Cediranib
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Also known as Azd-2171AZD2171RecentinZD-2171SID103905340SID137275941Cediranib maleateÊCediranib maleateÂ
Summary
Cediranib (CHEMBL491473) is a phase-3 clinical-stage small molecule (ATC L01EK02) targeting PDGFRA, PDGFRB, and KIT; indicated across 29 conditions including neoplasm and glioblastoma; with CIViC clinical evidence for 2 variant-indication associations (e.g. BRCA1 Mutation in ovarian cancer).
At a glance
- Status: Max clinical phase 3 (not approved)
- Modality: Small molecule
- ATC class: L01EK02
- Targets: 8 (PDGFRA, PDGFRB, KIT…)
- Indications: 29 conditions
- Clinical trials: 56
- Precision-oncology evidence (CIViC): 2 variant–indication associations
- Chemistry: 450.5 Da · C25H27FN4O3
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL491473 |
| Name | Cediranib |
| Type | Small molecule |
| Max phase | 3 |
| FDA approved | no |
| PubChem CID | 9933475 |
| ATC | L01EK02 |
| Molecular formula | C25H27FN4O3 |
| Molecular weight | 450.5 |
| InChIKey | XXJWYDDUDKYVKI-UHFFFAOYSA-N |
SMILES: CC1=CC2=C(N1)C=CC(=C2F)OC3=NC=NC4=CC(=C(C=C43)OC)OCCCN5CCCC5
IUPAC name: 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline
Also known as: Azd-2171, AZD-2171, AZD2171, Cediranib, Recentin, ZD-2171, SID103905340, CEDIRANIB, SID137275941, Cediranib maleateÊ, Cediranib maleateÂ
Parent form; salt/anhydrous children: CHEMBL2103798
Patent coverage: 3,303 distinct patent families (9,098 SureChEMBL compound mentions), from 4 matched compound structure(s). One matched structure accounts for 6,553 (72%) 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 | 7.44 | 6.2% | P16234 |
| PDGFRB | platelet derived growth factor receptor beta | Inhibition | 8.3 | 2.3% | P09619 |
| KIT | KIT proto-oncogene, receptor tyrosine kinase | Inhibition | 8.52 | 0.5% | P10721 |
| CSF1R | colony stimulating factor 1 receptor | Inhibition | 6.96 | 0% | P07333 |
| FLT3 | fms related receptor tyrosine kinase 3 | Inhibition | 6 | 0.9% | P36888 |
| FLT1 | fms related receptor tyrosine kinase 1 | Inhibition | 8.3 | 0.1% | P17948 |
| KDR | kinase insert domain receptor | Inhibition | 8.96 | 1.1% | P35968 |
| FLT4 | fms related receptor tyrosine kinase 4 | Inhibition | 8.52 | 0.2% | P35916 |
Broader ChEMBL bioactivity targets: 89 (assay-derived). Sample: Serine/threonine-protein kinase TAO2, Serine/threonine-protein kinase/endoribonuclease IRE1, Receptor tyrosine-protein kinase erbB-2, Tyrosine-protein kinase Fyn, 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.
Bioactivity
ChEMBL activities: 194 potent at pChembl ≥ 5 of 203 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| KIT | 9.57 | Kd | 0.27 | nM | CHEMBL_ACT_7567185 |
| KIT | 9.51 | Kd | 0.31 | nM | CHEMBL_ACT_7567187 |
| KIT | 9.49 | Kd | 0.32 | nM | CHEMBL_ACT_7567186 |
| PDGFRB | 9.49 | Kd | 0.32 | nM | CHEMBL_ACT_7567270 |
| KIT | 9.42 | Kd | 0.38 | nM | CHEMBL_ACT_7567180 |
| PDGFRA | 9.39 | Kd | 0.41 | nM | CHEMBL_ACT_7567432 |
| KDR | 9.3 | IC50 | 0.5 | nM | CHEMBL_ACT_18955285 |
| KDR | 9.3 | Ki | 0.5 | nM | CHEMBL_ACT_27790661 |
| KIT | 9.27 | Kd | 0.54 | nM | CHEMBL_ACT_7567184 |
| FLT1 | 9.13 | Kd | 0.74 | nM | CHEMBL_ACT_7567248 |
| KDR | 9 | IC50 | 1 | nM | CHEMBL_ACT_12138565 |
| KDR | 9 | IC50 | 1 | nM | CHEMBL_ACT_23289709 |
| KDR | 8.96 | Kd | 1.1 | nM | CHEMBL_ACT_7567255 |
| DDR1 | 8.77 | Kd | 1.7 | nM | CHEMBL_ACT_7567245 |
| KDR | 8.76 | IC50 | 1.72 | nM | CHEMBL_ACT_25484192 |
| FLT1 | 8.67 | IC50 | 2.13 | nM | CHEMBL_ACT_25484155 |
| KDR | 8.57 | IC50 | 2.7 | nM | CHEMBL_ACT_16394871 |
| FLT4 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_12138564 |
| FLT4 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_23289717 |
| KDR | 8.4 | IC50 | 4 | nM | CHEMBL_ACT_3595763 |
| FLT4 | 8.37 | Kd | 4.3 | nM | CHEMBL_ACT_7567249 |
| FLT1 | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_12138566 |
| PDGFRB | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_23289726 |
| FLT1 | 8.3 | IC50 | 5 | nM | CHEMBL_ACT_23289735 |
| STK35 | 8.27 | Kd | 5.4 | nM | CHEMBL_ACT_7569087 |
| RET | 8.21 | Kd | 6.1 | nM | CHEMBL_ACT_7569053 |
| FLT4 | 8.2 | Ki | 6.31 | nM | CHEMBL_ACT_9635456 |
| RET | 8.12 | Kd | 7.5 | nM | CHEMBL_ACT_7569054 |
| ACSL5 | 8.1 | Kd | 8 | nM | CHEMBL_ACT_17880028 |
| FLT1 | 8.1 | Ki | 7.94 | nM | CHEMBL_ACT_9661362 |
Target pathways
Aggregated over 8 target gene(s): PDGFRA, PDGFRB, KIT, CSF1R, FLT3, FLT1, KDR, FLT4.
Top Reactome pathways
82 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| PIP3 activates AKT signaling | 4 | FLT3, KIT, PDGFRA, PDGFRB |
| Constitutive Signaling by Aberrant PI3K in Cancer | 4 | FLT3, KIT, PDGFRA, PDGFRB |
| RAF/MAP kinase cascade | 4 | FLT3, KIT, PDGFRA, PDGFRB |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 4 | FLT3, KIT, PDGFRA, PDGFRB |
| VEGF binds to VEGFR leading to receptor dimerization | 3 | FLT1, FLT4, KDR |
| Downstream signal transduction | 2 | PDGFRA, PDGFRB |
| Signaling by PDGF | 2 | PDGFRA, PDGFRB |
| Neuropilin interactions with VEGF and VEGFR | 2 | FLT1, KDR |
| High laminar flow shear stress activates signaling by PIEZO1 and PECAM1:CDH5:KDR in endothelial cells | 2 | FLT4, KDR |
| 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 |
| Integrin cell surface interactions | 1 | KDR |
| PI3K/AKT Signaling in Cancer | 1 | KIT |
| VEGFA-VEGFR2 Pathway | 1 | KDR |
| Other interleukin signaling | 1 | CSF1R |
| VEGFR2 mediated cell proliferation | 1 | KDR |
| 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 |
| 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 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| cell surface receptor protein tyrosine kinase signaling pathway | 8 |
| positive regulation of cell population proliferation | 8 |
| cell migration | 8 |
| protein autophosphorylation | 8 |
| protein phosphorylation | 8 |
| peptidyl-tyrosine phosphorylation | 7 |
| positive regulation of cell migration | 7 |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 7 |
| positive regulation of ERK1 and ERK2 cascade | 5 |
| positive regulation of MAPK cascade | 5 |
| chemotaxis | 4 |
| angiogenesis | 4 |
| hemopoiesis | 4 |
| vascular endothelial growth factor signaling pathway | 4 |
| regulation of actin cytoskeleton organization | 3 |
Indications & clinical
Indications
29 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 |
| glioblastoma | 3 | MONDO:0018177 | EFO:0000519 |
| ovarian neoplasm | 3 | MONDO:0021068 | EFO:0003893 |
| ovarian cancer | 3 | MONDO:0008170 | MONDO:0008170 |
| renal cell carcinoma | 2 | MONDO:0005086 | EFO:0000681 |
| breast carcinoma | 2 | MONDO:0004989 | EFO:0000305 |
| prostate adenocarcinoma | 2 | MONDO:0005082 | EFO:0000673 |
| non-small cell lung carcinoma | 2 | MONDO:0005233 | EFO:0003060 |
| biliary tract neoplasm | 2 | MONDO:0005304 | EFO:0003891 |
| alveolar soft part sarcoma | 2 | MONDO:0011655 | EFO:0007143 |
| small cell lung carcinoma | 2 | MONDO:0008433 | EFO:0000702 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| metastatic prostate carcinoma | 2 | MONDO:0004956 | EFO:0000196 |
| colorectal neoplasm | 2 | MONDO:0005335 | MONDO:0005575 |
| rectal cancer | 1 | MONDO:0006519 | EFO:1000657 |
| acute myeloid leukemia | 1 | MONDO:0018874 | EFO:0000222 |
| leukemia | 1 | MONDO:0005059 | EFO:0000565 |
| metastatic melanoma | 1 | MONDO:0005191 | EFO:0002617 |
| metastatic neoplasm | 1 | MONDO:0024883 | EFO:0009709 |
| thyroid gland carcinoma | 1 | MONDO:0015075 | EFO:0002892 |
| gastric neoplasm | 1 | MONDO:0021085 | MONDO:0001056 |
| peritoneal neoplasm | 1 | MONDO:0006901 | MONDO:0002087 |
| fallopian tube neoplasm | 1 | MONDO:0021092 | MONDO:0002158 |
| lung neoplasm | 1 | MONDO:0021117 | MONDO:0008903 |
| endometrium neoplasm | 1 | MONDO:0021251 | MONDO:0011962 |
| brain neoplasm | 1 | MONDO:0021211 | EFO:0003833 |
3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 56.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 24 |
| PHASE1 | 20 |
| PHASE3 | 4 |
| PHASE2/PHASE3 | 3 |
| PHASE1/PHASE2 | 3 |
| EARLY_PHASE1 | 1 |
| Not specified | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT02502266 | PHASE2/PHASE3 | ACTIVE_NOT_RECRUITING | Testing the Combination of Cediranib and Olaparib in Comparison to Each Drug Alone or Other Chemotherapy in Recurrent Platinum-Resistant Ovarian Cancer |
| NCT00384176 | PHASE2/PHASE3 | COMPLETED | First Line Metastatic Colorectal Cancer Therapy in Combination With FOLFOX |
| NCT00399035 | PHASE3 | COMPLETED | Cediranib (AZD2171, RECENTIN™) in Addition to Chemotherapy in Patients With Untreated Metastatic Colorectal Cancer |
| NCT00532194 | PHASE3 | UNKNOWN | An RCT of Concurrent and Maintenance Cediranib in Women With Platinum-sensitive Relapsed Ovarian Cancer |
| NCT00777153 | PHASE3 | COMPLETED | Cediranib in Combination With Lomustine Chemotherapy in Recurrent Glioblastoma |
| NCT00939848 | PHASE2/PHASE3 | COMPLETED | Cediranib Versus Placebo Plus Cisplatin/Gemcitabine Chemotherapy for Patients With Advanced Biliary Tract Cancers |
| NCT03278717 | PHASE3 | UNKNOWN | Study Evaluating the Efficacy of Maintenance Olaparib and Cediranib or Olaparib Alone in Ovarian Cancer Patients |
| NCT02484404 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Phase I/II Study of the Anti-Programmed Death Ligand-1 Durvalumab Antibody (MEDI4736) in Combination With Olaparib and/or Cediranib for Advanced Solid Tumors and Advanced or Recurrent Ovarian, Triple Negative Breast, Lung, Prostate and Colorectal Can… |
| NCT02893917 | PHASE2 | ACTIVE_NOT_RECRUITING | Testing Two Oral Drugs Combination (Cediranib and Olaparib) Compared to a Single Drug (Olaparib) for Men With Advanced Prostate Cancer |
| NCT02974621 | PHASE2 | ACTIVE_NOT_RECRUITING | Cediranib Maleate and Olaparib Compared to Bevacizumab in Treating Patients With Recurrent Glioblastoma |
| NCT03334617 | PHASE2 | ACTIVE_NOT_RECRUITING | Phase II Umbrella Study of Novel Anti-cancer Agents in Participants With NSCLC Who Progressed on an Anti-PD-1/PD-L1 Containing Therapy |
| NCT03851614 | PHASE2 | ACTIVE_NOT_RECRUITING | Study of DNA Damage, Angiogenesis, and PD-L1 Inhibitors in Advanced Solid Tumors |
| NCT04090567 | PHASE2 | RECRUITING | Olaparib With Cediranib or AZD6738 for the Treatment of Advanced or Metastatic Germline BRCA Mutated Breast Cancer |
| NCT04487587 | PHASE2 | ACTIVE_NOT_RECRUITING | A Phase II Clinical Trial of Cediranib and Olaparib Maintenance in Advanced Recurrent Cervical Cancer |
| NCT00264004 | PHASE2 | COMPLETED | Study to Investigate the Management of Hypertension and Efficacy of AZD2171 in Patients With Advanced Solid Tumours |
| NCT00278889 | PHASE2 | COMPLETED | Second Line ColoRectal Cancer Therapy in Combination With Combination of FOL- Folinic Acid(Leucovorin), F - Fluorouracil and OX - Oxaliplatin (FOLFOX) |
| NCT00306891 | PHASE2 | COMPLETED | Effect of Food Upon Pharmacokinetics of Single Oral Dose of Cediranib (AZD2171, Recentin™) |
| NCT00385203 | PHASE2 | COMPLETED | The Biological Activity of Cediranib (AZD2171) in Gastro-Intestinal Stromal Tumours(GIST). |
| NCT00423332 | PHASE2 | COMPLETED | Cediranib (AZD2171, RECENTIN™) in Metastatic or Recurrent Renal Cell Carcinoma |
| NCT00436956 | PHASE2 | COMPLETED | AZD2171 to Treat Prostate Cancer |
| NCT00454805 | PHASE2 | COMPLETED | AZD2171 in Addition to Fulvestrant in Patients With Advanced Breast Cancer. |
| NCT00494221 | PHASE1/PHASE2 | COMPLETED | A Phase I/II Study of Cediranib (AZD2171) in Japanese Metastatic Colorectal Cancer Patients in Combination With FOLFOX |
| NCT00942877 | PHASE2 | COMPLETED | Phase II Study of Cediranib (AZD2171) in Patients With Alveolar Soft Part Sarcoma |
| NCT01208051 | PHASE1/PHASE2 | COMPLETED | Cediranib Maleate With or Without Lenalidomide for the Treatment of Thyroid Cancer |
| NCT01262612 | PHASE2 | TERMINATED | Cediranib as Palliative Treatment in Patients With Symptomatic Malignant Ascites or Pleural Effusion |
| NCT01337401 | PHASE2 | UNKNOWN | A Trial of Cediranib in the Treatment of Patients With Alveolar Soft Part Sarcoma (CASPS) |
| NCT01391962 | PHASE2 | COMPLETED | Sunitinib or Cediranib for Alveolar Soft Part Sarcoma |
| NCT02340611 | PHASE2 | COMPLETED | A Study of Cediranib and Olaparib at the Time Ovarian Cancer Worsens on Olaparib |
| NCT02889900 | PHASE2 | COMPLETED | Efficacy and Safety Study of Cediranib in Combination With Olaparib in Patients With Recurrent Platinum-Resistant Ovarian Cancer |
| NCT02899728 | PHASE2 | TERMINATED | Olaparib, Cediranib Maleate, and Standard Chemotherapy in Treating Patients With Small Cell Lung Cancer |
| NCT03117933 | PHASE2 | COMPLETED | Olaparib +/- Cediranib or Chemotherapy in Patients With Platinum-resistant Ovarian Cancer |
| NCT03314740 | PHASE2 | COMPLETED | Best Approach in Recurrent-Ovarian-Cancer-with Cediranib-Olaparib |
| NCT03570437 | PHASE2 | UNKNOWN | Does Cediranib With Paclitaxel, or Cediranib and Olaparib, Treat Advanced Endometrial Cancer Better Than Paclitaxel? |
| NCT03741426 | PHASE2 | UNKNOWN | WIRE - Novel Treatments in Renal Cell Cancer |
| NCT00750841 | PHASE1 | ACTIVE_NOT_RECRUITING | Study of the Effect of Rifampicin on the Pharmacokinetics (PK) of Multiple Doses of Cediranib in Patients With Solid Tumours |
| NCT01364051 | PHASE1 | ACTIVE_NOT_RECRUITING | Cediranib Maleate and Selumetinib Sulfate in Treating Patients With Solid Malignancies |
| NCT00243347 | PHASE1 | COMPLETED | The Effects of AZD2171 in Patients With Non-Small Cell Lung Cancer or Head & Neck Cancer |
| NCT00321581 | PHASE1 | COMPLETED | AZD2171 to Treat Children and Adolescents With Solid Tumors or Acute Myelogenous Leukemia |
| NCT00475956 | PHASE1 | COMPLETED | Safety and Tolerability Study of AZD2171 in Combination With AZD0530 in Patients With Advanced Solid Tumours |
| NCT00501605 | PHASE1 | COMPLETED | Phase I Study With AZD2171 in Patients With Advanced Solid Malignant Tumors and Liver Metastases |
Clinical evidence (CIViC)
Variant × indication × effect (2 predictive associations from 2 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| BRCA1 Mutation | Ovarian Cancer | Sensitivity/Response | Cediranib + Olaparib | CIViC B | EID1677 |
| BRCA2 Mutation | Ovarian Cancer | Sensitivity/Response | Cediranib + Olaparib | CIViC B | EID1678 |
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.
250 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| Afatinib | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| Crizotinib | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| PAZOPANIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| AXITINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| FEDRATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| MIDOSTAURIN | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| NINTEDANIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| QUIZARTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| SORAFENIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| SUNITINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| VANDETANIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| DOVITINIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| LESTAURTINIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| LINIFANIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| MOTESANIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| SEMAXANIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| CENISERTIB | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| DORAMAPIMOD | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| FORETINIB | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| ILORASERTIB | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| R-406 | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| RAF-265 | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| SU-014813 | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| TANDUTINIB | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| TOZASERTIB | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| Selumetinib | PubChem | Approved | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| Gefitinib | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA |
| DASATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, KDR, KIT, PDGFRA, PDGFRB |
| ERLOTINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| PEXIDARTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, KDR, KIT, PDGFRA, PDGFRB |
| PONATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, KDR, KIT, PDGFRA, PDGFRB |
| TIVOZANIB | ChEMBL | Phase 4 (approved) | FLT1, FLT3, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| BRIVANIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| VATALANIB | ChEMBL | Phase 3 | CSF1R, FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| REBASTINIB | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, FLT4, KDR, KIT, PDGFRA |
| Idelalisib | PubChem | Approved | CSF1R, FLT1, FLT3, FLT4, KIT, PDGFRA, PDGFRB |
| IMATINIB | ChEMBL + PubChem | Phase 4 (approved) | CSF1R, FLT3, KDR, KIT, PDGFRA, PDGFRB |
| ENTRECTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT1, FLT3, FLT4, KDR, KIT |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT3, FLT4, KDR, KIT, PDGFRA |
| LENVATINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR, KIT, PDGFRA, PDGFRB |
| CANERTINIB | ChEMBL | Phase 3 | FLT1, FLT3, KDR, KIT, PDGFRA, PDGFRB |
| CEP-32496 | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, KDR, KIT, PDGFRB |
| OSI-632 | ChEMBL | Phase 2 | FLT1, FLT3, FLT4, KDR, PDGFRA, PDGFRB |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, FLT4, KDR, KIT |
| CABOZANTINIB | ChEMBL | Phase 4 (approved) | FLT1, FLT3, FLT4, KDR, KIT |
| NILOTINIB | ChEMBL | Phase 4 (approved) | CSF1R, FLT3, KIT, PDGFRA, PDGFRB |
| NINTEDANIB ESYLATE | ChEMBL | Phase 4 (approved) | FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| BARASERTIB | ChEMBL | Phase 3 | FLT3, KDR, KIT, PDGFRA, PDGFRB |
| SARACATINIB | ChEMBL | Phase 3 | FLT3, KDR, KIT, PDGFRA, PDGFRB |
| VIMSELTINIB | ChEMBL | Phase 3 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB |
| AT-9283 | ChEMBL | Phase 2 | FLT1, FLT3, FLT4, KDR, PDGFRA |
| BFH-772 | ChEMBL | Phase 2 | FLT1, FLT4, KDR, KIT, PDGFRB |
| CEP-11981 | ChEMBL | Phase 2 | CSF1R, FLT1, FLT3, KDR, PDGFRA |
| ENMD-2076 | ChEMBL | Phase 2 | CSF1R, FLT3, KDR, KIT, PDGFRA |
| MK-2461 | ChEMBL | Phase 2 | FLT1, FLT3, FLT4, KDR, PDGFRB |
| SOTULETINIB | ChEMBL | Phase 2 | CSF1R, FLT3, KIT, PDGFRA, PDGFRB |
| CERITINIB | ChEMBL | Phase 4 (approved) | FLT3, KDR, KIT, PDGFRA |
Related Atlas pages
- Genes: PDGFRA, PDGFRB, KIT, CSF1R, FLT3, FLT1, KDR, FLT4
- Diseases: neoplasm, glioblastoma, ovarian neoplasm, ovarian cancer, ovarian carcinoma
- Drugs: Afatinib, Crizotinib, Pazopanib, Regorafenib, Axitinib, Fedratinib, Midostaurin, Nintedanib, Quizartinib, Sorafenib, Sunitinib, Vandetanib, Dovitinib, Lestaurtinib, Linifanib, Motesanib, Semaxanib, Selumetinib, Gefitinib, Dasatinib, Erlotinib, Pexidartinib, Ponatinib, Tivozanib, Brivanib, Vatalanib, Idelalisib, Imatinib, Entrectinib, Infigratinib, Lenvatinib, Canertinib, Bosutinib, Brigatinib, Cabozantinib, Nilotinib, Barasertib, Saracatinib, Vimseltinib, Ceritinib