Sitravatinib
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Also known as MG-516MG-91516MGCD-516MGCD516
Summary
Sitravatinib (CHEMBL3989926) is a phase-3 clinical-stage small molecule (ATC L01EX26) targeting PDGFRA, KIT, and FLT3; indicated across 18 conditions including neoplasm and non-small cell lung carcinoma.
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- ATC class: L01EX26
- Targets: 12 (PDGFRA, KIT, FLT3…)
- Indications: 18 conditions
- Clinical trials: 34
- Chemistry: 629.7 Da · C33H29F2N5O4S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL3989926 |
| Name | Sitravatinib |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 25212148 |
| ATC | L01EX26 |
| Molecular formula | C33H29F2N5O4S |
| Molecular weight | 629.7 |
| InChIKey | WLAVZAAODLTUSW-UHFFFAOYSA-N |
SMILES: COCCNCC1=CN=C(C=C1)C2=CC3=NC=CC(=C3S2)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F
IUPAC name: 1-N’-[3-fluoro-4-[2-[5-[(2-methoxyethylamino)methyl]-2-pyridinyl]thieno[3,2-b]pyridin-7-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Also known as: MG-516, MG-91516, MGCD-516, MGCD516, Sitravatinib, SITRAVATINIB
Parent form; salt/anhydrous children: CHEMBL4298164
Patent coverage: 396 distinct patent families (982 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 906 (92%) 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 | 7.52 | 6.2% | P16234 |
| KIT | KIT proto-oncogene, receptor tyrosine kinase | Inhibition | 8.22 | 0.5% | P10721 |
| FLT3 | fms related receptor tyrosine kinase 3 | Inhibition | 8.1 | 0.9% | P36888 |
| FLT1 | fms related receptor tyrosine kinase 1 | Inhibition | 8.22 | 0.1% | P17948 |
| KDR | kinase insert domain receptor | Inhibition | 8.3 | 1.1% | P35968 |
| FLT4 | fms related receptor tyrosine kinase 4 | Inhibition | 8.7 | 0.2% | P35916 |
| MET | MET proto-oncogene, receptor tyrosine kinase | Inhibition | 7.7 | 2.4% | P08581 |
| NTRK1 | neurotrophic receptor tyrosine kinase 1 | Inhibition | 8.3 | 0.1% | P04629 |
| EPHA3 | EPH receptor A3 | Inhibition | 9 | 0.4% | P29320 |
| AXL | AXL receptor tyrosine kinase | Inhibition | 8.82 | 1.1% | P30530 |
| MERTK | MER proto-oncogene, tyrosine kinase | Inhibition | 8.7 | 0.6% | Q12866 |
| DDR2 | discoidin domain receptor tyrosine kinase 2 | Inhibition | 9.3 | 0% | Q16832 |
Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Mast/stem cell growth factor receptor Kit, Receptor-type tyrosine-protein kinase FLT3, Vascular endothelial growth factor receptor 2, High affinity nerve growth factor receptor, Hepatocyte growth factor receptor, Tyrosine-protein kinase receptor UFO, BDNF/NT-3 growth factors receptor.
Bioactivity
ChEMBL activities: 8 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| AXL | 8.82 | IC50 | 1.5 | nM | CHEMBL_ACT_18946682 |
| KDR | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_18772571 |
| KDR | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_18946681 |
| NTRK1 | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_18946684 |
| KIT | 8.22 | IC50 | 6 | nM | CHEMBL_ACT_18946679 |
| FLT3 | 8.1 | IC50 | 8 | nM | CHEMBL_ACT_18946680 |
| NTRK2 | 8.05 | IC50 | 9 | nM | CHEMBL_ACT_18946683 |
| MET | 7.7 | IC50 | 20 | nM | CHEMBL_ACT_18772566 |
Target pathways
Aggregated over 12 target gene(s): PDGFRA, KIT, FLT3, FLT1, KDR, FLT4, MET, NTRK1, EPHA3, AXL, MERTK, DDR2.
Top Reactome pathways
122 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| PIP3 activates AKT signaling | 4 | FLT3, KIT, MET, PDGFRA |
| Constitutive Signaling by Aberrant PI3K in Cancer | 4 | FLT3, KIT, MET, PDGFRA |
| RAF/MAP kinase cascade | 4 | FLT3, KIT, MET, PDGFRA |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 4 | FLT3, KIT, MET, PDGFRA |
| VEGF binds to VEGFR leading to receptor dimerization | 3 | FLT1, FLT4, KDR |
| Developmental Biology | 2 | KIT, MET |
| Signal Transduction | 2 | KIT, MET |
| Disease | 2 | KIT, MET |
| Neuropilin interactions with VEGF and VEGFR | 2 | FLT1, KDR |
| Negative regulation of the PI3K/AKT network | 2 | KIT, MET |
| Generic Transcription Pathway | 2 | KIT, MET |
| PI3K/AKT Signaling in Cancer | 2 | KIT, MET |
| VEGFA-VEGFR2 Pathway | 2 | AXL, KDR |
| Diseases of signal transduction by growth factor receptors and second messengers | 2 | KIT, MET |
| MAPK family signaling cascades | 2 | KIT, MET |
| MAPK1/MAPK3 signaling | 2 | KIT, MET |
| RNA Polymerase II Transcription | 2 | KIT, MET |
| Gene expression (Transcription) | 2 | KIT, MET |
| Intracellular signaling by second messengers | 2 | KIT, MET |
| Signaling by Receptor Tyrosine Kinases | 2 | KIT, MET |
| MITF-M-regulated melanocyte development | 2 | KIT, MET |
| High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells | 2 | FLT4, KDR |
| Dengue Virus Attachment and Entry | 2 | AXL, MERTK |
| Hemostasis | 1 | MERTK |
| PI3K Cascade | 1 | FLT3 |
| Signaling by SCF-KIT | 1 | KIT |
| Regulation of KIT signaling | 1 | KIT |
| PLC-gamma1 signalling | 1 | NTRK1 |
| Signalling to RAS | 1 | NTRK1 |
| Frs2-mediated activation | 1 | NTRK1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| cell surface receptor protein tyrosine kinase signaling pathway | 12 |
| protein phosphorylation | 12 |
| cell migration | 9 |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 9 |
| peptidyl-tyrosine phosphorylation | 8 |
| protein autophosphorylation | 8 |
| positive regulation of cell population proliferation | 7 |
| positive regulation of cell migration | 5 |
| positive regulation of ERK1 and ERK2 cascade | 5 |
| positive regulation of MAPK cascade | 5 |
| negative regulation of apoptotic process | 5 |
| signal transduction | 4 |
| spermatogenesis | 4 |
| vascular endothelial growth factor signaling pathway | 4 |
| cell differentiation | 4 |
Indications & clinical
Indications
18 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 |
| non-small cell lung carcinoma | 3 | MONDO:0005233 | EFO:0003060 |
| hepatocellular carcinoma | 3 | MONDO:0007256 | EFO:0000182 |
| adenocarcinoma | 2 | MONDO:0004970 | EFO:0000228 |
| clear cell renal carcinoma | 2 | MONDO:0005005 | EFO:0000349 |
| liposarcoma | 2 | MONDO:0005060 | EFO:0000569 |
| squamous cell carcinoma | 2 | MONDO:0005096 | EFO:0000707 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| renal cell carcinoma | 2 | MONDO:0005086 | EFO:0000681 |
| small cell lung carcinoma | 2 | MONDO:0008433 | EFO:0000702 |
| melanoma | 2 | MONDO:0005105 | EFO:0000756 |
| esophageal squamous cell carcinoma | 2 | MONDO:0005580 | EFO:0005922 |
| endometrium neoplasm | 2 | MONDO:0021251 | MONDO:0011962 |
| liver disorder | 1 | MONDO:0005154 | EFO:0001421 |
| oral cavity squamous cell carcinoma | 0 | MONDO:0004958 | EFO:0000199 |
3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 34.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 17 |
| PHASE1 | 9 |
| PHASE3 | 4 |
| PHASE1/PHASE2 | 2 |
| PHASE2/PHASE3 | 1 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT04164199 | PHASE3 | ACTIVE_NOT_RECRUITING | Study of Tislelizumab, Pamiparib, and Other Investigational Agents in Participants With Advanced Malignancies |
| NCT03906071 | PHASE3 | COMPLETED | Phase 3 Study of Sitravatinib Plus Nivolumab vs Docetaxel in Patients With Advanced Non-Squamous Non-Small Cell Lung Cancer |
| NCT04887870 | PHASE2/PHASE3 | COMPLETED | Study of Sitravatinib With or Without Other Anticancer Therapies Receiving Clinical Benefit From Parent Study |
| NCT04921358 | PHASE3 | TERMINATED | Tislelizumab in Combination With Sitravatinib in Participants With Locally Advanced or Metastatic Non-Small Cell Lung Cancer |
| NCT05564338 | PHASE3 | WITHDRAWN | Efficacy and Safety of Sitravatinib Plus Tislelizumab or Placebo Plus Tislelizumab Versus Placebo as Adjuvant Treatment in Participants With Hepatocellular Carcinoma |
| NCT05407519 | PHASE2 | RECRUITING | A Study to Evaluate Tislelizumab Combined With Sitravatinib as Adjuvant Therapy in Participants With HCC at High Risk of Recurrence After Curative Resection |
| NCT02664935 | PHASE2 | COMPLETED | National Lung Matrix Trial: Multi-drug Phase II Trial in Non-Small Cell Lung Cancer |
| NCT02954991 | PHASE2 | TERMINATED | Phase 2 Study of Glesatinib, Sitravatinib or Mocetinostat in Combination With Nivolumab in Non-Small Cell Lung Cancer |
| NCT02978859 | PHASE2 | COMPLETED | Sitravatinib in Advanced Liposarcoma and Other Soft Tissue Sarcomas |
| NCT03015740 | PHASE1/PHASE2 | COMPLETED | Sitravatinib and Nivolumab in Treating Patients With Advanced or Metastatic Kidney Cancer |
| NCT03606174 | PHASE2 | TERMINATED | A Phase 2 Study of Sitravatinib in Combination With PD-(L)1 Checkpoint Inhibitor Regimens in Patients With Advanced or Metastatic Urothelial Carcinoma |
| NCT03680521 | PHASE2 | COMPLETED | Neoadjuvant Sitravatinib in Combination With Nivolumab in Patients With Clear Cell Renal Cell Carcinoma |
| NCT03941873 | PHASE1/PHASE2 | COMPLETED | A Study to Investigate Sitravatinib as Monotherapy and in Combination With Tislelizumab in Participants With Unresectable Locally Advanced or Metastatic Hepatocellular Carcinoma or Gastric/Gastroesophageal Junction Cancer |
| NCT04123704 | PHASE2 | TERMINATED | Sitravatinib in Metastatic Breast Cancer |
| NCT04727996 | PHASE2 | UNKNOWN | Phase II Study of Sitravatinib in Combination With Tislelizumab in Patients With Advanced Biliary Tract Cancer |
| NCT04734262 | PHASE2 | UNKNOWN | A Phase II Study to Explore the Safety, Tolerability, and Preliminary Antitumor Activity of Sitravatinib Plus Tislelizumab or Combination With Nab-paclitaxel in Patients With Locally Recurrent or Metastatic Triple Negative Breast Cancer (TNBC) |
| NCT04904302 | PHASE2 | TERMINATED | Sitravatinib and Nivolumab for the Treatment of Metastatic or Advanced Clear Cell Renal Cell Cancer |
| NCT04925986 | PHASE2 | TERMINATED | Sitravatinib Plus Pembrolizumab in Patients With Advanced Treatment-Naïve PD-L1+ Non-Squamous NSCLC |
| NCT05104801 | PHASE2 | UNKNOWN | Sitravatinib With or Without Tislelizumab in Patients With Unresectable or Metastatic Melanoma |
| NCT05176925 | PHASE2 | TERMINATED | Tislelizumab Combined With Sitravatinib as Consolidation Treatment Following Concurrent Chemoradiation in Patients With Locally Advanced, Unresectable NSCLC |
| NCT05228496 | PHASE2 | UNKNOWN | A Study to Investigate the Efficacy and Safety of Tislelizumab Combined With Sitravatinib as Maintenance Therapy for ES-SCLC |
| NCT05419817 | PHASE2 | WITHDRAWN | Pembrolizumab With Sitravatinib in Recurrent Endometrial Cancer and Other Solid Tumors With Deficient Mismatch Repair System |
| NCT05461794 | PHASE2 | TERMINATED | Study To Investigate the Efficacy and Safety of Sitravatinib in Combination With Tislelizumab in Participants With Esophageal Squamous Cell Carcinoma |
| NCT05614453 | PHASE2 | WITHDRAWN | Tislelizumab in Combination With Sitravatinib for Recurrent/Metastatic Cervical Cancer After Platinum-Based Chemotherapy |
| NCT02219711 | PHASE1 | COMPLETED | Phase 1/1b Study of MGCD516 in Patients With Advanced Cancer |
| NCT03666143 | PHASE1 | COMPLETED | A Phase 1b Study to Assess Sitravatinib in Combination With Tislelizumab in Participants With Advanced Solid Tumors |
| NCT04472650 | PHASE1 | COMPLETED | Relative Bioavailability of Two Different Capsule Formulations of Sitravatinib in Healthy Adults |
| NCT04518046 | PHASE1 | COMPLETED | Study of Sitravatinib, Nivolumab and Ipilimumab in Advanced or Metastatic Clear-Cell Renal Cell Carcinoma or Other Solid Malignancies |
| NCT04772612 | PHASE1 | COMPLETED | A Study to Evaluate the Effect of Mild, Moderate, and Severe Hepatic Impairment on Pharmacokinetics of Sitravatinib |
| NCT04800614 | PHASE1 | COMPLETED | A Study to Explore the Effect of Food Before a Single Dose of Sitravatinib |
| NCT04887194 | PHASE1 | COMPLETED | PK Study to Assess Drug-drug Interaction and QTc Between Sitravatinib and a Cocktail of Substrates |
| NCT04935112 | PHASE1 | COMPLETED | A Study to Explore the Effect of Acid-reducing Agents |
| NCT05255276 | PHASE1 | COMPLETED | PK Study to Assess Drug-drug Interaction Between Sitravatinib and a P-gp Inducer and an Inhibitor. |
| NCT03575598 | EARLY_PHASE1 | COMPLETED | Sitravatinib (MGCD516) and Nivolumab in Oral Cavity Cancer Window Opportunity Study |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
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.
280 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| Afatinib | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| AXITINIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| Crizotinib | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| FEDRATINIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| Gefitinib | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| SORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| SUNITINIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| LESTAURTINIB | ChEMBL | Phase 3 | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| LINIFANIB | ChEMBL | Phase 3 | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| FORETINIB | ChEMBL | Phase 2 | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| R-406 | ChEMBL | Phase 2 | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| SU-014813 | ChEMBL | Phase 2 | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| TOZASERTIB | ChEMBL | Phase 2 | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| Selumetinib | PubChem | Approved | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| ERLOTINIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, PDGFRA |
| MIDOSTAURIN | ChEMBL + PubChem | Phase 4 (approved) | AXL, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| QUIZARTINIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, NTRK1, PDGFRA |
| VANDETANIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, PDGFRA |
| CEDIRANIB | ChEMBL | Phase 3 | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, PDGFRA |
| REBASTINIB | ChEMBL | Phase 2 | AXL, DDR2, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| Idelalisib | PubChem | Approved | AXL, DDR2, EPHA3, FLT1, FLT3, FLT4, KIT, MERTK, MET, NTRK1, PDGFRA |
| CABOZANTINIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, FLT1, FLT3, FLT4, KDR, KIT, MERTK, MET, NTRK1 |
| DOVITINIB | ChEMBL | Phase 3 | AXL, DDR2, FLT1, FLT3, FLT4, KDR, KIT, MERTK, NTRK1, PDGFRA |
| DORAMAPIMOD | ChEMBL | Phase 2 | DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MERTK, NTRK1, PDGFRA |
| TANDUTINIB | ChEMBL | Phase 2 | AXL, DDR2, FLT1, FLT3, FLT4, KDR, KIT, MERTK, NTRK1, PDGFRA |
| BOSUTINIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT3, KIT, MERTK, MET, NTRK1, PDGFRA |
| ENTRECTINIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, FLT1, FLT3, FLT4, KDR, KIT, MET, NTRK1 |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | DDR2, FLT1, FLT3, FLT4, KDR, KIT, MET, NTRK1, PDGFRA |
| TIVOZANIB | ChEMBL + PubChem | Phase 4 (approved) | DDR2, EPHA3, FLT1, FLT3, FLT4, KDR, KIT, MET, PDGFRA |
| BMS-777607 | ChEMBL | Phase 2 | AXL, DDR2, FLT3, KDR, KIT, MERTK, MET, NTRK1, PDGFRA |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | AXL, DDR2, FLT1, FLT3, FLT4, KDR, KIT, MET, PDGFRA |
| ILORASERTIB | ChEMBL | Phase 2 | AXL, FLT1, FLT3, FLT4, KDR, KIT, MET, NTRK1, PDGFRA |
| DASATINIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, DDR2, EPHA3, FLT1, FLT3, KDR, KIT, PDGFRA |
| CANERTINIB | ChEMBL | Phase 3 | AXL, EPHA3, FLT1, FLT3, KDR, KIT, MET, PDGFRA |
| CENISERTIB | ChEMBL | Phase 2 | AXL, FLT1, FLT3, FLT4, KDR, KIT, MET, PDGFRA |
| OSI-632 | ChEMBL | Phase 2 | AXL, DDR2, FLT1, FLT3, FLT4, KDR, MET, PDGFRA |
| RAF-265 | ChEMBL | Phase 2 | DDR2, FLT1, FLT3, FLT4, KDR, KIT, MET, PDGFRA |
| PONATINIB | ChEMBL + PubChem | Phase 4 (approved) | DDR2, FLT1, FLT3, KDR, KIT, NTRK1, PDGFRA |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT3, FLT4, KDR, KIT, MET, PDGFRA |
| AT-9283 | ChEMBL | Phase 2 | FLT1, FLT3, FLT4, KDR, MERTK, MET, PDGFRA |
| BEMCENTINIB | ChEMBL | Phase 2 | AXL, FLT3, KDR, KIT, MERTK, MET, PDGFRA |
| MERESTINIB | ChEMBL | Phase 2 | AXL, DDR2, FLT3, KDR, MERTK, MET, NTRK1 |
| MK-2461 | ChEMBL | Phase 2 | FLT1, FLT3, FLT4, KDR, MERTK, MET, NTRK1 |
| BRIGATINIB | ChEMBL + PubChem | Phase 4 (approved) | EPHA3, FLT3, FLT4, KDR, KIT, MET |
| IMATINIB | ChEMBL + PubChem | Phase 4 (approved) | DDR2, EPHA3, FLT3, KDR, KIT, PDGFRA |
| NERATINIB | ChEMBL + PubChem | Phase 4 (approved) | AXL, EPHA3, FLT3, KDR, MERTK, MET |
| PEXIDARTINIB | ChEMBL + PubChem | Phase 4 (approved) | DDR2, FLT1, FLT3, KDR, KIT, PDGFRA |
| CERITINIB | ChEMBL | Phase 4 (approved) | FLT3, KDR, KIT, MET, NTRK1, PDGFRA |
| LENVATINIB | ChEMBL | Phase 4 (approved) | DDR2, FLT1, FLT4, KDR, KIT, PDGFRA |
| ALVOCIDIB | ChEMBL | Phase 3 | AXL, EPHA3, FLT3, KIT, MERTK, PDGFRA |
| MOTESANIB | ChEMBL | Phase 3 | FLT1, FLT3, FLT4, KDR, KIT, PDGFRA |
| SEMAXANIB | ChEMBL | Phase 3 | FLT1, FLT3, FLT4, KDR, KIT, PDGFRA |
| CEP-32496 | ChEMBL | Phase 2 | DDR2, FLT1, FLT3, KDR, KIT, MET |
| DANUSERTIB | ChEMBL | Phase 2 | DDR2, FLT3, FLT4, KDR, KIT, NTRK1 |
| ENMD-2076 | ChEMBL | Phase 2 | DDR2, FLT3, KDR, KIT, NTRK1, PDGFRA |
| GLESATINIB | ChEMBL | Phase 2 | AXL, DDR2, FLT3, KDR, MERTK, MET |
| PELITINIB | ChEMBL | Phase 2 | AXL, EPHA3, FLT3, KDR, MERTK, MET |
| Binimetinib | PubChem | Approved | DDR2, FLT3, KDR, MERTK, MET, NTRK1 |
Related Atlas pages
- Genes: PDGFRA, KIT, FLT3, FLT1, KDR, FLT4, MET, NTRK1, EPHA3, AXL, MERTK, DDR2
- Diseases: neoplasm, non-small cell lung carcinoma, hepatocellular carcinoma
- Drugs: Afatinib, Axitinib, Crizotinib, Fedratinib, Gefitinib, Pazopanib, Sorafenib, Sunitinib, Nintedanib, Lestaurtinib, Linifanib, Selumetinib, Erlotinib, Midostaurin, Quizartinib, Vandetanib, Cediranib, Idelalisib, Cabozantinib, Dovitinib, Bosutinib, Entrectinib, Regorafenib, Tivozanib, Dasatinib, Canertinib, Ponatinib, Infigratinib, Brigatinib, Imatinib, Neratinib, Pexidartinib, Ceritinib, Lenvatinib, Alvocidib, Motesanib, Semaxanib, Binimetinib