:0005091 | MONDO:0100096 |
| gastrointestinal stromal tumor | 3 | MONDO:0011719 | MONDO:0011719 |
| 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 | MONDO:0007254 |
| lung neoplasm | 2 | MONDO:0021117 | MONDO:0008903 |
| spinal cord injury | 2 | MONDO:0043797 | EFO:1001919 |
| desmoid tumor | 2 | MONDO:0007608 | EFO:0009907 |
| chordoma | 2 | MONDO:0008978 | MONDO:0008978 |
| tuberculosis | 2 | MONDO:0018076 | MONDO:0018076 |
| lymphoid leukemia | 2 | MONDO:0005402 | EFO:0004289 |
| clear cell renal carcinoma | 1 | MONDO:0005005 | EFO:0000349 |
| colorectal adenocarcinoma | 1 | MONDO:0005008 | EFO:0000365 |
| fibrosarcoma | 1 | MONDO:0005164 | EFO:0002087 |
| anaplastic large cell lymphoma | 1 | MONDO:0020325 | EFO:0003032 |
| seasonal allergic rhinitis | 1 | MONDO:0005324 | EFO:0003956 |
| acute lung injury | 1 | MONDO:0015796 | EFO:0004610 |
| non-Hodgkin lymphoma | 1 | MONDO:0018908 | EFO:0005952 |
| desmoplastic small round cell tumor | 1 | MONDO:0019373 | EFO:1000895 |
| thymic carcinoma | 1 | MONDO:0006451 | EFO:1000576 |
| hematopoietic and lymphoid system neoplasm | 1 | MONDO:0002334 | MONDO:0044881 |
| cirrhosis of liver | 1 | MONDO:0005155 | EFO:0001422 |
| malignant pancreatic neoplasm | 1 | MONDO:0009831 | EFO:1000359 |
| colorectal neoplasm | 1 | MONDO:0005335 | MONDO:0005575 |
| head and neck squamous cell carcinoma | 0 | MONDO:0010150 | EFO:0000181 |
| head and neck cancer | 0 | MONDO:0005627 | EFO:0006859 |
3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 469.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 239 |
| PHASE3 | 72 |
| PHASE1 | 61 |
| PHASE1/PHASE2 | 44 |
| Not specified | 29 |
| PHASE4 | 18 |
| PHASE2/PHASE3 | 3 |
| EARLY_PHASE1 | 3 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT03844360 | PHASE4 | RECRUITING | Dose Individualization of Antineoplastic Drugs and Anti-Infective Drug in Children With Hematoplastic Disease |
| NCT04877522 | PHASE4 | RECRUITING | Asciminib Roll-over Study |
| NCT05367765 | PHASE4 | 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 | PHASE4 | COMPLETED | Gleevec Trial in Patients With Newly Diagnosed Chronic Phase Chronic Myelogenous Leukemia |
| NCT00171899 | PHASE4 | COMPLETED | Study Comparing Standard Dose and High-dose Imatinib Mesylate in Patients With Chronic Phase Philadelphia Chromosome Positive (Ph+) Chronic Myelogenous Leukemia (CML) |
| NCT00171977 | PHASE4 | COMPLETED | Post-Marketing Clinical Study of Postoperative Adjuvant Therapy With Imatinib Mesylate in Patients With Gastrointestinal Stromal Tumors (GIST) |
| NCT00372476 | PHASE4 | COMPLETED | Efficacy and Safety of Imatinib and Vinorelbine in Patients With Advanced Breast Cancer |
| NCT00390897 | PHASE4 | COMPLETED | Glivec® (Imatinib Mesylate, STI571) in Monotherapy Versus Glivec®-Interferon Alpha in the Treatment of Chronic-Phase Chronic Myeloid Leukaemia |
| NCT00510354 | PHASE4 | COMPLETED | Treatment of Patients With Everolimus and Imatinib Mesylate Who Have Progressive Gastro Intestinal Stromal Tumors (GIST) and Are Resistant to Imatinib Mesylate |
| NCT01297777 | PHASE4 | COMPLETED | Imatinib in KIT-negative Systemic Mastocytosis |
| NCT01491763 | PHASE4 | UNKNOWN | Chemotherapy and Imatinib in Young Adults With Acute Lymphoblastic Leukemia Ph (BCR-ABL) POSITIVE |
| NCT01578213 | PHASE4 | COMPLETED | Validation of Digital-PCR Analysis Through Programmed Imatinib Interruption in PCR Negative CML Patients |
| NCT01742299 | PHASE4 | 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 | PHASE4 | UNKNOWN | Efficacy and Safety of Imatinib Mesylate as First-line Treatment for the Patients With Chronic Phase of Chronic Myeloid Leukemia |
| NCT02602314 | PHASE4 | UNKNOWN | Sustained Treatment-free Remission in BCR-ABL+ Chronic Myeloid Leukemia |
| NCT02894645 | PHASE4 | UNKNOWN | Malaysia-Singapore Acute Lymphoblastic Leukemia 2010 Study |
| NCT05071482 | PHASE4 | TERMINATED | Flumatinib Versus Imatinib Combined With Chemotherapy for de Novo Ph+ ALL |
| NCT05220280 | PHASE4 | UNKNOWN | SOLIDARITY Finland Plus Long-COVID |
| NCT02413736 | PHASE3 | ACTIVE_NOT_RECRUITING | Three Versus Five Years of Adjuvant Imatinib as Treatment of Patients With Operable GIST |
| NCT02735707 | PHASE3 | RECRUITING | Randomized, Embedded, Multifactorial Adaptive Platform Trial for Community- Acquired Pneumonia |
| NCT03007147 | PHASE3 | ACTIVE_NOT_RECRUITING | Imatinib Mesylate and Combination Chemotherapy in Treating Patients With Newly Diagnosed Philadelphia Chromosome Positive Acute Lymphoblastic Leukemia |
| NCT03589326 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Ponatinib Versus Imatinib in Adults With Acute Lymphoblastic Leukemia |
| NCT03722420 | PHASE3 | ACTIVE_NOT_RECRUITING | Randomized Evaluation of Radotinib Versus Imatinib in Phase III Study for Efficacy With Chinese Patients (RERISE China) |
| NCT04307576 | PHASE3 | RECRUITING | A Treatment Study Protocol for Participants 0-45 Years With Acute Lymphoblastic Leukaemia |
| NCT04722848 | PHASE3 | ACTIVE_NOT_RECRUITING | Sequential Treatment With Ponatinib and Blinatumomab vs Chemotherapy and Imatinib in Newly Diagnosed Adult Ph+ ALL |
| NCT04971226 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Oral Asciminib Versus Other TKIs in Adult Patients With Newly Diagnosed Ph+ CML-CP |
| NCT05970900 | PHASE3 | NOT_YET_RECRUITING | Preoperative Imatinib Mesylate Combined With Rectal-sparing Surgery in Patients With c-KIT Gene-mutant Rectal GIST |
| NCT06682169 | PHASE3 | 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 | PHASE3 | NOT_YET_RECRUITING | A Phase III Randomized Controlled Trial Evaluating the Efficacy and Safety of Tofacitinib Combined With Imatinib in Patients With Moderate-to-Severe Palmoplantar Pustulosis |
| NCT07585266 | PHASE3 | NOT_YET_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 | PHASE3 | COMPLETED | Stem Cell Transplantation Compared With Standard Chemotherapy in Treating Patients With Acute Lymphoblastic Leukemia in First Remission |
| NCT00006343 | PHASE3 | COMPLETED | STI571 Compared With Interferon Alfa Plus Cytarabine in Treating Patients With Newly Diagnosed Chronic Myelogenous Leukemia |
| NCT00009906 | PHASE3 | TERMINATED | Comparison of Two Different Doses of STI571 in Treating Patients With Metastatic or Unresectable Gastrointestinal Stromal Tumor |
| NCT00022737 | PHASE3 | COMPLETED | Combination Chemotherapy With or Without Peripheral Stem Cell Transplant in Treating Children With Acute Lymphoblastic Leukemia |
| NCT00041197 | PHASE3 | COMPLETED | Imatinib Mesylate in Treating Patients With Primary Gastrointestinal Stromal Tumor That Has Been Completely Removed By Surgery |
| NCT00050531 | PHASE3 | COMPLETED | High-Dose Gleevec Alone or in Combination With Peg-Intron and GM-CSF in Early Phase Chronic Myelogenous Leukemia (CML) |
| NCT00055874 | PHASE3 | 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 | PHASE3 | COMPLETED | Imatinib Mesylate or Observation Only in Treating Patients Who Have Undergone Surgery for Localized Gastrointestinal Stromal Tumor |
| NCT00116935 | PHASE3 | COMPLETED | Study Comparing 12 Months Versus 36 Months of Imatinib in the Treatment of Gastrointestinal Stromal Tumor (GIST) |
| NCT00124748 | PHASE3 | TERMINATED | Efficacy of 400 Mg Versus 800 Mg Imatinib in Chronic Myeloid Leukemia in Chronic Phase Patients - TOPS (Tyrosine Kinase Inhibitor Optimization and Selectivity) |
Clinical evidence (CIViC)
Variant × indication × effect (203 predictive associations from 263 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| FIP1L1::PDGFRA Fusion | Myeloid And Lymphoid Neoplasms With Eosinophilia And Abnormalities Of PDGFRA, PDGFRB, And FGFR1 | Sensitivity/Response | Imatinib | CIViC A | EID1445 +2 |
| KIT Exon 11 Mutation | Gastrointestinal Stromal Tumor | Sensitivity/Response | Imatinib | CIViC A | EID654 +2 |
| BCR::ABL1 Fusion | Chronic Myeloid Leukemia | Sensitivity/Response | Imatinib | CIViC A | EID260 +1 |
| KIT Exon 9 Mutation | Gastrointestinal Stromal Tumor | Sensitivity/Response | Imatinib | CIViC A | EID1221 +1 |
| PDGFRB Fusion | Myeloproliferative Neoplasm | Sensitivity/Response | Imatinib | CIViC A | EID11272 +1 |
| BCR::ABL1 Fusion | Acute Myeloid Leukemia | Sensitivity/Response | Imatinib | CIViC A | EID259 |
| COL1A1::PDGFB Fusion | Dermatofibrosarcoma Protuberans | Sensitivity/Response | Imatinib | CIViC A | EID11271 |
| FIP1L1::PDGFRA Fusion | Myeloproliferative Neoplasm | Sensitivity/Response | Imatinib | CIViC A | EID11273 |
| KIT Mutation | Gastrointestinal Stromal Tumor | Sensitivity/Response | Imatinib | CIViC A | EID11282 |
| PDGFRA D842V | Gastrointestinal Stromal Tumor | Sensitivity/Response | Imatinib | CIViC A | EID11545 |
| PDGFRA Mutation | Gastrointestinal Stromal Tumor | Sensitivity/Response | Imatinib | CIViC B | EID11331 +1 |
| BCL2L11 Deletion Polymorphism | Chronic Myeloid Leukemia | Sensitivity/Response | Imatinib | CIViC B | EID9701 |
| CTNNB1 S45F | Desmoid Tumor | Sensitivity/Response | Imatinib | CIViC B | EID11018 |
| ETV6::ABL1 Fusion | Myeloid Neoplasm | Sensitivity/Response | Imatinib + Dasatinib + Nilotinib | CIViC B | EID11326 |
| IKZF1 Deletion | B-lymphoblastic Leukemia/lymphoma | Sensitivity/Response | Methotrexate + Daunorubicin + Cytarabine + Fludarabine + Imatinib | CIViC B | EID7366 |
| KIT EXPRESSION | Gastrointestinal Stromal Tumor | Sensitivity/Response | Imatinib | CIViC B | EID2480 |
| KIT Exon 11 Mutation | Melanoma | Sensitivity/Response | Imatinib | CIViC B | EID58 |
| KIT Mutation | Melanoma | Sensitivity/Response | Imatinib | CIViC B | EID1222 |
| KIT Y503_F504insAY | Gastrointestinal Stromal Tumor | Sensitivity/Response | Imatinib | CIViC B | EID2394 |
| NOT KIT D816V | Systemic Mastocytosis | Sensitivity/Response | Imatinib | CIViC B | EID11158 |
| KIT Exon 11 W557del/K558del | Gastrointestinal Stromal Tumor | Reduced Sensitivity | Imatinib | CIViC B | EID12935 |
| KIT Exon 9 Mutation | Gastrointestinal Stromal Tumor | Reduced Sensitivity | Imatinib | CIViC B | EID2477 |
| BCR::ABL1 Fusion AND ABL1 T315I | Chronic Myeloid Leukemia | Resistance | Imatinib | CIViC B | EID234 +4 |
| KIT Q694K | Gastrointestinal Stromal Tumor | Resistance | Imatinib | CIViC B | EID2498 +4 |
| KIT S692L | Gastrointestinal Stromal Tumor | Resistance | Imatinib | CIViC B | EID2493 +4 |
| PDGFRA D842V | Gastrointestinal Stromal Tumor | Resistance | Imatinib | CIViC B | EID15 +4 |
| KIT S501_A502INSAY | Gastrointestinal Stromal Tumor | Resistance | Imatinib | CIViC B | EID2855 +3 |
| KIT T661I | Gastrointestinal Stromal Tumor | Resistance | Imatinib | CIViC B | EID2491 +3 |
| BCL2L11 Deletion Polymorphism | Chronic Myeloid Leukemia | Resistance | Imatinib | CIViC B | EID1280 |
| KIT Amplification | Mucosal Melanoma | Resistance | Imatinib | CIViC B | EID1466 |
+173 more predictive associations (showing top 30 by level).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 39 clinical and 212 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.
129 molecules share ≥1 primary target. Top 60 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 |
| Dabrafenib | ChEMBL + PubChem | Phase 4 (approved) | ABL1, DDR1 |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | ABL1, DDR1 |
| BRIVANIB | ChEMBL | Phase 3 | ABL1, DDR1 |
Related Atlas pages
- Genes: DDR1, DDR2, ABL1
- Diseases: acute lymphoblastic leukemia, chronic myeloid leukemia, leukemia, neoplasm, sarcoma, pulmonary arterial hypertension, stroke disorder, myeloid leukemia, pulmonary hypertension, graft versus host disease, severe acute respiratory syndrome, gastrointestinal stromal tumor, pneumonia, influenza, myeloid/lymphoid neoplasms associated with eosinophilia and abnormality of PDGFRA, PDGFRB, FGFR1 or JAK2, myeloproliferative neoplasm, acute myeloid leukemia by FAB classification, dermatofibrosarcoma protuberans, desmoid tumor, myeloid neoplasm, B-cell acute lymphoblastic leukemia, melanoma, systemic mastocytosis, mucosal melanoma
- Drugs: Afatinib, Cabozantinib, Crizotinib, Dasatinib, Entrectinib, Erlotinib, Fedratinib, Gefitinib, Ibrutinib, Lapatinib, Pazopanib, Ponatinib, Quizartinib, Regorafenib, Ruxolitinib, Sorafenib, Tirbanibulin, Tovorafenib, Vandetanib, Axitinib, Bosutinib, Lenvatinib, Nilotinib, Nintedanib, Sunitinib, Tivozanib, Cediranib, Dovitinib, Lestaurtinib, Linifanib, Masitinib, Saracatinib, Tesevatinib, Binimetinib, dacomitinib, Fostamatinib, Idelalisib, Selumetinib, Trametinib, Dabrafenib, Midostaurin, Brivanib
- Biomarker genes: BCL2L11, CTNNB1, KIT, PDGFRA