Quizartinib
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Also known as AC-010220Ac-220AC010220AC220ASP-2689AC010220.2HCLAC 220AC220 (QUIZARTINIB)QUIZARTINIB DIHYDROCHLORIDEQUIZARTINIB (AC220)AC708SID137275856
Summary
Quizartinib (CHEMBL576982) is an approved small-molecule EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor (ATC L01EX11) targeting PDGFRA, PDGFRB, and KIT; indicated across 4 conditions including acute myeloid leukemia and neoplasm; with CIViC clinical evidence for 21 variant-indication associations (e.g. FLT3 D835 & I836 in acute myeloid leukemia).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EX11
- Targets: 6 (PDGFRA, PDGFRB, KIT…)
- Indications: 4 conditions
- Clinical trials: 42
- Precision-oncology evidence (CIViC): 21 variant–indication associations
- Chemistry: 560.7 Da · C29H32N6O4S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL576982 |
| Name | Quizartinib |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 24889392 |
| ChEBI | CHEBI:90217 |
| ATC | L01EX11 |
| Molecular formula | C29H32N6O4S |
| Molecular weight | 560.7 |
| InChIKey | CVWXJKQAOSCOAB-UHFFFAOYSA-N |
SMILES: CC(C)(C)C1=CC(=NO1)NC(=O)NC2=CC=C(C=C2)C3=CN4C5=C(C=C(C=C5)OCCN6CCOCC6)SC4=N3
IUPAC name: 1-(5-tert-butyl-1,2-oxazol-3-yl)-3-[4-[6-(2-morpholin-4-ylethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl]urea
ChEBI definition: A member of the class of phenylureas that is urea in which one of the amino groups has been substituted by a 5-tert-butyl-1,2-oxazol-3-yl group while the other has been substituted by a phenyl group substituted at the para- position by an imidazo[2,1-b][1,3]benzothiazol-2-yl group that, in turn, is substituted at position 7 by a 2-(morpholin-4-yl)ethoxy group.
Pharmacological roles (ChEBI): EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, antineoplastic agent, necroptosis inhibitor.
Also known as: AC-010220, Ac-220, AC-220, AC010220, AC220, ASP-2689, Quizartinib, QUIZARTINIB, AC010220.2HCL, AC 220, AC220 (QUIZARTINIB), QUIZARTINIB DIHYDROCHLORIDE
Parent form; salt/anhydrous children: CHEMBL2105709
Patent coverage: 1,995 distinct patent families (4,432 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 4,150 (94%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| PDGFRA | platelet derived growth factor receptor alpha | Inhibition | 7.96 | 6.2% | P16234 |
| PDGFRB | platelet derived growth factor receptor beta | Inhibition | 8.11 | 2.3% | P09619 |
| KIT | KIT proto-oncogene, receptor tyrosine kinase | Inhibition | 8.32 | 0.5% | P10721 |
| CSF1R | colony stimulating factor 1 receptor | Inhibition | 7.92 | 0% | P07333 |
| FLT3 | fms related receptor tyrosine kinase 3 | Inhibition | 8.38 | 0.9% | P36888 |
| RET | ret proto-oncogene | Inhibition | 8 | 0.4% | P07949 |
Broader ChEMBL bioactivity targets: 74 (assay-derived). Sample: Homeodomain-interacting protein kinase 4, Receptor-interacting serine/threonine-protein kinase 3, Macrophage colony-stimulating factor 1 receptor, Tyrosine-protein kinase ABL1, Vascular endothelial growth factor receptor 1, Platelet-derived growth factor receptor beta, Mast/stem cell growth factor receptor Kit, Vascular endothelial growth factor receptor 3, Receptor-type tyrosine-protein kinase FLT3, Platelet-derived growth factor receptor alpha.
Bioactivity
ChEMBL activities: 353 potent at pChembl ≥ 5 of 377 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| FLT3 | 9.7 | IC50 | 0.2 | nM | CHEMBL_ACT_25754091 |
| FLT3 | 9.63 | IC50 | 0.24 | nM | CHEMBL_ACT_28884431 |
| FLT3 | 9.63 | IC50 | 0.24 | nM | CHEMBL_ACT_28884899 |
| FLT3 | 9.4 | IC50 | 0.4 | nM | CHEMBL_ACT_25754088 |
| FLT3 | 9.25 | IC50 | 0.56 | nM | CHEMBL_ACT_29231733 |
| FLT3 | 9.24 | Kd | 0.57 | nM | CHEMBL_ACT_28884635 |
| FLT3 | 9.21 | IC50 | 0.62 | nM | CHEMBL_ACT_25754096 |
| CDK7 | 9.21 | IC50 | 0.62 | nM | CHEMBL_ACT_28884419 |
| CDK7 | 9.21 | IC50 | 0.62 | nM | CHEMBL_ACT_28884893 |
| CDK7 | 9.21 | IC50 | 0.62 | nM | CHEMBL_ACT_28884917 |
| FLT3 | 9.17 | IC50 | 0.67 | nM | CHEMBL_ACT_25754099 |
| FLT3 | 9.14 | IC50 | 0.73 | nM | CHEMBL_ACT_25754090 |
| FLT3 | 9.1 | IC50 | 0.8 | nM | CHEMBL_ACT_3450432 |
| FLT3 | 9.07 | EC50 | 0.86 | nM | CHEMBL_ACT_25754102 |
| FLT3 | 9.05 | IC50 | 0.9 | nM | CHEMBL_ACT_24909848 |
| FLT3 | 9.05 | IC50 | 0.89 | nM | CHEMBL_ACT_25754089 |
| FLT3 | 8.96 | IC50 | 1.1 | nM | CHEMBL_ACT_18893333 |
| FLT3 | 8.96 | IC50 | 1.1 | nM | CHEMBL_ACT_22960942 |
| FLT3 | 8.96 | IC50 | 1.1 | nM | CHEMBL_ACT_24797158 |
| FLT3 | 8.96 | IC50 | 1.1 | nM | CHEMBL_ACT_24992734 |
| FLT3 | 8.96 | IC50 | 1.1 | nM | CHEMBL_ACT_26122112 |
| FLT3 | 8.96 | IC50 | 1.1 | nM | CHEMBL_ACT_29231737 |
| FLT3 | 8.96 | IC50 | 1.1 | nM | CHEMBL_ACT_3444908 |
| FLT3 | 8.89 | Kd | 1.3 | nM | CHEMBL_ACT_19250427 |
| FLT3 | 8.89 | Kd | 1.3 | nM | CHEMBL_ACT_19469397 |
| FLT3 | 8.89 | Kd | 1.3 | nM | CHEMBL_ACT_20679564 |
| FLT3 | 8.89 | Kd | 1.3 | nM | CHEMBL_ACT_7585814 |
| FLT3 | 8.85 | Kd | 1.4 | nM | CHEMBL_ACT_28884530 |
| FLT3 | 8.82 | Kd | 1.5 | nM | CHEMBL_ACT_28884650 |
| FLT3 | 8.8 | Kd | 1.6 | nM | CHEMBL_ACT_25755744 |
Target pathways
Aggregated over 6 target gene(s): PDGFRA, PDGFRB, KIT, CSF1R, FLT3, RET.
Top Reactome pathways
78 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| RAF/MAP kinase cascade | 5 | FLT3, KIT, PDGFRA, PDGFRB, RET |
| PIP3 activates AKT signaling | 4 | FLT3, KIT, PDGFRA, PDGFRB |
| Constitutive Signaling by Aberrant PI3K in Cancer | 4 | FLT3, KIT, PDGFRA, PDGFRB |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 4 | FLT3, KIT, PDGFRA, PDGFRB |
| Downstream signal transduction | 2 | PDGFRA, PDGFRB |
| Signaling by PDGF | 2 | PDGFRA, PDGFRB |
| PI3K Cascade | 1 | FLT3 |
| Developmental Biology | 1 | KIT |
| Signaling by SCF-KIT | 1 | KIT |
| Regulation of KIT signaling | 1 | KIT |
| Signal Transduction | 1 | KIT |
| Disease | 1 | KIT |
| Negative regulation of the PI3K/AKT network | 1 | KIT |
| Generic Transcription Pathway | 1 | KIT |
| PI3K/AKT Signaling in Cancer | 1 | KIT |
| Other interleukin signaling | 1 | CSF1R |
| Diseases of signal transduction by growth factor receptors and second messengers | 1 | KIT |
| MAPK family signaling cascades | 1 | KIT |
| MAPK1/MAPK3 signaling | 1 | KIT |
| RNA Polymerase II Transcription | 1 | KIT |
| Gene expression (Transcription) | 1 | KIT |
| RET signaling | 1 | RET |
| Transcriptional Regulation by VENTX | 1 | CSF1R |
| Transcriptional regulation by the AP-2 (TFAP2) family of transcription factors | 1 | KIT |
| TFAP2 (AP-2) family regulates transcription of growth factors and their receptors | 1 | KIT |
| Intracellular signaling by second messengers | 1 | KIT |
| Signaling by Receptor Tyrosine Kinases | 1 | KIT |
| FLT3 Signaling | 1 | FLT3 |
| STAT5 Activation | 1 | FLT3 |
| Dasatinib-resistant KIT mutants | 1 | KIT |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| cell surface receptor protein tyrosine kinase signaling pathway | 6 |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 6 |
| protein phosphorylation | 6 |
| positive regulation of cell population proliferation | 5 |
| cell migration | 5 |
| positive regulation of cell migration | 5 |
| protein autophosphorylation | 5 |
| peptidyl-tyrosine phosphorylation | 4 |
| signal transduction | 4 |
| regulation of actin cytoskeleton organization | 3 |
| cell chemotaxis | 3 |
| positive regulation of ERK1 and ERK2 cascade | 3 |
| chemotaxis | 3 |
| cytokine-mediated signaling pathway | 3 |
| hemopoiesis | 3 |
Indications & clinical
Indications
4 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 myeloid leukemia | 3 | MONDO:0018874 | EFO:0000222 |
| neoplasm | 3 | MONDO:0005070 | EFO:0000616 |
| liver disorder | 1 | MONDO:0005154 | EFO:0001421 |
| myelodysplastic syndrome | 1 | MONDO:0018881 | EFO:0000198 |
Clinical trials
Total trials: 42.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE1 | 17 |
| PHASE1/PHASE2 | 10 |
| PHASE2 | 7 |
| PHASE3 | 5 |
| Not specified | 2 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT06578247 | PHASE3 | RECRUITING | Quizartinib or Placebo Plus Chemotherapy in Newly Diagnosed Patients With FLT3-ITD Negative AML |
| NCT07478991 | PHASE3 | NOT_YET_RECRUITING | Azacytidine, Venetoclax Plus Minus Quizartinib for First Line Older/Unfit AML Patients (VENP-A-QUI) |
| NCT02039726 | PHASE3 | COMPLETED | (QuANTUM-R): An Open-label Study of Quizartinib Monotherapy vs. Salvage Chemotherapy in Acute Myeloid Leukemia (AML) Subjects Who Are FLT3-ITD Positive |
| NCT02668653 | PHASE3 | COMPLETED | Quizartinib With Standard of Care Chemotherapy and as Continuation Therapy in Patients With Newly Diagnosed FLT3-ITD (+) Acute Myeloid Leukemia (AML) |
| NCT04676243 | PHASE3 | WITHDRAWN | Daunorubicin or Idarubicin With Cytarabine Plus Quizartinib vs Physician’s Choice in Newly Diagnosed FLT3-ITD+ AML |
| NCT03661307 | PHASE1/PHASE2 | RECRUITING | Quizartinib, Decitabine, and Venetoclax in Treating Participants With Untreated or Relapsed Acute Myeloid Leukemia or High Risk Myelodysplastic Syndrome |
| NCT03793478 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Safety and Efficacy of Quizartinib in Children and Young Adults With Acute Myeloid Leukemia (AML), a Cancer of the Blood |
| NCT04047641 | PHASE1/PHASE2 | RECRUITING | Cladribine, Idarubicin, Cytarabine, and Quizartinib in Treating Patients With Newly Diagnosed, Relapsed, or Refractory Acute Myeloid Leukemia or High-Risk Myelodysplastic Syndrome |
| NCT04128748 | PHASE1/PHASE2 | RECRUITING | Liposomal Cytarabine and Daunorubicin (CPX-351) and Quizartinib for the Treatment of Acute Myeloid Leukemia and High Risk Myelodysplastic Syndrome |
| NCT04493138 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Azacitidine and Quizartinib for the Treatment of Myelodysplastic Syndrome or Myelodysplastic/Myeloproliferative Neoplasm With FLT3 or CBL Mutations |
| NCT06262438 | PHASE2 | RECRUITING | CHIP-AML22/Quizartinib: Quizartinib + Chemotherapy in Newly Diagnosed Pediatric FLT3-ITD+ and NPM1wt AML Patients |
| NCT00989261 | PHASE2 | COMPLETED | Efficacy Study for AC220 to Treat Acute Myeloid Leukemia (AML) |
| NCT01236144 | PHASE1/PHASE2 | COMPLETED | A Trial to Establish the Feasibility of Combining Either the Tyrosine Kinase Inhibitor AC220,CXCR4 Inhibitor Plerixafor or HSP90 Inhibitor Ganetespib With Chemotherapy in Older Patients With Acute Myeloid Leukaemia and High Risk Myelodysplastic Syndrome. |
| NCT01565668 | PHASE2 | COMPLETED | Open Label Study to Evaluate Safety and Efficacy of 2 Doses of Quizartinib in Patients With Relapsed or Refractory Acute Myeloid Leukemia |
| NCT01892371 | PHASE1/PHASE2 | COMPLETED | Quizartinib With Azacitidine or Cytarabine in Treating Patients With Relapsed or Refractory Acute Myeloid Leukemia or Myelodysplastic Syndrome |
| NCT02984995 | PHASE2 | COMPLETED | Phase 2 Study of Quizartinib in Participants With Acute Myeloid Leukemia (AML) FLT3 Internal Tandem Duplication (FLT3/ITD) Mutation |
| NCT03135054 | PHASE2 | UNKNOWN | Combination of Quizartinib and Omacetaxine Mepesuccinate for AML Carrying FLT3-ITD |
| NCT03735875 | PHASE1/PHASE2 | TERMINATED | Venetoclax and Quizartinib in Treating Patients With FLT3-mutated Recurrent or Refractory Acute Myeloid Leukemia |
| NCT04107727 | PHASE2 | COMPLETED | Trial to Compare Efficacy and Safety of Chemotherapy/Quizartinib vs Chemotherapy/Placebo in Adults FMS-like Tyrosine Kinase 3 (FLT3) Wild-type Acute Myeloid Leukemia (AML) |
| NCT04112589 | PHASE1/PHASE2 | UNKNOWN | A Clinical Trial to Assess the Efficacy and Safety of the Combination of a Drug Call Quizartinib With Chemotherapy (FLAG-IDA) in Patients With Acute Myeloid Leukemia That Has Not Responded to the First Treatment or That Has Returned After the First Treatment |
| NCT04209725 | PHASE2 | TERMINATED | A Study of CPX-351 (Vyxeos™) With Quizartinib for the Treatment of FLT3-ITD Mutation-Positive Acute Myeloid Leukemia |
| NCT04687761 | PHASE1/PHASE2 | COMPLETED | Clinical Trial to Assess the Safety and Tolerability of the Combination of Low-dose Cytarabine or Azacitidine Plus Venetoclax and Quizartinib in Newly Diagnosed AML Patients Aged Equal or More Than 60 Years Old |
| NCT05735184 | PHASE1 | RECRUITING | A Study to Investigate the Safety and Tolerability of Ziftomenib in Combination With Venetoclax/Azacitidine, Venetoclax, 7+3, or 7+3+Quizartinib in Patients With AML |
| NCT06740799 | PHASE1 | RECRUITING | Assessment of Quizartinib Pharmacokinetic in Subjects With Severe Hepatic Impairment |
| NCT06769490 | PHASE1 | RECRUITING | Dose Escalation and Expansion of Ziftomenib in Combination With Quizartinib in Acute Myeloid Leukemia |
| NCT00462761 | PHASE1 | COMPLETED | A Phase I Study of AC220 in Patients With Relapsed/Refractory Acute Myeloid Leukemia Regardless of FLT3 Status |
| NCT01049893 | PHASE1 | COMPLETED | Dose Finding, Safety and Tolerability Study for AC220 to Treat Advanced Solid Tumors |
| NCT01390337 | PHASE1 | COMPLETED | A Study to Assess AC220 Given in Combination With Induction and Consolidation Therapy in Newly Diagnosed Acute Myeloid Leukemia (AML) |
| NCT01411267 | PHASE1 | COMPLETED | AC220 for Children With Relapsed/Refractory ALL or AML |
| NCT01468467 | PHASE1 | COMPLETED | A Study of AC220 Given After Transplant in Subjects With Acute Myeloid Leukemia (AML) |
| NCT02675478 | PHASE1 | COMPLETED | Phase 1 Study of Quizartinib |
| NCT02834390 | PHASE1 | COMPLETED | Study of Quizartinib in Japanese Patients With Newly Diagnosed Acute Myeloid Leukemia (AML) |
| NCT03552029 | PHASE1 | TERMINATED | Milademetan Plus Quizartinib Combination Study in FLT3-ITD Mutant Acute Myeloid Leukemia (AML) |
| NCT03723681 | PHASE1 | COMPLETED | Study of Quizartinib in Combination With Standard Therapies in Chinese Participants With Newly Diagnosed Acute Myeloid Leukemia (AML) |
| NCT04459598 | PHASE1 | COMPLETED | A Study of the Effect of a Moderate CYP3A Inducer Efavirenz on Quizartinib Pharmacokinetics in Healthy Participants |
| NCT04473664 | PHASE1 | COMPLETED | A Study of Quizartinib Pharmacokinetics in Participants With Moderate Hepatic Impairment |
| NCT04796831 | PHASE1 | COMPLETED | A Study to Determine the Absolute Oral Bioavailability of Quizartinib Using a Radiolabeled Microtracer in Healthy Subjects |
| NCT06740825 | PHASE1 | COMPLETED | Study to Assess the Effect of a CYP3A Weak Inducer Rufinamide on Quizartinib Pharmacokinetics in Healthy Subjects |
| NCT06772246 | PHASE1 | COMPLETED | A Study to Evaluate QTc Prolongation With Quizartinib in Healthy Subjects Under Rapid Acceleration of Heart Rate |
| NCT04459585 | EARLY_PHASE1 | COMPLETED | A Study of the Effect of Quizartinib on the Pharmacokinetics of the P-gp Substrate Dabigatran Etexilate in Healthy Participants |
Clinical evidence (CIViC)
Variant × indication × effect (21 predictive associations from 22 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| FLT3 D835 & I836 | Acute Myeloid Leukemia | Sensitivity/Response | Lestaurtinib + Quizartinib + Sorafenib + FLT3/ABL/Aurora Kinase Inhibitor KW-2449 | CIViC B | EID8925 |
| FLT3 F691L | Acute Myeloid Leukemia | Resistance | Quizartinib | CIViC B | EID9718 +1 |
| FLT3 D835 | Acute Myeloid Leukemia | Resistance | Quizartinib + Sorafenib | CIViC B | EID1038 |
| FLT3 N676K | Core Binding Factor Acute Myeloid Leukemia | Quizartinib + Midostaurin | CIViC B | EID8263 | |
| FLT3 D593del | Cancer | Sensitivity/Response | Sorafenib + Sunitinib + Quizartinib + Linifanib | CIViC D | EID11094 |
| FLT3 D835V | Acute Myeloid Leukemia | Sensitivity/Response | Quizartinib | CIViC D | EID3012 |
| FLT3 D835Y | Cancer | Sensitivity/Response | Quizartinib + KW2449 + R406 + Ponatinib + AG1295 + Sorafenib + Sunitinib + AGS324 + Linifanib | CIViC D | EID11086 |
| FLT3 E573del | Acute Myeloid Leukemia | Sensitivity/Response | Lestaurtinib + Midostaurin + Quizartinib + Ponatinib + Sorafenib + Crenolanib | CIViC D | EID9307 |
| FLT3 ITD | Cancer | Sensitivity/Response | FLT3 Tyrosine Kinase Inhibitor TTT-3002 + R406 + Ponatinib + Crenolanib + KW2449 + Sorafenib + Sunitinib + Quizartinib + Linifanib + AGS324 + AG1295 + Lestaurtinib + Midostaurin | CIViC D | EID11084 |
| FLT3 ITD & D839G | Acute Myeloid Leukemia | Sensitivity/Response | Quizartinib | CIViC D | EID8896 |
| FLT3 N841I | Acute Myeloid Leukemia | Sensitivity/Response | Quizartinib | CIViC D | EID12511 |
| FLT3 Overexpression AND FLT3LG Expression | Cancer | Sensitivity/Response | Quizartinib + Linifanib + Lestaurtinib + Midostaurin + Ponatinib + FLT3 Tyrosine Kinase Inhibitor TTT-3002 + Sunitinib | CIViC D | EID11088 |
| FLT3 S574del | Acute Myeloid Leukemia | Sensitivity/Response | Lestaurtinib + Crenolanib + Sorafenib + Ponatinib + Quizartinib + Midostaurin | CIViC D | EID9308 |
| FLT3 Y572C | Acute Myeloid Leukemia | Sensitivity/Response | Quizartinib | CIViC D | EID12789 |
| FLT3 Y572del | Acute Myeloid Leukemia | Sensitivity/Response | Quizartinib | CIViC D | EID12860 |
| FLT3 Y572del | Acute Myeloid Leukemia | Sensitivity/Response | Midostaurin + Quizartinib + Lestaurtinib + Sorafenib + Crenolanib + Ponatinib | CIViC D | EID9306 |
| FGF2 EXPRESSION | Acute Myeloid Leukemia | Resistance | Quizartinib | CIViC D | EID1711 |
| FLT3 D835 | Acute Myeloid Leukemia | Resistance | Ponatinib + Quizartinib | CIViC D | EID1036 |
| FLT3 ITD AND ( FLT3 Y842C OR FLT3 Y842H ) | Cancer | Resistance | Quizartinib | CIViC D | EID12628 |
| FLT3 ITD&F691(I/L) | Acute Myeloid Leukemia | Resistance | Quizartinib | CIViC D | EID9779 |
| FLT3 Y842C | Acute Myeloid Leukemia | Resistance | Quizartinib | CIViC D | EID8654 |
Pharmacology
Pharmacogenomics
No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
188 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| Afatinib | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| Crizotinib | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| AXITINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| DASATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| NILOTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| PONATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| SORAFENIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| SUNITINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| VANDETANIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| CEDIRANIB | ChEMBL | Phase 3 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| DOVITINIB | ChEMBL | Phase 3 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| LESTAURTINIB | ChEMBL | Phase 3 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| LINIFANIB | ChEMBL | Phase 3 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| MOTESANIB | ChEMBL | Phase 3 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| SEMAXANIB | ChEMBL | Phase 3 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| CENISERTIB | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| DORAMAPIMOD | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| FORETINIB | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| ILORASERTIB | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| R-406 | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| RAF-265 | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| SU-014813 | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| TOZASERTIB | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| Idelalisib | PubChem | Approved | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| Selumetinib | PubChem | Approved | CSF1R, FLT3, KIT, PDGFRA, PDGFRB, RET |
| Gefitinib | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, RET |
| IMATINIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | FLT3, KIT, PDGFRA, PDGFRB, RET |
| PEXIDARTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB |
| TIVOZANIB | ChEMBL | Phase 4 (approved) | FLT3, KIT, PDGFRA, PDGFRB, RET |
| BARASERTIB | ChEMBL | Phase 3 | FLT3, KIT, PDGFRA, PDGFRB, RET |
| BRIVANIB | ChEMBL | Phase 3 | CSF1R, KIT, PDGFRA, PDGFRB, RET |
| CANERTINIB | ChEMBL | Phase 3 | FLT3, KIT, PDGFRA, PDGFRB, RET |
| SARACATINIB | ChEMBL | Phase 3 | FLT3, KIT, PDGFRA, PDGFRB, RET |
| VATALANIB | ChEMBL | Phase 3 | CSF1R, KIT, PDGFRA, PDGFRB, RET |
| VIMSELTINIB | ChEMBL | Phase 3 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB |
| CEP-32496 | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRB, RET |
| ENMD-2076 | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, RET |
| REBASTINIB | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, RET |
| SOTULETINIB | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB |
| TANDUTINIB | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, RET |
| CERITINIB | ChEMBL | Phase 4 (approved) | FLT3, KIT, PDGFRA, RET |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, RET |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | FLT3, KIT, PDGFRA, RET |
| LENVATINIB | ChEMBL | Phase 4 (approved) | KIT, PDGFRA, PDGFRB, RET |
| ALVOCIDIB | ChEMBL | Phase 3 | CSF1R, FLT3, KIT, PDGFRA |
| CRENOLANIB | ChEMBL | Phase 3 | FLT3, PDGFRA, PDGFRB, RET |
| MASITINIB | ChEMBL | Phase 3 | CSF1R, KIT, PDGFRA, PDGFRB |
| BEMCENTINIB | ChEMBL | Phase 2 | FLT3, KIT, PDGFRA, RET |
| BMS-777607 | ChEMBL | Phase 2 | FLT3, KIT, PDGFRA, RET |
| CEP-11981 | ChEMBL | Phase 2 | CSF1R, FLT3, PDGFRA, RET |
| MILCICLIB | ChEMBL | Phase 2 | FLT3, KIT, PDGFRB, RET |
Related Atlas pages
- Genes: PDGFRA, PDGFRB, KIT, CSF1R, FLT3, RET
- Diseases: acute myeloid leukemia, neoplasm, acute myeloid leukemia by FAB classification, core binding factor acute myeloid leukemia, cancer
- Drugs: Afatinib, Crizotinib, Pazopanib, Regorafenib, Axitinib, Bosutinib, Dasatinib, Fedratinib, Midostaurin, Nilotinib, Nintedanib, Ponatinib, Sorafenib, Sunitinib, Vandetanib, Cediranib, Dovitinib, Lestaurtinib, Linifanib, Motesanib, Semaxanib, Idelalisib, Selumetinib, Gefitinib, Imatinib, Erlotinib, Pexidartinib, Tivozanib, Barasertib, Brivanib, Canertinib, Saracatinib, Vatalanib, Vimseltinib, Brigatinib, Ceritinib, Entrectinib, Infigratinib, Lenvatinib, Alvocidib, Crenolanib, Masitinib
- Biomarker genes: FGF13