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Erdafitinib

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Also known as BalversaJnj-42756493Erdafitinib (JNJ-42756493)Erdafitnib

Summary

Erdafitinib (CHEMBL3545376) is an approved small molecule (ATC L01EN01) targeting FGFR1, FGFR2, and FGFR3; indicated across 16 conditions including neoplasm and urothelial carcinoma; with CIViC clinical evidence for 33 variant-indication associations (e.g. FGFR3::v Fusion in transitional cell carcinoma).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01EN01
  • Targets: 5 (FGFR1, FGFR2, FGFR3…)
  • Indications: 16 conditions
  • Clinical trials: 35
  • Precision-oncology evidence (CIViC): 33 variant–indication associations
  • Chemistry: 446.5 Da · C25H30N6O2

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL3545376
NameErdafitinib
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID67462786
ATCL01EN01
Molecular formulaC25H30N6O2
Molecular weight446.5
InChIKeyOLAHOMJCDNXHFI-UHFFFAOYSA-N

SMILES: CC(C)NCCN(C1=CC2=NC(=CN=C2C=C1)C3=CN(N=C3)C)C4=CC(=CC(=C4)OC)OC

IUPAC name: N’-(3,5-dimethoxyphenyl)-N’-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-N-propan-2-ylethane-1,2-diamine

Also known as: Balversa, Erdafitinib, Jnj-42756493, JNJ-42756493, ERDAFITINIB, Erdafitinib (JNJ-42756493), erdafitinib, ErdafItinib, Erdafitnib

Parent form; salt/anhydrous children: CHEMBL3918638, CHEMBL3919709, CHEMBL3948043, CHEMBL3975791

Patent coverage: 1,173 distinct patent families (2,794 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 2,665 (95%) 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).

GeneTargetActionpAffinityCancer dependencyUniProt
FGFR1fibroblast growth factor receptor 1Inhibition8.9411.5%P11362
FGFR2fibroblast growth factor receptor 2Inhibition8.641.7%P21802
FGFR3fibroblast growth factor receptor 3Inhibition8.520.5%P22607
FGFR4fibroblast growth factor receptor 4Inhibition8.250.7%P22455
KDRkinase insert domain receptorInhibition7.441.1%P35968

Broader ChEMBL bioactivity targets: 17 (assay-derived). Sample: 5-hydroxytryptamine receptor 2B, Alpha-2C adrenergic receptor, Muscarinic acetylcholine receptor M1, Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, D(3) dopamine receptor, Delta-type opioid receptor, Sodium-dependent dopamine transporter, Adenosine receptor A3, Fibroblast growth factor receptor 3, Vascular endothelial growth factor receptor 2, 3’,5’-cyclic-AMP phosphodiesterase 4D, Vascular endothelial growth factor receptor 2, Fibroblast growth factor receptor 1, Fibroblast growth factor receptor 4, Fibroblast growth factor receptor 2, TEL/KDR.

Bioactivity

ChEMBL activities: 80 potent at pChembl ≥ 5 of 85 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
FGFR210.27IC500.05nMCHEMBL_ACT_29151885
FGFR310.18IC500.07nMCHEMBL_ACT_29152172
P3591810IC500.1nMCHEMBL_ACT_19130930
FGFR29.96IC500.11nMCHEMBL_ACT_29152142
FGFR29.72IC500.19nMCHEMBL_ACT_29152154
FGFR29.7IC500.2nMCHEMBL_ACT_29057018
FGFR19.6IC500.25nMCHEMBL_ACT_26010488
FGFR39.51IC500.31nMCHEMBL_ACT_29152196
FGFR39.38IC500.42nMCHEMBL_ACT_24873120
FGFR39.38IC500.42nMCHEMBL_ACT_26010490
FGFR29.38IC500.42nMCHEMBL_ACT_29152160
FGFR19.3IC500.5nMCHEMBL_ACT_29140675
FGFR39.15IC500.7nMCHEMBL_ACT_29140688
FGFR39.11IC500.77nMCHEMBL_ACT_29152190
FGFR29.1IC500.8nMCHEMBL_ACT_29140682
FGFR18.92IC501.2nMCHEMBL_ACT_19245634
FGFR18.92IC501.2nMCHEMBL_ACT_23284804
FGFR18.92IC501.2nMCHEMBL_ACT_24661111
FGFR18.92IC501.2nMCHEMBL_ACT_26025570
FGFR18.92IC501.2nMCHEMBL_ACT_29057057
FGFR18.92IC501.2nMCHEMBL_ACT_29064066
FGFR18.92IC501.2nMCHEMBL_ACT_29152317
FGFR28.82IC501.5nMCHEMBL_ACT_24873116
FGFR28.82IC501.5nMCHEMBL_ACT_26010489
FGFR18.81IC501.53nMCHEMBL_ACT_24805349
FGFR38.79IC501.62nMCHEMBL_ACT_24805367
FGFR18.73IC501.86nMCHEMBL_ACT_16871515
FGFR48.7IC502nMCHEMBL_ACT_24873124
FGFR48.7IC502nMCHEMBL_ACT_26010491
FGFR48.62IC502.4nMCHEMBL_ACT_29140694
FGFR28.6IC502.5nMCHEMBL_ACT_19245633
FGFR28.6IC502.5nMCHEMBL_ACT_23284808
FGFR28.6IC502.5nMCHEMBL_ACT_24661118
FGFR38.6IC502.5nMCHEMBL_ACT_24805468
FGFR28.6IC502.5nMCHEMBL_ACT_26025563
FGFR28.6IC502.5nMCHEMBL_ACT_29057058
FGFR28.6IC502.5nMCHEMBL_ACT_29064067
FGFR28.6IC502.5nMCHEMBL_ACT_29152325
FGFR38.52IC503nMCHEMBL_ACT_19130922
FGFR38.52IC503nMCHEMBL_ACT_19245632
FGFR38.52IC503nMCHEMBL_ACT_20711793
FGFR38.52IC503nMCHEMBL_ACT_23284812
FGFR38.52IC503nMCHEMBL_ACT_24661115
FGFR38.52IC503nMCHEMBL_ACT_25034770
FGFR38.52IC503nMCHEMBL_ACT_26025576
FGFR38.52IC503nMCHEMBL_ACT_29057059
FGFR38.52IC503nMCHEMBL_ACT_29064068
FGFR38.52IC503nMCHEMBL_ACT_29152333
FGFR38.42IC503.8nMCHEMBL_ACT_16872757
FGFR48.42IC503.8nMCHEMBL_ACT_22850384
FGFR28.35IC504.47nMCHEMBL_ACT_16872136
FGFR28.28IC505.28nMCHEMBL_ACT_24805444
FGFR48.24IC505.7nMCHEMBL_ACT_19245631
FGFR48.24IC505.7nMCHEMBL_ACT_23284816
FGFR48.24IC505.7nMCHEMBL_ACT_24661076
FGFR48.24IC505.7nMCHEMBL_ACT_26025582
FGFR48.24IC505.7nMCHEMBL_ACT_29057060
FGFR48.24IC505.7nMCHEMBL_ACT_29064069
FGFR48.24IC505.7nMCHEMBL_ACT_29152341
FGFR48.18IC506.61nMCHEMBL_ACT_16873382
FGFR28.07IC508.5nMCHEMBL_ACT_29152136
FGFR38IC509.9nMCHEMBL_ACT_29152178
FGFR37.8IC5015.85nMCHEMBL_ACT_16867462
FGFR47.73IC5018.7nMCHEMBL_ACT_24805394
KDR7.43IC5037nMCHEMBL_ACT_19130927
KDR7.43IC5036.8nMCHEMBL_ACT_19245643
KDR7.43IC5036.8nMCHEMBL_ACT_20711816
KDR7.32IC5047.86nMCHEMBL_ACT_16874008
FGFR37.25IC5056nMCHEMBL_ACT_29152184
FGFR17.08IC5083.18nMCHEMBL_ACT_16874630
FGFR36.95IC50112.6nMCHEMBL_ACT_24805427
KDR6.2IC50627nMCHEMBL_ACT_26033298
FGFR26.07IC50850.7nMCHEMBL_ACT_24805410
FGFR15.78IC501658nMCHEMBL_ACT_24805403
SLC6A45.64AC502300nMCHEMBL_ACT_25150894
KDR5.48IC503311nMCHEMBL_ACT_16868730
HTR2B5.39AC504100nMCHEMBL_ACT_25228072
PDE4D5.22AC506000nMCHEMBL_ACT_25185912
SLC6A35.11AC507800nMCHEMBL_ACT_25124521
SLC6A25.06AC508700nMCHEMBL_ACT_25145565

Target pathways

Aggregated over 5 target gene(s): FGFR1, FGFR2, FGFR3, FGFR4, KDR.

Top Reactome pathways

62 total, by targets touching each:

PathwayTargetsGenes
PI3K Cascade4FGFR1, FGFR2, FGFR3, FGFR4
PIP3 activates AKT signaling4FGFR1, FGFR2, FGFR3, FGFR4
Constitutive Signaling by Aberrant PI3K in Cancer4FGFR1, FGFR2, FGFR3, FGFR4
RAF/MAP kinase cascade4FGFR1, FGFR2, FGFR3, FGFR4
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling4FGFR1, FGFR2, FGFR3, FGFR4
betaKlotho-mediated ligand binding1FGFR4
Signaling by FGFR1 amplification mutants1FGFR1
Signaling by activated point mutants of FGFR11FGFR1
FGFR4 mutant receptor activation1FGFR4
Signaling by activated point mutants of FGFR31FGFR3
FGFR4 ligand binding and activation1FGFR4
FGFR1b ligand binding and activation1FGFR1
FGFR3b ligand binding and activation1FGFR3
FGFR3c ligand binding and activation1FGFR3
FGFR1c ligand binding and activation1FGFR1
FGFR1c and Klotho ligand binding and activation1FGFR1
FGFR2c ligand binding and activation1FGFR2
FGFR2b ligand binding and activation1FGFR2
Neuropilin interactions with VEGF and VEGFR1KDR
VEGF binds to VEGFR leading to receptor dimerization1KDR
Signaling by FGFR2 amplification mutants1FGFR2
t(4;14) translocations of FGFR31FGFR3
Activated point mutants of FGFR21FGFR2
Integrin cell surface interactions1KDR
NCAM signaling for neurite out-growth1FGFR1
VEGFA-VEGFR2 Pathway1KDR
Signal transduction by L11FGFR1
VEGFR2 mediated cell proliferation1KDR
Phospholipase C-mediated cascade: FGFR11FGFR1
Phospholipase C-mediated cascade; FGFR21FGFR2
Phospholipase C-mediated cascade; FGFR31FGFR3
Phospholipase C-mediated cascade; FGFR41FGFR4
Downstream signaling of activated FGFR11FGFR1
SHC-mediated cascade:FGFR11FGFR1
PI-3K cascade:FGFR11FGFR1
FRS-mediated FGFR1 signaling1FGFR1
PI-3K cascade:FGFR21FGFR2
SHC-mediated cascade:FGFR21FGFR2
FRS-mediated FGFR2 signaling1FGFR2
SHC-mediated cascade:FGFR31FGFR3
FRS-mediated FGFR3 signaling1FGFR3
PI-3K cascade:FGFR31FGFR3
FRS-mediated FGFR4 signaling1FGFR4
SHC-mediated cascade:FGFR41FGFR4
PI-3K cascade:FGFR41FGFR4
Negative regulation of FGFR1 signaling1FGFR1
Negative regulation of FGFR2 signaling1FGFR2
Negative regulation of FGFR3 signaling1FGFR3
Negative regulation of FGFR4 signaling1FGFR4
Signaling by FGFR2 in disease1FGFR2

Dominant GO biological processes

GO termTargets
protein phosphorylation5
positive regulation of cell population proliferation5
positive regulation of MAPK cascade5
fibroblast growth factor receptor signaling pathway4
peptidyl-tyrosine phosphorylation4
protein autophosphorylation4
positive regulation of ERK1 and ERK2 cascade4
angiogenesis3
positive regulation of mesenchymal cell proliferation3
positive regulation of phospholipase activity3
cell migration3
skeletal system morphogenesis3
positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction3
positive regulation of cell communication3
positive regulation of signaling3

Indications & clinical

Indications

3 approved indications. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

IndicationPhaseMONDOEFO
neoplasm4MONDO:0005070EFO:0000616
urothelial carcinoma4MONDO:0040679EFO:0008528
urinary bladder neoplasm4MONDO:0004987EFO:0000294

10 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)PhaseMONDOEFO
plasma cell myeloma2MONDO:0009693EFO:0001378
squamous cell lung carcinoma2MONDO:0005097EFO:0000708
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
metastatic prostate carcinoma2MONDO:0004956EFO:0000196
prostate adenocarcinoma2MONDO:0005082EFO:0000673
prostate carcinoma2MONDO:0005159EFO:0001663
hepatocellular carcinoma1MONDO:0007256EFO:0000182
lymphoma1MONDO:0005062EFO:0000574
liver disorder1MONDO:0005154EFO:0001421
breast neoplasm1MONDO:0021100MONDO:0007254

3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 35.

Phase distribution

PhaseTrials
PHASE218
PHASE19
PHASE1/PHASE23
Not specified3
PHASE31
EARLY_PHASE11

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03390504PHASE3ACTIVE_NOT_RECRUITINGA Study of Erdafitinib Compared With Vinflunine or Docetaxel or Pembrolizumab in Participants With Advanced Urothelial Cancer and Selected Fibroblast Growth Factor Receptor (FGFR) Gene Aberrations
NCT02365597PHASE2ACTIVE_NOT_RECRUITINGAn Efficacy and Safety Study of Erdafitinib (JNJ-42756493) in Participants With Urothelial Cancer
NCT02465060PHASE2ACTIVE_NOT_RECRUITINGTargeted Therapy Directed by Genetic Testing in Treating Patients With Advanced Refractory Solid Tumors, Lymphomas, or Multiple Myeloma (The MATCH Screening Trial)
NCT02925234PHASE2RECRUITINGThe Drug Rediscovery Protocol (DRUP Trial)
NCT03155620PHASE2ACTIVE_NOT_RECRUITINGTargeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphomas, or Histiocytic Disorders (The Pediatric MATCH Screening Trial)
NCT03210714PHASE2ACTIVE_NOT_RECRUITINGErdafitinib in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With FGFR Mutations (A Pediatric MATCH Treatment Trial)
NCT03473743PHASE1/PHASE2ACTIVE_NOT_RECRUITINGA Study of Erdafitinib in Participants With Metastatic or Locally Advanced Urothelial Cancer
NCT04917809PHASE2ACTIVE_NOT_RECRUITINGA Study of Oral Erdafitinib in People With Recurrent Non-Invasive Bladder Cancer
NCT05859334PHASE2RECRUITINGTesting the Anti-cancer Drug Erdafitinib for Brain Cancers That Have Returned or Progressed Following Treatment
NCT06308822PHASE2ACTIVE_NOT_RECRUITINGTesting JNJ-42756493 (Erdafitinib) as Potentially Targeting Treatment in Cancers With FGFR Amplifications (MATCH-Subprotocol K1)
NCT06351371PHASE2ACTIVE_NOT_RECRUITINGTesting JNJ-42756493 (Erdafitinib) as Potentially Targeting Treatment in Cancers With FGFR Mutations or Fusions (MATCH - Subprotocol K2)
NCT06511648PHASE2RECRUITINGErdafitinib Monotherapy or in Combination With Cetrelimab in Muscle-invasive Bladder Cancer Patients With Fibroblast Growth Factor Receptor (FGFR ) Gene Alterations
NCT02421185PHASE1/PHASE2COMPLETEDStudy to Evaluate the Safety, Pharmacokinetics, and Pharmacodynamics of JNJ-42756493 (Erdafitinib) in Participants With Advanced Hepatocellular Carcinoma
NCT02699606PHASE2COMPLETEDA Study to Evaluate the Clinical Efficacy of JNJ-42756493 (Erdafitinib), A Pan-Fibroblast Growth Factor Receptor (FGFR) Tyrosine Kinase Inhibitor, In Asian Participants With Advanced Non-Small-Cell Lung Cancer, Urothelial Cancer, Esophageal Cancer Or Cholangiocarcinoma
NCT02952573PHASE2TERMINATEDTesting JNJ-42756493 In Combination With Dexamethasone in Multiple Myeloma That Came Back After a Period of Improvement
NCT03732703PHASE1/PHASE2COMPLETEDMyeloma-Developing Regimens Using Genomics (MyDRUG)
NCT03827850PHASE2TERMINATEDFGFR Inhibitor in FGFR Dysregulated Cancer
NCT03999515PHASE2TERMINATEDErdafitinib and Abiraterone Acetate or Enzalutamide in Treating Patients With Double Negative Prostate Cancer
NCT04083976PHASE2COMPLETEDA Study of Erdafitinib in Participants With Advanced Solid Tumors and Fibroblast Growth Factor Receptor (FGFR) Gene Alterations
NCT04172675PHASE2COMPLETEDA Study of Erdafitinib Versus Investigator Choice of Intravesical Chemotherapy in Participants Who Received Bacillus Calmette-Guérin (BCG) and Recurred With High Risk Non-Muscle-Invasive Bladder Cancer (NMIBC)
NCT04754425PHASE2TERMINATEDErdafitinib for the Treatment of Patients With Castration-Resistant Prostate Cancer
NCT05564416PHASE2WITHDRAWNTesting Anti-Cancer Drugs Erdafitinib With or Without Atezolizumab in Patients With Localized Bladder Cancer Not Able to Receive Cisplatin Chemotherapy, NERA Trial
NCT04963153PHASE1ACTIVE_NOT_RECRUITINGTesting Combination Erdafitinib and Enfortumab Vedotin in Metastatic Bladder Cancer After Treatment With Chemotherapy and Immunotherapy
NCT02231489PHASE1COMPLETEDStudy to Assess the Relative Bioavailability of Orally Administered JNJ-42756493 Tablet Versus JNJ-42756493 Capsule in Healthy Participants
NCT02692677PHASE1COMPLETEDA Study to Assess the Absorption, Metabolism, and Routes of Excretion Following Oral Administration of (14C) Radiolabeled JNJ–42756493 to Healthy Male Participants
NCT03066687PHASE1COMPLETEDA Study to Determine the Effect of Food on the Pharmacokinetics of Erdafitinib in Healthy Participants
NCT03135106PHASE1COMPLETEDA Study to Evaluate the Effect of Fluconazole and Itraconazole on Erdafitinib Pharmacokinetics in Healthy Adult Participants
NCT03238196PHASE1COMPLETEDFulvestrant, Palbociclib and Erdafitinib in ER+/HER2-/FGFR-amplified Metastatic Breast Cancer
NCT03547037PHASE1COMPLETEDA Study to Evaluate the Safety, Pharmacokinetics, Pharmacodynamics, and Immunogenicity of JNJ-63723283, an Anti-Programmed Cell Death (PD)-1 Monoclonal Antibody, as Monotherapy or in Combination With Erdafitinib in Japanese Participants With Advanced Solid Cancers
NCT03587363PHASE1TERMINATEDA Study to Evaluate the Effect of Hepatic Impairment on the Pharmacokinetics of Erdafitinib
NCT04330248PHASE1COMPLETEDA Study of Steady-state Carbamazepine on the Single-dose of Erdafitinib Tablets in Healthy Adult Participants
NCT06204614EARLY_PHASE1ENROLLING_BY_INVITATIONDrug Screening Using IMD in Bladder Cancer
NCT03825484Not specifiedAPPROVED_FOR_MARKETINGExpanded Access Program (EAP) for Participants With Advanced Cancers and Fibroblast Growth Factor Receptor (FGFR) Genetic Alterations Who Have Exhausted All Treatment Options
NCT05052372Not specifiedTERMINATEDBiomarker Research Study for Patients With FGFR-Mutant Bladder Cancer Receiving Erdafitinib
NCT06328491Not specifiedCOMPLETEDErdafitinib in Metastatic Steroid-cell Ovarian Cancer

Clinical evidence (CIViC)

Variant × indication × effect (33 predictive associations from 36 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
FGFR3::v FusionTransitional Cell CarcinomaSensitivity/ResponseErdafitinibCIViC AEID7262 +1
FGFR2 Mutation OR FGFR2::v Fusion OR FGFR2::? FusionTransitional Cell CarcinomaSensitivity/ResponseErdafitinibCIViC AEID7261
FGFR2::v FusionBladder CarcinomaSensitivity/ResponseErdafitinibCIViC AEID11257
FGFR2::v FusionTransitional Cell CarcinomaSensitivity/ResponseErdafitinibCIViC AEID7423
FGFR3 G370CTransitional Cell CarcinomaSensitivity/ResponseErdafitinibCIViC AEID7307
FGFR3 MutationTransitional Cell CarcinomaSensitivity/ResponseErdafitinibCIViC AEID7422
FGFR3 R248CTransitional Cell CarcinomaSensitivity/ResponseErdafitinibCIViC AEID7305
FGFR3 S249CTransitional Cell CarcinomaSensitivity/ResponseErdafitinibCIViC AEID7306
FGFR3 Y373CTransitional Cell CarcinomaSensitivity/ResponseErdafitinibCIViC AEID7308
FGFR3::v FusionBladder CarcinomaSensitivity/ResponseErdafitinibCIViC AEID11258
FGFR3 S249CUrothelial CarcinomaSensitivity/ResponseErdafitinibCIViC BEID12953 +1
FGFR1 AmplificationBreast CancerSensitivity/ResponseErdafitinibCIViC BEID12469
FGFR1 Amplification OR FGFR2 Amplification OR FGFR3 Amplification OR FGFR4 AmplificationCancerSensitivity/ResponseErdafitinibCIViC BEID12024
FGFR2::? FusionCholangiocarcinomaSensitivity/ResponseErdafitinibCIViC BEID10406
FGFR2::v FusionCancerSensitivity/ResponseErdafitinibCIViC BEID1918
FGFR3 MutationBladder Urothelial CarcinomaSensitivity/ResponseErdafitinibCIViC BEID10397
FGFR3::TACC3 FusionCancerSensitivity/ResponseErdafitinibCIViC BEID1919
FGFR1 AmplificationBreast CancerPalbociclib + Erdafitinib + FulvestrantCIViC BEID12485
FGFR2 MutationCholangiocarcinomaSensitivity/ResponseErdafitinibCIViC CEID10375 +1
FGFR2::? FusionBladder Urothelial CarcinomaSensitivity/ResponseErdafitinibCIViC CEID10404
FGFR2::BICC1 FusionTransitional Cell CarcinomaSensitivity/ResponseErdafitinibCIViC CEID1917
FGFR2::BICC1 FusionEndometrial CancerSensitivity/ResponseErdafitinibCIViC CEID1920
FGFR3 G802_X807del AND IGHA1::FGFR3 FusionMultiple MyelomaSensitivity/ResponseErdafitinibCIViC CEID11033
FGFR3::TACC3 Fusion AND FGFR2::CCDC6 FusionAdrenal CarcinomaSensitivity/ResponseErdafitinibCIViC CEID4861
FGFR3::v FusionBladder Urothelial CarcinomaSensitivity/ResponseErdafitinibCIViC CEID10405
FGFR3 Y373C AND FGFR3 N540KUrothelial CarcinomaResistanceErdafitinib + FutibatinibCIViC CEID12704
PIK3CA E545K AND FGFR3 S249C AND FGFR3 N540KUrothelial CarcinomaResistanceErdafitinibCIViC CEID12703
FGFR1 AmplificationLung CancerSensitivity/ResponseErdafitinibCIViC DEID7954
FGFR2 AmplificationStomach CancerSensitivity/ResponseErdafitinibCIViC DEID7953
FGFR2 OverexpressionColorectal CancerSensitivity/ResponseErdafitinibCIViC DEID7832

+3 more predictive associations (showing top 30 by level).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

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.

190 molecules share ≥1 primary target. Top 100 by shared-target count:

MoleculeSourceStatusShared targets
CrizotinibChEMBL + PubChemPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
GefitinibChEMBL + PubChemPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
PAZOPANIBChEMBL + PubChemPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
BRIGATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
FEDRATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
FUTIBATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
INFIGRATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
LENVATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
NINTEDANIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
NINTEDANIB ESYLATEChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
PONATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
SUNITINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
VANDETANIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4, KDR
BRIVANIBChEMBLPhase 3FGFR1, FGFR2, FGFR3, FGFR4, KDR
CEDIRANIBChEMBLPhase 3FGFR1, FGFR2, FGFR3, FGFR4, KDR
DOVITINIBChEMBLPhase 3FGFR1, FGFR2, FGFR3, FGFR4, KDR
LESTAURTINIBChEMBLPhase 3FGFR1, FGFR2, FGFR3, FGFR4, KDR
LINIFANIBChEMBLPhase 3FGFR1, FGFR2, FGFR3, FGFR4, KDR
SEMAXANIBChEMBLPhase 3FGFR1, FGFR2, FGFR3, FGFR4, KDR
FEXAGRATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4, KDR
FGFR INHIBITOR DEBIO 1347ChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4, KDR
OSI-632ChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4, KDR
R-406ChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4, KDR
REBASTINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4, KDR
SU-014813ChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4, KDR
TANDUTINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4, KDR
TOZASERTIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4, KDR
AfatinibPubChemApprovedFGFR1, FGFR2, FGFR3, FGFR4, KDR
SelumetinibPubChemApprovedFGFR1, FGFR2, FGFR3, FGFR4, KDR
AXITINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, KDR
CERITINIBChEMBLPhase 4 (approved)FGFR2, FGFR3, FGFR4, KDR
DASATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, KDR
MIDOSTAURINChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, KDR
PEMIGATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, FGFR4
SORAFENIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3, KDR
AT-9283ChEMBLPhase 2FGFR1, FGFR2, FGFR3, KDR
DORAMAPIMODChEMBLPhase 2FGFR1, FGFR2, FGFR4, KDR
E-7090ChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
FISOGATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
FORETINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, KDR
LIRAFUGRATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
LUCITANIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, KDR
MK-2461ChEMBLPhase 2FGFR1, FGFR2, FGFR3, KDR
RESIGRATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
SEGIGRATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3, FGFR4
IdelalisibPubChemApprovedFGFR1, FGFR2, FGFR3, FGFR4
ENTRECTINIBChEMBLPhase 4 (approved)FGFR1, FGFR3, KDR
ALISERTIBChEMBLPhase 3FGFR1, FGFR3, KDR
MOTESANIBChEMBLPhase 3FGFR1, FGFR4, KDR
BMS-754807ChEMBLPhase 2FGFR1, FGFR2, FGFR3
CENISERTIBChEMBLPhase 2FGFR1, FGFR3, KDR
CEP-11981ChEMBLPhase 2FGFR1, FGFR3, KDR
DERAZANTINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
ILORASERTIBChEMBLPhase 2FGFR1, FGFR3, KDR
ROGARATINIBChEMBLPhase 2FGFR1, FGFR3, FGFR4
RX-518ChEMBLPhase 2FGFR1, FGFR2, KDR
REGORAFENIBChEMBL + PubChemPhase 4 (approved)FGFR1, KDR
CABOZANTINIBChEMBLPhase 4 (approved)FGFR1, KDR
ERLOTINIBChEMBLPhase 4 (approved)FGFR2, KDR
IBRUTINIBChEMBLPhase 4 (approved)FGFR2, KDR
NICLOSAMIDEChEMBLPhase 4 (approved)FGFR1, KDR
TIVOZANIBChEMBLPhase 4 (approved)FGFR1, KDR
UPADACITINIBChEMBLPhase 4 (approved)FGFR1, KDR
ORANTINIBChEMBLPhase 3FGFR1, KDR
SURUFATINIBChEMBLPhase 3FGFR1, KDR
AG-13958ChEMBLPhase 2FGFR1, KDR
DANUSERTIBChEMBLPhase 2FGFR1, KDR
ENMD-2076ChEMBLPhase 2FGFR1, KDR
RAF-265ChEMBLPhase 2FGFR1, KDR
TOCERANIBChEMBLPhase 2FGFR1, KDR
BinimetinibPubChemApprovedFGFR1, KDR
GENTIAN VIOLETChEMBL + PubChemPhase 4 (approved)KDR
ABEMACICLIBChEMBLPhase 4 (approved)KDR
ABROCITINIBChEMBLPhase 4 (approved)KDR
ACALABRUTINIBChEMBLPhase 4 (approved)KDR
ALECTINIBChEMBLPhase 4 (approved)KDR
AUROTHIOGLUCOSEChEMBLPhase 4 (approved)KDR
CABOZANTINIB S-MALATEChEMBLPhase 4 (approved)KDR
CAPIVASERTIBChEMBLPhase 4 (approved)FGFR1
ENASIDENIBChEMBLPhase 4 (approved)KDR
ESTRAMUSTINEChEMBLPhase 4 (approved)KDR
FOSTAMATINIB DISODIUMChEMBLPhase 4 (approved)KDR
FRUQUINTINIBChEMBLPhase 4 (approved)KDR
GLAFENINEChEMBLPhase 4 (approved)KDR
HEXACHLOROPHENEChEMBLPhase 4 (approved)KDR
IMATINIBChEMBLPhase 4 (approved)KDR
INDIGOTINDISULFONATEChEMBLPhase 4 (approved)KDR
ISOXICAMChEMBLPhase 4 (approved)KDR
MEBENDAZOLEChEMBLPhase 4 (approved)KDR
MESALAMINEChEMBLPhase 4 (approved)KDR
NERATINIBChEMBLPhase 4 (approved)KDR
NOVOBIOCINChEMBLPhase 4 (approved)KDR
OLMUTINIBChEMBLPhase 4 (approved)KDR
OLSALAZINEChEMBLPhase 4 (approved)KDR
OSIMERTINIBChEMBLPhase 4 (approved)KDR
PEXIDARTINIBChEMBLPhase 4 (approved)KDR
PHENYL AMINOSALICYLATEChEMBLPhase 4 (approved)KDR
PIPERAZINEChEMBLPhase 4 (approved)KDR
QUIZARTINIBChEMBLPhase 4 (approved)KDR
SELPERCATINIBChEMBLPhase 4 (approved)KDR

About this page

Generated deterministically by Sugi Atlas from primary biomedical databases via BioBTree. Every record on this page traces to a primary source.

Generated
Atlas version
v1.1.4
BioBTree
v2.0.2

Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot