Nilotinib
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Also known as AMN 107AMN-107AMN107NSC-747599SID124894352SID99460838TasignaSID124894351NILOTINIB (AMN-107)Nilotinib hydrochloride monohydrateÊNilotinib hydrochloride monohydrateÂNilotinib
Summary
Nilotinib (CHEMBL255863) is an approved small-molecule antineoplastic agent (ATC L01EA03) targeting DDR1, DDR2, and ABL1; indicated across 27 conditions including neoplasm and chronic myeloid leukemia; with CIViC clinical evidence for 55 variant-indication associations (e.g. BCR::ABL1 Fusion in b-lymphoblastic leukemia/lymphoma).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EA03
- Targets: 3 (DDR1, DDR2, ABL1)
- Indications: 27 conditions
- Clinical trials: 161
- Precision-oncology evidence (CIViC): 55 variant–indication associations
- Chemistry: 529.5 Da · C28H22F3N7O
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL255863 |
| Name | Nilotinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 644241 |
| ChEBI | CHEBI:52172 |
| ATC | L01EA03 |
| Molecular formula | C28H22F3N7O |
| Molecular weight | 529.5 |
| InChIKey | HHZIURLSWUIHRB-UHFFFAOYSA-N |
SMILES: CC1=C(C=C(C=C1)C(=O)NC2=CC(=CC(=C2)C(F)(F)F)N3C=C(N=C3)C)NC4=NC=CC(=N4)C5=CN=CC=C5
IUPAC name: 4-methyl-N-[3-(4-methylimidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide
Pharmacological roles (ChEBI): antineoplastic agent, tyrosine kinase inhibitor, anticoronaviral agent.
Also known as: AMN 107, AMN-107, AMN107, Nilotinib, NSC-747599, nilotinib, SID124894352, SID99460838, Tasigna, SID124894351, NILOTINIB, NILOTINIB (AMN-107)
Parent form; salt/anhydrous children: CHEMBL1201740, CHEMBL6068409
Patent coverage: 10,155 distinct patent families (38,627 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 38,522 (100%) 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 | 7.37 | 0.1% | Q08345 |
| DDR2 | discoidin domain receptor tyrosine kinase 2 | Inhibition | 9.3 | 0% | Q16832 |
| ABL1 | ABL proto-oncogene 1, non-receptor tyrosine kinase | Inhibition | 7.8 | 1.2% | P00519 |
Broader ChEMBL bioactivity targets: 90 (assay-derived). Sample: Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma, Receptor-interacting serine/threonine-protein kinase 3, Tyrosine-protein kinase Fyn, Macrophage colony-stimulating factor 1 receptor, Tyrosine-protein kinase ABL1, RAF proto-oncogene serine/threonine-protein kinase, Calcium-dependent protein kinase 1, Platelet-derived growth factor receptor beta, Mast/stem cell growth factor receptor Kit, Receptor-type tyrosine-protein kinase FLT3.
Bioactivity
ChEMBL activities: 222 potent at pChembl ≥ 5 of 228 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| ABL1 | 9.48 | IC50 | 0.33 | nM | CHEMBL_ACT_13280053 |
| ABL1 | 9.06 | IC50 | 0.87 | nM | CHEMBL_ACT_26276617 |
| ABL1 | 9 | IC50 | 1 | nM | CHEMBL_ACT_24707069 |
| ABL1 | 8.96 | IC50 | 1.1 | nM | CHEMBL_ACT_26276633 |
| DDR1 | 8.96 | Kd | 1.1 | nM | CHEMBL_ACT_7594531 |
| ABL1 | 8.92 | IC50 | 1.2 | nM | CHEMBL_ACT_20704576 |
| DDR2 | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_14665982 |
| ABL1 | 8.66 | IC50 | 2.2 | nM | CHEMBL_ACT_26276621 |
| ABL1 | 8.44 | Kd | 3.6 | nM | CHEMBL_ACT_12617325 |
| DDR1 | 8.43 | IC50 | 3.7 | nM | CHEMBL_ACT_3471375 |
| CA2 | 8.39 | Ki | 4.1 | nM | CHEMBL_ACT_2692390 |
| ABL1 | 8.31 | Kd | 4.9 | nM | CHEMBL_ACT_18916459 |
| ABL1 | 8.31 | Kd | 4.9 | nM | CHEMBL_ACT_7594667 |
| DDR2 | 8.28 | IC50 | 5.2 | nM | CHEMBL_ACT_3471376 |
| ABL1 | 8.26 | IC50 | 5.56 | nM | CHEMBL_ACT_20609025 |
| DDR2 | 8.22 | Kd | 6 | nM | CHEMBL_ACT_14666022 |
| DDR2 | 8.21 | Kd | 6.2 | nM | CHEMBL_ACT_12617323 |
| ABL1 | 8.15 | IC50 | 7 | nM | CHEMBL_ACT_26325698 |
| ABL1 | 8.05 | IC50 | 9 | nM | CHEMBL_ACT_26325638 |
| ABL1 | 8.05 | IC50 | 9 | nM | CHEMBL_ACT_26325731 |
| P00520 | 8 | IC50 | 10 | nM | CHEMBL_ACT_26325963 |
| ABL1 | 8 | Kd | 10 | nM | CHEMBL_ACT_7594670 |
| ABL1 | 8 | Kd | 10 | nM | CHEMBL_ACT_7594675 |
| MAP3K20 | 7.96 | Kd | 11 | nM | CHEMBL_ACT_7596380 |
| ABL1 | 7.92 | IC50 | 12 | nM | CHEMBL_ACT_26325626 |
| ABL1 | 7.92 | Kd | 12 | nM | CHEMBL_ACT_7594665 |
| ABL1 | 7.9 | IC50 | 12.7 | nM | CHEMBL_ACT_19289513 |
| ABL1 | 7.89 | IC50 | 12.8 | nM | CHEMBL_ACT_12623337 |
| ABL1 | 7.89 | IC50 | 13 | nM | CHEMBL_ACT_26325701 |
| P00520 | 7.89 | IC50 | 13 | nM | CHEMBL_ACT_26325823 |
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
27 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 |
|---|---|---|---|
| neoplasm | 3 | MONDO:0005070 | EFO:0000616 |
| chronic myeloid leukemia | 3 | MONDO:0011996 | EFO:0000339 |
| leukemia | 3 | MONDO:0005059 | EFO:0000565 |
| soft tissue sarcoma | 3 | MONDO:0018078 | EFO:1001968 |
| myeloid leukemia | 3 | MONDO:0004643 | MONDO:0004643 |
| Alzheimer disease | 3 | MONDO:0004975 | MONDO:0004975 |
| gastrointestinal stromal tumor | 3 | MONDO:0011719 | MONDO:0011719 |
| acute lymphoblastic leukemia | 2 | MONDO:0004967 | EFO:0000220 |
| acute myeloid leukemia | 2 | MONDO:0018874 | EFO:0000222 |
| melanoma | 2 | MONDO:0005105 | EFO:0000756 |
| pulmonary arterial hypertension | 2 | MONDO:0015924 | EFO:0001361 |
| cutaneous melanoma | 2 | MONDO:0005012 | EFO:0000389 |
| metastatic melanoma | 2 | MONDO:0005191 | EFO:0002617 |
| cerebellar ataxia | 2 | MONDO:0000437 | MONDO:0000437 |
| graft versus host disease | 2 | MONDO:0013730 | MONDO:0013730 |
| Parkinson disease | 2 | MONDO:0005180 | MONDO:0005180 |
| acoustic neuroma | 2 | MONDO:0001569 | HP:0009588 |
| paraganglioma | 2 | MONDO:0000448 | EFO:1000453 |
| glioma | 2 | MONDO:0021042 | MONDO:0021637 |
| tenosynovial giant cell tumor, diffuse type | 2 | MONDO:0024686 | MONDO:0024686 |
| breast neoplasm | 1 | MONDO:0021100 | MONDO:0007254 |
| Huntington disease | 1 | MONDO:0007739 | MONDO:0007739 |
| chordoma | 1 | MONDO:0008978 | MONDO:0008978 |
| colonic neoplasm | 0 | MONDO:0005401 | MONDO:0021063 |
3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 161.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 60 |
| PHASE1 | 27 |
| PHASE3 | 26 |
| Not specified | 18 |
| PHASE4 | 17 |
| PHASE1/PHASE2 | 10 |
| EARLY_PHASE1 | 2 |
| PHASE2/PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04877522 | PHASE4 | RECRUITING | Asciminib Roll-over Study |
| NCT00756509 | PHASE4 | COMPLETED | Treatment of Patients With Metastatic or Unresectable Gastrointestinal Stromal Tumors in First Line With Nilotinib |
| NCT00786812 | PHASE4 | COMPLETED | Study of Treatment With Nilotinib in Adult Patients With Imatinib - Resistant or - Intolerant Chronic Myeloid Leukemia in Blast Crisis, Accelerated Phase or Chronic Phase |
| NCT00980018 | PHASE4 | COMPLETED | An Exploratory Trial to Assess the Improvement of Adverse Events in Chronic Myelogenous Leukemia Patients Treated With Imatinib When Switched to Nilotinib Treatment |
| NCT01043874 | PHASE4 | COMPLETED | Study to Evaluate Nilotinib in Chronic Myelogenous Leukemia (CML) Patients With SubOptimal Response |
| NCT01061177 | PHASE4 | COMPLETED | Nilotinib in Newly Diagnosed Adult Philadelphia Chromosome & /or BCR-ABL Positive Chronic Myeloid Leukaemia in Chronic Phase |
| NCT01131325 | PHASE4 | TERMINATED | Study of Nilotinib in Ph+ CML-CP Patients With Low Imatinib Trough Plasma Concentrations |
| NCT01206088 | PHASE4 | COMPLETED | Tasigna in Glivec-resistant or Intolerant Patients in CML |
| NCT01227577 | PHASE4 | COMPLETED | CMR Rate of Newly Diagnosed CML-CP Patients Treated With Nilotinib |
| NCT01368523 | PHASE4 | COMPLETED | Study of Oral AMN107 (Nilotinib) in Adult Patients With Imatinib - Resistant or - Intolerant Chronic Myeloid Leukemia in Blast Crisis, Accelerated Phase or Chronic Phase Previously Enrolled to CAMN107A2109 Trial |
| NCT01605981 | PHASE4 | WITHDRAWN | Trial Evaluating Nilotinib as Treatment for Newly Diagnosed CML Patients in Accelerated Phase. |
| NCT01735955 | PHASE4 | COMPLETED | Study to Allow Access to Nilotinib for Patients Who Are on Nilotinib Treatment in a Novartis-sponsored Study |
| NCT02086487 | PHASE4 | TERMINATED | Efficacy and Safety Assessment of NIlotinib in CML Patients With Suboptimal Response on Imatinib Therapy |
| NCT02389920 | PHASE4 | UNKNOWN | Multicenter, PhaseⅣ, Open Label Trial of Nilotinib in Adult Patients Diagnosed Philadelphia Chromosome Positive(Ph+) Chronic Myeloid Leukemia in CP/AP Intolerant to Dasatinib |
| NCT02546674 | PHASE4 | COMPLETED | Study Assessing Deep Molecular Response in Adult Patients With CML in Chronic Phase Treated With Nilotinib Firstline. |
| NCT02602314 | PHASE4 | UNKNOWN | Sustained Treatment-free Remission in BCR-ABL+ Chronic Myeloid Leukemia |
| NCT03332511 | PHASE4 | COMPLETED | Efficacy and Safety of Nilotinib in CML-CP |
| NCT04971226 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study of Oral Asciminib Versus Other TKIs in Adult Patients With Newly Diagnosed Ph+ CML-CP |
| NCT05456191 | PHASE3 | ACTIVE_NOT_RECRUITING | A Study to Investigate Tolerability and Efficacy of Asciminib (Oral) Versus Nilotinib (Oral) in Adult Participants (≥18 Years of Age) With Newly Diagnosed Philadelphia Chromosome Positive Chronic Myelogenous Leukemia in Chronic Phase (Ph+ CML-CP) |
| NCT00264160 | PHASE2/PHASE3 | COMPLETED | Efficacy and Safety of Oral AMN107 in Adults With Chronic Myelogenous Leukemia Resistant and/or Intolerant to Imatinib Mesylate Therapy |
| NCT00471328 | PHASE3 | COMPLETED | Efficacy and Safety of Nilotinib (AMN107) Compared With Current Treatment Options in Patients With GIST Who Have Failed Both Imatinib and Sunitinib |
| NCT00471497 | PHASE3 | 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) |
| NCT00519090 | PHASE3 | TERMINATED | Nilotinib vs Imatinib in Adult Patients With Philadelphia (Ph+) Chronic Myelogenous Leukemia in Chronic Phase (CML-CP) |
| NCT00751036 | PHASE3 | TERMINATED | Nilotinib 800 Mg And Imatinib 800 Mg For The Treatment Of Patients With Gastrointestinal Stromal Tumors (Gist) Refractory To Imatinib 400 Mg |
| NCT00760877 | PHASE3 | 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 | PHASE3 | COMPLETED | A Study of Nilotinib Versus Imatinib in GIST Patients |
| NCT00802841 | PHASE3 | COMPLETED | Randomized Phase Lll Study of Imatinib Dose Optimization vs Nilotinib in CML Patients With Suboptimal Response to Imatinib |
| NCT01126892 | PHASE3 | COMPLETED | A Study of Nilotinib in Adult Patients With Imatinib Resistant or - Intolerant Chronic Myeloid Leukemia in Blast Crisis, Accelerated Phase or Chronic Phase |
| NCT01254188 | PHASE3 | COMPLETED | Safety and Efficacy of Nilotinib in Newly Diagnosed Chronic Myeloid Leukemia Patients |
| NCT01275196 | PHASE3 | COMPLETED | Safety and Efficacy of Nilotinib vs. Imatinib in the Treatment of Newly Diagnosed Chinese Ph+ CML-CP Patients |
| NCT01289028 | PHASE3 | COMPLETED | Efficacy of Nilotinib in Adult Patients With Gastrointestinal Stromal Tumors Resistant to Imatinib and Sunitinib. |
| NCT01400074 | PHASE3 | UNKNOWN | Efficacy of Nilotinib Versus Imatinib in Ph+ CML in Early CP Who Have a Suboptimal Molecular Response to Imatinib |
| NCT01535391 | PHASE3 | COMPLETED | Nilotinib in PH+, BCR-, ABL+ CML Patients |
| NCT01657604 | PHASE3 | COMPLETED | TKI and Interferon Alpha Evaluation Initiated by the German Chronic Myeloid Leukemia Study Group - the TIGER Study |
| NCT01743989 | PHASE3 | COMPLETED | A Randomized Phase III Study to Assess the Effect of a Longer Duration of Consolidation Treatment With Nilotinib on TFR in CP CML. |
| NCT01819389 | PHASE3 | COMPLETED | Low-dose Nilotinib and Imatinib Combination in Chronic Myeloid Leukemia Patients, With Failure, Suboptimal Response or Treatment Intolerance |
| NCT02108951 | PHASE3 | TERMINATED | Study to Assess Efficacy and Safety of Nilotinib 300mg Twice Daily in Patients With Philadelphia Positive Chronic Myeloid Leukaemia (CML) in Chronic Phase Who Are Intolerant to Prior Tyrosine Kinase Inhibitors. |
| NCT02115386 | PHASE3 | TERMINATED | Trial to Evaluate the Improvement of Chronic Low-grade AEs in Patients With Ph+ CML With Optimal Response to Imatinib When Switched to Nilotinib |
| NCT02174445 | PHASE3 | TERMINATED | An Open-label, Randomised Multicenter Phase 3b Study to Determine the Confirmed Rate of Molecular Response ≥ 4 Log (MR4) at Two Years |
| NCT02272777 | PHASE3 | COMPLETED | A Study of Imatinib and Nilotinib in Patients With Chronic Myelogenous Leukemia in Chronic Phase |
Clinical evidence (CIViC)
Variant × indication × effect (55 predictive associations from 61 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| BCR::ABL1 Fusion | B-lymphoblastic Leukemia/lymphoma | Sensitivity/Response | Nilotinib | CIViC A | EID11288 |
| BCR::ABL1 Fusion | Chronic Myeloid Leukemia | Sensitivity/Response | Nilotinib + Dasatinib | CIViC A | EID261 |
| FLT3 Mutation | Acute Myeloid Leukemia | Sensitivity/Response | Nilotinib | CIViC B | EID5575 +1 |
| ETV6::ABL1 Fusion | Myeloid Neoplasm | Sensitivity/Response | Imatinib + Dasatinib + Nilotinib | CIViC B | EID11326 |
| KIT Mutation | Melanoma | Sensitivity/Response | Nilotinib | CIViC B | EID7145 |
| ABL1 TKD Mutation | Chronic Myeloid Leukemia | Resistance | Nilotinib | CIViC B | EID6342 |
| KIT Amplification | Melanoma | Resistance | Nilotinib | CIViC B | EID5907 |
| BCR::ABL1 Fusion AND ABL1 M244V | Chronic Myeloid Leukemia | Sensitivity/Response | Nilotinib | CIViC C | EID2639 |
| BCR::ABL1 Fusion AND ABL1 Y253H | Chronic Myeloid Leukemia | Resistance | Imatinib Mesylate + Nilotinib | CIViC C | EID6200 +2 |
| BCR::ABL1 Fusion AND ABL1 E255V | Chronic Myeloid Leukemia | Resistance | Imatinib Mesylate + Nilotinib | CIViC C | EID6971 +1 |
| BCR::ABL1 Fusion AND ABL1 E255K | Chronic Myeloid Leukemia | Resistance | Imatinib Mesylate + Nilotinib | CIViC C | EID6232 |
| BCR::ABL1 Fusion AND ABL1 F359C | Chronic Myeloid Leukemia | Resistance | Nilotinib + Imatinib Mesylate | CIViC C | EID6233 |
| BCR::ABL1 Fusion AND ABL1 F359V | Chronic Myeloid Leukemia | Resistance | Nilotinib + Imatinib Mesylate | CIViC C | EID6970 |
| ATF7IP::PDGFRB Fusion | Childhood B-cell Acute Lymphoblastic Leukemia | Sensitivity/Response | Nilotinib + Imatinib + Dasatinib + Ponatinib + Bafetinib + Rebastinib | CIViC D | EID7196 |
| BCR::ABL1 Fusion | Chronic Myeloid Leukemia | Sensitivity/Response | Bafetinib + Nilotinib + Dasatinib | CIViC D | EID7838 |
| BCR::ABL1 Fusion AND ABL1 D276G | Chronic Myeloid Leukemia | Sensitivity/Response | Nilotinib | CIViC D | EID2666 |
| BCR::ABL1 Fusion AND ABL1 F486S | Chronic Myeloid Leukemia | Sensitivity/Response | Nilotinib | CIViC D | EID2829 |
| BCR::ABL1 Fusion AND ABL1 G398R | Chronic Myeloid Leukemia | Sensitivity/Response | Nilotinib | CIViC D | EID2864 |
| BCR::ABL1 Fusion AND ABL1 M351T | Chronic Myeloid Leukemia | Sensitivity/Response | Nilotinib | CIViC D | EID2685 |
| BCR::ABL1 Fusion AND ABL1 V299L | Chronic Myeloid Leukemia | Sensitivity/Response | Nilotinib | CIViC D | EID2862 |
| KIT L576P | Lung Non-small Cell Carcinoma | Sensitivity/Response | Imatinib + Dasatinib + Nilotinib | CIViC D | EID303 |
| KIT Mutation | Acute Promyelocytic Leukemia | Sensitivity/Response | Nilotinib | CIViC D | EID5573 |
| KIT V559D | Gastrointestinal Stromal Tumor | Sensitivity/Response | Sorafenib + Nilotinib + Dasatinib + Imatinib | CIViC D | EID3033 |
| NUP214::ABL1 Fusion | B-lymphoblastic Leukemia/lymphoma | Sensitivity/Response | Ponatinib + Dasatinib + Imatinib + Nilotinib | CIViC D | EID9150 |
| BCR::ABL1 Fusion AND ABL1 F359C | Chronic Myeloid Leukemia | Resistance | Imatinib Mesylate + Nilotinib | CIViC D | EID2854 +1 |
| BCR::ABL1 Fusion AND ABL1 G250E | Chronic Myeloid Leukemia | Resistance | Nilotinib | CIViC D | EID2648 +1 |
| BCR::ABL1 Fusion AND ABL1 E255K | Chronic Myeloid Leukemia | Resistance | Nilotinib | CIViC D | EID2662 |
| BCR::ABL1 Fusion AND ABL1 E255K | Chronic Myeloid Leukemia | Resistance | Dasatinib + Nilotinib + Imatinib Mesylate | CIViC D | EID6194 |
| BCR::ABL1 Fusion AND ABL1 E255V | Chronic Myeloid Leukemia | Resistance | Nilotinib | CIViC D | EID2850 |
| BCR::ABL1 Fusion AND ABL1 E292V | Chronic Myeloid Leukemia | Resistance | Nilotinib | CIViC D | EID2853 |
+25 more predictive associations (showing top 30 by level).
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline, but PharmGKB curates 4 clinical and 13 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 |
| IMATINIB | ChEMBL | Phase 4 (approved) | ABL1, DDR1, DDR2 |
| LENVATINIB | 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: neoplasm, chronic myeloid leukemia, leukemia, soft tissue sarcoma, myeloid leukemia, Alzheimer disease, gastrointestinal stromal tumor, B-cell acute lymphoblastic leukemia, acute myeloid leukemia by FAB classification, myeloid neoplasm, melanoma, acute promyelocytic leukemia
- Drugs: Afatinib, Cabozantinib, Crizotinib, Dasatinib, Entrectinib, Erlotinib, Fedratinib, Gefitinib, Ibrutinib, Lapatinib, Pazopanib, Ponatinib, Quizartinib, Regorafenib, Ruxolitinib, Sorafenib, Tirbanibulin, Tovorafenib, Vandetanib, Axitinib, Bosutinib, Imatinib, Lenvatinib, Nintedanib, Sunitinib, Tivozanib, Cediranib, Dovitinib, Lestaurtinib, Linifanib, Masitinib, Saracatinib, Tesevatinib, Binimetinib, dacomitinib, Fostamatinib, Idelalisib, Selumetinib, Trametinib, Dabrafenib, Midostaurin, Brivanib
- Biomarker genes: FLT3, KIT, LYN