Nintedanib
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Also known as BIBF 1120Bibf-1120BIBF1120IntedanibNintedanib component of ofevOfevVargatefNINTEDANIB (BIBF 1120)NintedanibUS10669235
Summary
Nintedanib (CHEMBL502835) is an approved small-molecule antineoplastic agent (ATC L01EX09) targeting LATS1, PDGFRA, and PDGFRB; indicated across 50 conditions including neoplasm and systemic sclerosis; with CIViC clinical evidence for 1 variant-indication association (e.g. CCDC6::RET Fusion in lung non-small cell carcinoma).
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: L01EX09
- Targets: 10 (LATS1, PDGFRA, PDGFRB…)
- Indications: 50 conditions
- Clinical trials: 157
- Precision-oncology evidence (CIViC): 1 variant–indication association
- Chemistry: C31H33N5O4
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL502835 |
| Name | Nintedanib |
| Type | Small molecule |
| Max phase | 4 |
| ChEBI | CHEBI:85164 |
| ATC | L01EX09 |
| Molecular formula | C31H33N5O4 |
| InChIKey | XZXHXSATPCNXJR-ZIADKAODSA-N |
SMILES: COC(=O)c1ccc2c(c1)NC(=O)/C2=C(\Nc1ccc(N(C)C(=O)CN2CCN(C)CC2)cc1)c1ccccc1
ChEBI definition: A member of the class of oxindoles that is a kinase inhibitor used (in the form of its ethylsulfonate salt) for the treatment of idiopathic pulmonary fibrosis and cancer.
Pharmacological roles (ChEBI): antineoplastic agent, tyrosine kinase inhibitor, vascular endothelial growth factor receptor antagonist, fibroblast growth factor receptor antagonist, angiogenesis inhibitor, antifibrotic agent.
Also known as: BIBF 1120, Bibf-1120, BIBF-1120, BIBF1120, Intedanib, Nintedanib, Nintedanib component of ofev, Ofev, Vargatef, NINTEDANIB, NINTEDANIB (BIBF 1120), Nintedanib (BIBF 1120)
Parent form; salt/anhydrous children: CHEMBL3039504
Patent coverage: 3,489 distinct patent families (8,545 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 8,171 (96%) 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 |
|---|---|---|---|---|---|
| LATS1 | large tumor suppressor kinase 1 | Inhibition | 4.97 | 0.1% | O95835 |
| PDGFRA | platelet derived growth factor receptor alpha | Inhibition | 7.23 | 6.2% | P16234 |
| PDGFRB | platelet derived growth factor receptor beta | Inhibition | 7.19 | 2.3% | P09619 |
| FGFR1 | fibroblast growth factor receptor 1 | Inhibition | 7.16 | 11.5% | P11362 |
| FGFR2 | fibroblast growth factor receptor 2 | Inhibition | 7.43 | 1.7% | P21802 |
| FGFR3 | fibroblast growth factor receptor 3 | Inhibition | 6.97 | 0.5% | P22607 |
| FGFR4 | fibroblast growth factor receptor 4 | Inhibition | 6.21 | 0.7% | P22455 |
| FLT1 | fms related receptor tyrosine kinase 1 | Inhibition | 7.51 | 0.1% | P17948 |
| KDR | kinase insert domain receptor | Inhibition | 7.68 | 1.1% | P35968 |
| FLT4 | fms related receptor tyrosine kinase 4 | Inhibition | 7.89 | 0.2% | P35916 |
Broader ChEMBL bioactivity targets: 232 (assay-derived). Sample: Leucine-rich repeat serine/threonine-protein kinase 2, Rhodopsin kinase GRK7, Homeodomain-interacting protein kinase 4, Serine/threonine-protein kinase/endoribonuclease IRE1, Serine/threonine-protein kinase OSR1, STE20/SPS1-related proline-alanine-rich protein kinase, Mitogen-activated protein kinase kinase kinase 13, Serine/threonine-protein kinase ICK, Mitogen-activated protein kinase kinase kinase 15, Microtubule-associated serine/threonine-protein kinase 1.
Bioactivity
ChEMBL activities: 408 potent at pChembl ≥ 5 of 414 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| FLT3 | 9.38 | Kd | 0.42 | nM | CHEMBL_ACT_7574800 |
| FLT3 | 9.15 | Kd | 0.71 | nM | CHEMBL_ACT_7574799 |
| FLT3 | 9.15 | Kd | 0.7 | nM | CHEMBL_ACT_7574801 |
| KDR | 8.98 | IC50 | 1.05 | nM | CHEMBL_ACT_29116554 |
| PDGFRB | 8.74 | IC50 | 1.8 | nM | CHEMBL_ACT_18330886 |
| PDGFRB | 8.74 | IC50 | 1.8 | nM | CHEMBL_ACT_25952266 |
| MAP2K5 | 8.74 | Kd | 1.8 | nM | CHEMBL_ACT_7575034 |
| PDGFRA | 8.72 | IC50 | 1.9 | nM | CHEMBL_ACT_17957990 |
| PDGFRB | 8.7 | IC50 | 2 | nM | CHEMBL_ACT_13392443 |
| BMP2K | 8.66 | Kd | 2.2 | nM | CHEMBL_ACT_7574975 |
| PDGFRA | 8.64 | IC50 | 2.3 | nM | CHEMBL_ACT_18314194 |
| KCNH2 | 8.59 | IC50 | 2.6 | nM | CHEMBL_ACT_18330841 |
| FLT3 | 8.59 | Kd | 2.6 | nM | CHEMBL_ACT_7574803 |
| KIT | 8.57 | Kd | 2.7 | nM | CHEMBL_ACT_7573114 |
| KIT | 8.54 | Kd | 2.9 | nM | CHEMBL_ACT_7573116 |
| KDR | 8.54 | Kd | 2.9 | nM | CHEMBL_ACT_7573185 |
| RET | 8.52 | Kd | 3 | nM | CHEMBL_ACT_17935250 |
| FLT4 | 8.52 | IC50 | 3 | nM | CHEMBL_ACT_17957988 |
| KDR | 8.51 | IC50 | 3.1 | nM | CHEMBL_ACT_18330868 |
| KDR | 8.51 | IC50 | 3.1 | nM | CHEMBL_ACT_25952267 |
| FLT4 | 8.49 | IC50 | 3.2 | nM | CHEMBL_ACT_18314196 |
| KDR | 8.48 | IC50 | 3.3 | nM | CHEMBL_ACT_17957957 |
| PDGFRB | 8.46 | IC50 | 3.5 | nM | CHEMBL_ACT_18314118 |
| P9WI81 | 8.44 | Kd | 3.6 | nM | CHEMBL_ACT_7575018 |
| PDGFRB | 8.43 | IC50 | 3.7 | nM | CHEMBL_ACT_17957974 |
| FLT3 | 8.42 | Kd | 3.8 | nM | CHEMBL_ACT_13475365 |
| PDGFRB | 8.42 | IC50 | 3.8 | nM | CHEMBL_ACT_20681243 |
| KDR | 8.42 | Ki | 3.8 | nM | CHEMBL_ACT_27981029 |
| KDR | 8.42 | Ki | 3.8 | nM | CHEMBL_ACT_28409693 |
| KDR | 8.42 | Ki | 3.8 | nM | CHEMBL_ACT_28576667 |
Target pathways
Aggregated over 10 target gene(s): LATS1, PDGFRA, PDGFRB, FGFR1, FGFR2, FGFR3, FGFR4, FLT1, KDR, FLT4.
Top Reactome pathways
74 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| PIP3 activates AKT signaling | 6 | FGFR1, FGFR2, FGFR3, FGFR4, PDGFRA, PDGFRB |
| Constitutive Signaling by Aberrant PI3K in Cancer | 6 | FGFR1, FGFR2, FGFR3, FGFR4, PDGFRA, PDGFRB |
| RAF/MAP kinase cascade | 6 | FGFR1, FGFR2, FGFR3, FGFR4, PDGFRA, PDGFRB |
| PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling | 6 | FGFR1, FGFR2, FGFR3, FGFR4, PDGFRA, PDGFRB |
| PI3K Cascade | 4 | FGFR1, FGFR2, FGFR3, FGFR4 |
| 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 |
| betaKlotho-mediated ligand binding | 1 | FGFR4 |
| Signal Transduction | 1 | LATS1 |
| Signaling by FGFR1 amplification mutants | 1 | FGFR1 |
| Signaling by activated point mutants of FGFR1 | 1 | FGFR1 |
| FGFR4 mutant receptor activation | 1 | FGFR4 |
| Signaling by activated point mutants of FGFR3 | 1 | FGFR3 |
| FGFR4 ligand binding and activation | 1 | FGFR4 |
| FGFR1b ligand binding and activation | 1 | FGFR1 |
| FGFR3b ligand binding and activation | 1 | FGFR3 |
| FGFR3c ligand binding and activation | 1 | FGFR3 |
| FGFR1c ligand binding and activation | 1 | FGFR1 |
| FGFR1c and Klotho ligand binding and activation | 1 | FGFR1 |
| FGFR2c ligand binding and activation | 1 | FGFR2 |
| FGFR2b ligand binding and activation | 1 | FGFR2 |
| Signaling by FGFR2 amplification mutants | 1 | FGFR2 |
| Signaling by Hippo | 1 | LATS1 |
| t(4;14) translocations of FGFR3 | 1 | FGFR3 |
| Activated point mutants of FGFR2 | 1 | FGFR2 |
| Integrin cell surface interactions | 1 | KDR |
| NCAM signaling for neurite out-growth | 1 | FGFR1 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| protein phosphorylation | 10 |
| positive regulation of cell population proliferation | 9 |
| peptidyl-tyrosine phosphorylation | 8 |
| protein autophosphorylation | 8 |
| cell migration | 7 |
| positive regulation of ERK1 and ERK2 cascade | 7 |
| positive regulation of MAPK cascade | 7 |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | 6 |
| angiogenesis | 6 |
| cell surface receptor protein tyrosine kinase signaling pathway | 5 |
| positive regulation of cell migration | 5 |
| lung development | 4 |
| skeletal system morphogenesis | 4 |
| fibroblast growth factor receptor signaling pathway | 4 |
| in utero embryonic development | 3 |
Indications & clinical
Indications
50 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 |
| systemic sclerosis | 3 | MONDO:0005100 | EFO:0000717 |
| idiopathic pulmonary fibrosis | 3 | MONDO:0800504 | EFO:0000768 |
| non-small cell lung carcinoma | 3 | MONDO:0005233 | EFO:0003060 |
| colorectal neoplasm | 3 | MONDO:0005335 | EFO:0004142 |
| interstitial lung disease | 3 | MONDO:0015925 | EFO:0004244 |
| pulmonary fibrosis | 3 | MONDO:0002771 | EFO:0009448 |
| severe acute respiratory syndrome | 3 | MONDO:0005091 | MONDO:0100096 |
| colorectal adenocarcinoma | 3 | MONDO:0005008 | EFO:0000365 |
| renal cell carcinoma | 2 | MONDO:0005086 | EFO:0000681 |
| hepatocellular carcinoma | 2 | MONDO:0007256 | EFO:0000182 |
| acute myeloid leukemia | 2 | MONDO:0018874 | EFO:0000222 |
| small cell lung carcinoma | 2 | MONDO:0008433 | EFO:0000702 |
| cervical adenocarcinoma | 2 | MONDO:0005153 | EFO:0001416 |
| mesothelioma | 2 | MONDO:0005065 | EFO:0000588 |
| sarcoma | 2 | MONDO:0005089 | EFO:0000691 |
| malignant pleural mesothelioma | 2 | MONDO:0005112 | EFO:0000770 |
| gastric adenocarcinoma | 2 | MONDO:0005036 | EFO:0000503 |
| prostate adenocarcinoma | 2 | MONDO:0005082 | EFO:0000673 |
| glioblastoma | 2 | MONDO:0018177 | EFO:0000519 |
| squamous cell lung carcinoma | 2 | MONDO:0005097 | EFO:0000708 |
| anaplastic astrocytoma | 2 | MONDO:0016684 | EFO:0002499 |
| anaplastic oligodendroglioma | 2 | MONDO:0016696 | EFO:0002501 |
| ovarian neoplasm | 2 | MONDO:0021068 | EFO:0003893 |
| upper aerodigestive tract neoplasm | 2 | MONDO:0005398 | EFO:0004284 |
| gliosarcoma | 2 | MONDO:0016681 | EFO:1001465 |
| bronchiolitis obliterans syndrome | 2 | MONDO:0015265 | EFO:0007183 |
| urothelial carcinoma | 2 | MONDO:0040679 | EFO:0008528 |
| carcinoid tumor | 2 | MONDO:0005369 | EFO:0004243 |
| appendiceal neoplasm | 2 | MONDO:0001236 | MONDO:0001235 |
| peritoneal neoplasm | 2 | MONDO:0006901 | MONDO:0002087 |
| fallopian tube neoplasm | 2 | MONDO:0021092 | MONDO:0002158 |
| salivary gland cancer | 2 | MONDO:0004669 | MONDO:0004669 |
| breast neoplasm | 2 | MONDO:0021100 | MONDO:0007254 |
| ovarian cancer | 2 | MONDO:0008170 | MONDO:0008170 |
| lung neoplasm | 2 | MONDO:0021117 | MONDO:0008903 |
| endometrium neoplasm | 2 | MONDO:0021251 | MONDO:0011962 |
| lymphangioleiomyomatosis | 2 | MONDO:0011705 | MONDO:0011705 |
| hereditary hemorrhagic telangiectasia | 2 | MONDO:0019180 | MONDO:0019180 |
| neuroendocrine neoplasm | 2 | MONDO:0019496 | EFO:1001901 |
| plasma cell myeloma | 1 | MONDO:0009693 | EFO:0001378 |
| exocrine pancreatic carcinoma | 1 | MONDO:0005192 | EFO:0002618 |
| cutaneous melanoma | 1 | MONDO:0005012 | EFO:0000389 |
| female reproductive organ cancer | 1 | MONDO:0001416 | EFO:1001331 |
| lung adenocarcinoma | 1 | MONDO:0005061 | EFO:0000571 |
| colon adenocarcinoma | 1 | MONDO:0002271 | EFO:1001949 |
| rectal neoplasm | 1 | MONDO:0002165 | MONDO:0044937 |
| colonic neoplasm | 1 | MONDO:0005401 | MONDO:0021063 |
2 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 157.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE2 | 48 |
| PHASE1 | 45 |
| Not specified | 24 |
| PHASE3 | 21 |
| PHASE4 | 11 |
| PHASE1/PHASE2 | 7 |
| PHASE2/PHASE3 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT06479603 | PHASE4 | RECRUITING | RCT of Nintedanib in Fibrotic Sarcoidosis |
| NCT07485920 | PHASE4 | NOT_YET_RECRUITING | A Prospective, Multicenter Exploratory Clinical Study on Consolidation Therapy With Tislelizumab Combined With Nintedanib for Limited-stage Small Cell Lung Cancer |
| NCT02579603 | PHASE4 | COMPLETED | Safety, Tolerability and PK of Nintedanib in Combination With Pirfenidone in IPF |
| NCT02598193 | PHASE4 | COMPLETED | Safety and Tolerability Study of Pirfenidone in Combination With Nintedanib in Participants With Idiopathic Pulmonary Fibrosis (IPF) |
| NCT02606877 | PHASE4 | COMPLETED | A Study to Compare the Amount of Nintedanib and Pirfenidone in the Blood When Nintedanib and Pirfenidone Are Given Separately or in Combination |
| NCT02788474 | PHASE4 | COMPLETED | Effect of Nintedanib on Biomarkers of Extracellular Matrix Turnover in Patients With Idiopathic Pulmonary Fibrosis and Limited Forced Vital Capacity Impairment |
| NCT03717012 | PHASE4 | TERMINATED | Study of Pulmonary Rehabilitation in Patients With Idiopathic Pulmonary Fibrosis (IPF) |
| NCT03939520 | PHASE4 | COMPLETED | Management of Progressive Disease in Idiopathic Pulmonary Fibrosis |
| NCT04619680 | PHASE4 | COMPLETED | The Study of the Use of Nintedanib in Slowing Lung Disease in Patients With Fibrotic or Non-Fibrotic Interstitial Lung Disease Related to COVID-19 |
| NCT04856111 | PHASE4 | UNKNOWN | Pirfenidone vs. Nintedanib for Fibrotic Lung Disease After Coronavirus Disease-19 Pneumonia |
| NCT05799755 | PHASE4 | COMPLETED | Myositis Interstitial Lung Disease Nintedanib Trial |
| NCT06297096 | PHASE3 | RECRUITING | Study of the Efficacy of Nintedanib+Tocilizumab in Patients With Systemic Sclerosis and Interstitial Lung Disease |
| NCT07162961 | PHASE3 | NOT_YET_RECRUITING | Nintedanib for Improving Reproductive Outcomes in Adenomyosis |
| NCT07335562 | PHASE3 | RECRUITING | A Study to Compare the Efficacy and Safety of BMS-986353 (Zolacabtagene- Autoleucel / Zola-cel), CD19-CAR T Cells, Versus Standard of Care in Participants With Active Systemic Sclerosis |
| NCT00806819 | PHASE3 | COMPLETED | Lume Lung 2 : BIBF 1120 Plus Pemetrexed Compared to Placebo Plus Pemetrexed in 2nd Line Nonsquamous NSCLC |
| NCT01015118 | PHASE3 | COMPLETED | LUME-Ovar 1: Nintedanib (BIBF 1120) or Placebo in Combination With Paclitaxel and Carboplatin in First Line Treatment of Ovarian Cancer |
| NCT01335464 | PHASE3 | COMPLETED | Safety and Efficacy of BIBF 1120 at High Dose in Idiopathic Pulmonary Fibrosis Patients |
| NCT01335477 | PHASE3 | COMPLETED | Safety and Efficacy of BIBF 1120 at High Dose in Idiopathic Pulmonary Fibrosis Patients II |
| NCT01619085 | PHASE3 | COMPLETED | Extension Trial of the Long Term Safety of BIBF 1120 in Patients With Idiopathic Pulmonary Fibrosis |
| NCT01907100 | PHASE2/PHASE3 | TERMINATED | Nintedanib (BIBF 1120) in Mesothelioma |
| NCT01979952 | PHASE3 | COMPLETED | Nintedanib Twice Daily vs Placebo in Patients Diagnosed With Idiopathic Pulmonary Fibrosis (IPF) |
| NCT02149108 | PHASE3 | COMPLETED | Nintedanib (BIBF 1120) vs Placebo in Refractory Metastatic Colorectal Cancer (LUME-Colon 1) |
| NCT02231164 | PHASE3 | TERMINATED | LUME-Columbus: Nintedanib Plus Docetaxel in Advanced Non-small Cell Lung Cancer With Translational Research |
| NCT02597933 | PHASE3 | COMPLETED | A Trial to Compare Nintedanib With Placebo for Patients With Scleroderma Related Lung Fibrosis |
| NCT02802345 | PHASE3 | COMPLETED | Efficacy and Safety of Nintedanib Co-administered With Sildenafil in Idiopathic Pulmonary Fibrosis Patients With Advanced Lung Function Impairment |
| NCT02999178 | PHASE3 | COMPLETED | Efficacy and Safety of Nintedanib in Patients With Progressive Fibrosing Interstitial Lung Disease (PF-ILD) |
| NCT03283007 | PHASE3 | COMPLETED | Nintedanib in Lung Transplant Recipients With Bronchiolitis Obliterans Syndrome Grade 0p-1-2 |
| NCT03313180 | PHASE3 | COMPLETED | A Trial to Evaluate the Safety of Long Term Treatment With Nintedanib in Patients With Scleroderma Related Lung Fibrosis |
| NCT03820726 | PHASE3 | COMPLETED | A Follow-up Study Investigating Long Term Treatment With Nintedanib in Patients With Progressive Fibrosing Interstitial Lung Disease (PF-ILD) |
| NCT04093024 | PHASE3 | COMPLETED | A Study to Find Out How Nintedanib is Taken up in the Body and How Well it is Tolerated in Children and Adolescents With Interstitial Lung Disease (ILD) |
| NCT05065190 | PHASE3 | COMPLETED | A Study to Test How Well a Medicine Called Nintedanib Helps People in China With Progressive Lung Fibrosis |
| NCT05067517 | PHASE3 | WITHDRAWN | Efficacy & Safety of Nintedanib in Patients With Progressive Fibrosing Coal Mine Dust-Induced Interstitial Lung Disease |
| NCT05285982 | PHASE3 | COMPLETED | A Study to Evaluate Long-term Safety of Nintedanib in Children and Adolescents With Interstitial Lung Disease (InPedILD®-ON) |
| NCT03377023 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | Phase I/II Study of Nivolumab and Ipilimumab Combined With Nintedanib in Non Small Cell Lung Cancer |
| NCT03805477 | PHASE2 | RECRUITING | Nintedanib in Patients With Bronchiolitis Obliterans Syndrome Following Hematopoietic Stem Cell Transplantation |
| NCT04976036 | PHASE2 | RECRUITING | Efficacy of Nintedanib for Treatment of Epistaxis in Hereditary Hemorrhagic Telangiectasia (HHT) Patients |
| NCT06071013 | PHASE1/PHASE2 | RECRUITING | Nintedanib Plus EGFR TKI In EGFR-mutated Non-small Cell Lung Cancer Patients |
| NCT06643091 | PHASE2 | NOT_YET_RECRUITING | Nintedanib Treatment in Unicentric Castleman Disease |
| NCT07583589 | PHASE2 | NOT_YET_RECRUITING | Nintedanib With or Without Dextromethorphan in Patients With Idiopathic Pulmonary Fibrosis (IPF) |
| NCT00706628 | PHASE2 | COMPLETED | A Multi-centre 3-arm Randomised Phase II Trial of BIBF 1120 Versus BIBW 2992 Versus Sequential Administration of BIBF 1120 and BIBW 2992 in Patients With Hormone-resistant Prostate Cancer |
Clinical evidence (CIViC)
Variant × indication × effect (1 predictive associations from 1 curated evidence items):
| Variant | Indication | Effect | Therapy | Level | CIViC |
|---|---|---|---|---|---|
| CCDC6::RET Fusion | Lung Non-small Cell Carcinoma | Sensitivity/Response | Nintedanib | CIViC C | EID1601 |
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.
245 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| Crizotinib | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| Fedratinib | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| Lenvatinib | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| Pazopanib | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| SUNITINIB | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| Vandetanib | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| DOVITINIB | ChEMBL | Phase 3 | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| LESTAURTINIB | ChEMBL | Phase 3 | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| LINIFANIB | ChEMBL | Phase 3 | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| SU-014813 | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| TOZASERTIB | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| Afatinib | PubChem | Approved | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| Selumetinib | PubChem | Approved | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| Axitinib | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| Gefitinib | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, LATS1, PDGFRA |
| MIDOSTAURIN | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| Ponatinib | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, KDR, LATS1, PDGFRA, PDGFRB |
| Sorafenib | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| BRIVANIB | ChEMBL | Phase 3 | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| CEDIRANIB | ChEMBL | Phase 3 | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| SEMAXANIB | ChEMBL | Phase 3 | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| OSI-632 | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| R-406 | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| TANDUTINIB | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| Idelalisib | PubChem | Approved | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, LATS1, PDGFRA, PDGFRB |
| INFIGRATINIB | ChEMBL | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, PDGFRA |
| AT-9283 | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR3, FLT1, FLT4, KDR, LATS1, PDGFRA |
| DORAMAPIMOD | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR4, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| FORETINIB | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR3, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| REBASTINIB | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR3, FGFR4, FLT1, FLT4, KDR, PDGFRA |
| Erlotinib | ChEMBL + PubChem | Phase 4 (approved) | FGFR2, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| REGORAFENIB | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| Tivozanib | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| DASATINIB | ChEMBL | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FLT1, KDR, PDGFRA, PDGFRB |
| MOTESANIB | ChEMBL | Phase 3 | FGFR1, FGFR4, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| CENISERTIB | ChEMBL | Phase 2 | FGFR1, FGFR3, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| ILORASERTIB | ChEMBL | Phase 2 | FGFR1, FGFR3, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| LUCITANIB | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR3, FLT1, FLT4, KDR, PDGFRB |
| MK-2461 | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR3, FLT1, FLT4, KDR, PDGFRB |
| Ceritinib | ChEMBL + PubChem | Phase 4 (approved) | FGFR2, FGFR3, FGFR4, KDR, LATS1, PDGFRA |
| Entrectinib | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FGFR3, FLT1, FLT4, KDR, LATS1 |
| Quizartinib | ChEMBL + PubChem | Phase 4 (approved) | FLT1, FLT4, KDR, LATS1, PDGFRA, PDGFRB |
| BRIGATINIB | ChEMBL | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4, FLT4, KDR |
| RAF-265 | ChEMBL | Phase 2 | FGFR1, FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| Cabozantinib | ChEMBL + PubChem | Phase 4 (approved) | FGFR1, FLT1, FLT4, KDR, LATS1 |
| Pexidartinib | ChEMBL + PubChem | Phase 4 (approved) | FLT1, KDR, LATS1, PDGFRA, PDGFRB |
| ERDAFITINIB | ChEMBL | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4, KDR |
| FUTIBATINIB | ChEMBL | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4, KDR |
| ORANTINIB | ChEMBL | Phase 3 | FGFR1, FLT1, KDR, LATS1, PDGFRB |
| VATALANIB | ChEMBL | Phase 3 | FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| CEP-11981 | ChEMBL | Phase 2 | FGFR1, FGFR3, FLT1, KDR, PDGFRA |
| DEFOSBARASERTIB | ChEMBL | Phase 2 | FLT1, FLT4, KDR, PDGFRA, PDGFRB |
| FEXAGRATINIB | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR3, FGFR4, KDR |
| FGFR INHIBITOR DEBIO 1347 | ChEMBL | Phase 2 | FGFR1, FGFR2, FGFR3, FGFR4, KDR |
| Imatinib | ChEMBL + PubChem | Phase 4 (approved) | KDR, LATS1, PDGFRA, PDGFRB |
| PEMIGATINIB | ChEMBL | Phase 4 (approved) | FGFR1, FGFR2, FGFR3, FGFR4 |
| ALISERTIB | ChEMBL | Phase 3 | FGFR1, FGFR3, FLT1, KDR |
| CANERTINIB | ChEMBL | Phase 3 | FLT1, KDR, PDGFRA, PDGFRB |
| SURUFATINIB | ChEMBL | Phase 3 | FGFR1, FLT1, FLT4, KDR |
| BFH-772 | ChEMBL | Phase 2 | FLT1, FLT4, KDR, PDGFRB |
Related Atlas pages
- Genes: LATS1, PDGFRA, PDGFRB, FGFR1, FGFR2, FGFR3, FGFR4, FLT1, KDR, FLT4
- Diseases: neoplasm, systemic sclerosis, idiopathic pulmonary fibrosis, non-small cell lung carcinoma, colorectal neoplasm, interstitial lung disease, pulmonary fibrosis, severe acute respiratory syndrome, colorectal adenocarcinoma
- Drugs: Crizotinib, Fedratinib, Lenvatinib, Pazopanib, Sunitinib, Vandetanib, Dovitinib, Lestaurtinib, Linifanib, Afatinib, Selumetinib, Axitinib, Gefitinib, Midostaurin, Ponatinib, Sorafenib, Brivanib, Cediranib, Semaxanib, Idelalisib, Infigratinib, Erlotinib, Regorafenib, Tivozanib, Dasatinib, Motesanib, Ceritinib, Entrectinib, Quizartinib, Brigatinib, Cabozantinib, Pexidartinib, Erdafitinib, Futibatinib, Orantinib, Vatalanib, Imatinib, Pemigatinib, Alisertib, Canertinib, Surufatinib