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Pemigatinib

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Also known as Fgfr inhibitor incb054828Incb-054828Incb054828PemazyrePemigatinib

Summary

Pemigatinib (CHEMBL4297522) is an approved small molecule (ATC L01EN02) targeting FGFR1, FGFR2, and FGFR3; indicated across 14 conditions including neoplasm and cholangiocarcinoma; with CIViC clinical evidence for 6 variant-indication associations (e.g. FGFR2::v Fusion OR FGFR2::? Fusion in cholangiolocellular carcinoma).

At a glance

  • Status: Approved (max clinical phase 4)
  • Modality: Small molecule
  • ATC class: L01EN02
  • Targets: 3 (FGFR1, FGFR2, FGFR3)
  • Indications: 14 conditions
  • Clinical trials: 48
  • Precision-oncology evidence (CIViC): 6 variant–indication associations
  • Chemistry: 487.5 Da · C24H27F2N5O4

Identifiers

Drug identity and classification

FieldValue
ChEMBL IDCHEMBL4297522
NamePemigatinib
TypeSmall molecule
Max phase4
FDA approvedyes
PubChem CID86705695
ATCL01EN02
Molecular formulaC24H27F2N5O4
Molecular weight487.5
InChIKeyHCDMJFOHIXMBOV-UHFFFAOYSA-N

SMILES: CCN1C2=C3C=C(NC3=NC=C2CN(C1=O)C4=C(C(=CC(=C4F)OC)OC)F)CN5CCOCC5

IUPAC name: 11-(2,6-difluoro-3,5-dimethoxyphenyl)-13-ethyl-4-(morpholin-4-ylmethyl)-5,7,11,13-tetrazatricyclo[7.4.0.02,6]trideca-1,3,6,8-tetraen-12-one

Also known as: Fgfr inhibitor incb054828, Incb-054828, Incb054828, INCB054828, Pemazyre, Pemigatinib, PEMIGATINIB, Pemigatinib; Pemazyre

Patent coverage: 872 distinct patent families (2,055 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 1,992 (97%) 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 1Inhibition711.5%P11362
FGFR2fibroblast growth factor receptor 2Inhibition71.7%P21802
FGFR3fibroblast growth factor receptor 3Inhibition70.5%P22607

Broader ChEMBL bioactivity targets: 6 (assay-derived). Sample: Fibroblast growth factor receptor, Fibroblast growth factor receptor 3, Fibroblast growth factor receptor 2, Fibroblast growth factor receptor 1, Fibroblast growth factor receptor 4, Fibroblast growth factor receptor 2.

Bioactivity

ChEMBL activities: 50 potent at pChembl ≥ 5 of 50 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

TargetpChemblTypeValueUnitActivity ID
FGFR310IC500.1nMCHEMBL_ACT_26186118
FGFR29.62IC500.24nMCHEMBL_ACT_29151884
FGFR19.4IC500.4nMCHEMBL_ACT_23284803
FGFR19.4IC500.4nMCHEMBL_ACT_24661112
FGFR29.4IC500.4nMCHEMBL_ACT_24672426
FGFR19.4IC500.4nMCHEMBL_ACT_26025571
FGFR19.4IC500.4nMCHEMBL_ACT_26186116
FGFR19.4IC500.4nMCHEMBL_ACT_29055496
FGFR19.4IC500.4nMCHEMBL_ACT_29055497
FGFR19.4IC500.4nMCHEMBL_ACT_29152318
FGFR29.3IC500.5nMCHEMBL_ACT_23284807
FGFR29.3IC500.5nMCHEMBL_ACT_24661119
FGFR29.3IC500.5nMCHEMBL_ACT_26025562
FGFR29.3IC500.5nMCHEMBL_ACT_26186117
FGFR29.3IC500.5nMCHEMBL_ACT_29055498
FGFR29.3IC500.5nMCHEMBL_ACT_29152326
FGFR29.25IC500.56nMCHEMBL_ACT_29152153
FGFR19.05IC500.9nMCHEMBL_ACT_24672327
FGFR39.02IC500.96nMCHEMBL_ACT_29152171
FGFR39.01IC500.97nMCHEMBL_ACT_24805368
FGFR39IC501nMCHEMBL_ACT_24661116
FGFR39IC501nMCHEMBL_ACT_29152334
FGFR38.92IC501.2nMCHEMBL_ACT_23284811
FGFR38.92IC501.2nMCHEMBL_ACT_26025577
FGFR38.92IC501.2nMCHEMBL_ACT_29055499
FGFR38.77IC501.7nMCHEMBL_ACT_24672263
FGFR18.73IC501.88nMCHEMBL_ACT_24805350
FGFR38.62IC502.4nMCHEMBL_ACT_29152195
FGFR28.57IC502.7nMCHEMBL_ACT_29152159
FGFR28.52IC503nMCHEMBL_ACT_29152141

Target pathways

Aggregated over 3 target gene(s): FGFR1, FGFR2, FGFR3.

Top Reactome pathways

46 total, by targets touching each:

PathwayTargetsGenes
PI3K Cascade3FGFR1, FGFR2, FGFR3
PIP3 activates AKT signaling3FGFR1, FGFR2, FGFR3
Constitutive Signaling by Aberrant PI3K in Cancer3FGFR1, FGFR2, FGFR3
RAF/MAP kinase cascade3FGFR1, FGFR2, FGFR3
PI5P, PP2A and IER3 Regulate PI3K/AKT Signaling3FGFR1, FGFR2, FGFR3
Signaling by FGFR1 amplification mutants1FGFR1
Signaling by activated point mutants of FGFR11FGFR1
Signaling by activated point mutants of FGFR31FGFR3
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
Signaling by FGFR2 amplification mutants1FGFR2
t(4;14) translocations of FGFR31FGFR3
Activated point mutants of FGFR21FGFR2
NCAM signaling for neurite out-growth1FGFR1
Signal transduction by L11FGFR1
Phospholipase C-mediated cascade: FGFR11FGFR1
Phospholipase C-mediated cascade; FGFR21FGFR2
Phospholipase C-mediated cascade; FGFR31FGFR3
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

Dominant GO biological processes

GO termTargets
protein phosphorylation3
positive regulation of cell population proliferation3
fibroblast growth factor receptor signaling pathway3
positive regulation of phospholipase activity3
positive regulation of MAPK cascade3
skeletal system morphogenesis3
positive regulation of cell communication3
positive regulation of signaling3
negative regulation of transcription by RNA polymerase II2
MAPK cascade2
skeletal system development2
angiogenesis2
ureteric bud development2
in utero embryonic development2
epithelial to mesenchymal transition2

Indications & clinical

Indications

14 indications (3 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).

IndicationTrial phaseMONDOEFO
neoplasm4MONDO:0005070EFO:0000616
cholangiocarcinoma4MONDO:0019087EFO:0005221
urothelial carcinoma2MONDO:0040679EFO:0008528
endometrium neoplasm2MONDO:0021251MONDO:0011962
exocrine pancreatic carcinoma2MONDO:0005192EFO:0002618
non-small cell lung carcinoma2MONDO:0005233EFO:0003060
colorectal carcinoma2MONDO:0024331EFO:1001951
breast neoplasm2MONDO:0021100MONDO:0007254
dedifferentiated liposarcoma2MONDO:0020563EFO:0003085
gastric neoplasm2MONDO:0021085MONDO:0001056
acute myeloid leukemia1MONDO:0018874EFO:0000222

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

Clinical trials

Total trials: 48.

Phase distribution

PhaseTrials
PHASE237
PHASE15
PHASE1/PHASE23
Not specified2
PHASE31

Top trials by phase / activity

NCTPhaseStatusTitle
NCT03656536PHASE3TERMINATEDA Study to Evaluate the Efficacy and Safety of Pemigatinib Versus Chemotherapy in Unresectable or Metastatic Cholangiocarcinoma
NCT02925234PHASE2RECRUITINGThe Drug Rediscovery Protocol (DRUP Trial)
NCT04463771PHASE2ACTIVE_NOT_RECRUITINGSafety and Efficacy of Retifanlimab (INCMGA00012) Alone or in Combination With Other Therapies in Participants With Advanced or Metastatic Endometrial Cancer Who Have Progressed on or After Platinum-based Chemotherapy.
NCT05159245PHASE2RECRUITINGThe Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs
NCT05651672PHASE2RECRUITINGPemigatinib in the Advanced Gastrointestinal Cancer With FGFR 1-3 Alterations
NCT06300528PHASE2RECRUITINGPemigatinib in Patients With Relapsed or Refractory B-cell Non-Hodgkin Lymphomas
NCT06389799PHASE2RECRUITINGA Phase 2, Open Label Study of PEmigatinib and REtifanlimab in Advanced Dedifferentiated LIposarcoma (PERELI)
NCT06439485PHASE1/PHASE2RECRUITINGPhase I/II Trial of Pemigatinib in Combination With Atezolizumab and Bevacizumab for Treatment of Advanced Cholangiocarcinoma With FGFR2 Fusion
NCT06530823PHASE2NOT_YET_RECRUITINGPemigatinib Combined With Durvalumab for Previously Treated Biliary Tract Carcinoma
NCT06551896PHASE2NOT_YET_RECRUITINGPemigatinib and Immune Checkpoint Inhibitor Treated FGFR1/2/3 Alteration Advanced Solid Tumor
NCT06653777PHASE2RECRUITINGEfficacy of Pemigatinib in Patients With Solid Tumors Characterized by an Alteration of the Gene FGFR in Tumor Cells
NCT06728410PHASE2RECRUITINGA Phase II Study of Pemigatinib Plus Durvalumab in Previously Treated Advanced Intrahepatic Cholangiocarcinoma Patients With FGFR-2 Fusion or Rearrangement
NCT06906562PHASE2RECRUITINGA Phase II Nationwide, Fully Decentralized, Telemedicine Study of Pemigatinib in Adult Patients With Advanced or Metastatic Pancreatic Cancer With FGFR Genetic Alterations
NCT07434843PHASE2RECRUITINGPH 2 Pemigatinib in SDH-deficient GIST
NCT02393248PHASE1/PHASE2TERMINATEDOpen-Label, Dose-Escalation Study of Pemigatinib in Subjects With Advanced Malignancies - (FIGHT-101)
NCT02872714PHASE2COMPLETEDA Study to Evaluate the Efficacy and Safety of Pemigatinib (INCB054828) in Subjects With Urothelial Carcinoma - (FIGHT-201)
NCT02924376PHASE2COMPLETEDEfficacy and Safety of Pemigatinib in Subjects With Advanced/Metastatic or Surgically Unresectable Cholangiocarcinoma Who Failed Previous Therapy - (FIGHT-202)
NCT03011372PHASE2COMPLETEDA Study to Evaluate the Efficacy and Safety of Pemigatinib (INCB054828) in Subjects With Myeloid/Lymphoid Neoplasms With FGFR1 Rearrangement - (FIGHT-203)
NCT03498521PHASE2COMPLETEDA Phase II Randomized Study Comparing the Efficacy and Safety of Targeted Therapy or Cancer Immunotherapy Versus Platinum-Based Chemotherapy in Patients With Cancer of Unknown Primary Site
NCT03822117PHASE2TERMINATEDEfficacy and Safety of Pemigatinib in Previously Treated Locally Advanced/Metastatic or Surgically Unresectable Solid Tumor Malignancies Harboring Activating FGFR Mutations or Translocations (FIGHT-207)
NCT03914794PHASE2COMPLETEDA Study of Pemigatinib in Non-muscle Invasive Bladder Cancer Patients With Recurrent Low- or Intermediate-Risk Tumors
NCT04003610PHASE2TERMINATEDPemigatinib + Pembrolizumab vs Pemigatinib Alone vs Standard of Care for Urothelial Carcinoma (FIGHT-205)
NCT04003623PHASE2TERMINATEDEfficacy and Safety of Pemigatinib in Participants With Solid Tumors With FGFR Mutations or Translocations (FIGHT-208)
NCT04096417PHASE2UNKNOWNPemigatinib for the Treatment of Metastatic or Unresectable Colorectal Cancer Harboring FGFR Alterations
NCT04256980PHASE2COMPLETEDPemigatinib in Treating Patients With Advanced/Metastatic or Surgically Unresectable Cholangiocarcinoma Including FGFR2 Rearrangement
NCT04294277PHASE2TERMINATEDSafety and Efficacy of Pemigatinib in Patients With High-risk Urothelial Cancer After Radical Surgery
NCT04591431PHASE2UNKNOWNThe Rome Trial From Histology to Target: the Road to Personalize Target Therapy and Immunotherapy
NCT04949191PHASE2TERMINATEDThe Purpose of the Study is to Continue to Provide Pemigatinib to Patients With Advanced Malignancies.
NCT05004974PHASE2UNKNOWNSintilimab With Pemigatinib in Patients With PD-L1-positive and FGFR Mutated Advanced Non-small Cell Lung Cancer
NCT05202236PHASE2UNKNOWNA Single-Arm Phase II Exploratory Clinical Study of Pemigatinib in the Treatment of Advanced Gastric and Colorectal Cancer Patients With FGFR Alterations Who Have Failed Standard Therapy
NCT05216120PHASE2WITHDRAWNPemigatinib in Subjects With Adenosquamous Carcinoma of the Pancreas
NCT05253807PHASE2COMPLETEDStudy to Evaluate the Efficacy and Safety of Pemigatinib in Participants With Relapsed or Refractory Advanced Non-Small Cell Lung Cancer With an FGFR Alteration
NCT05267106PHASE2TERMINATEDStudy to Evaluate the Efficacy and Safety of Pemigatinib in Participants With Previously Treated Glioblastoma or Other Primary Central Nervous System Tumors Harboring Activating FGFR1-3 Alterations
NCT05287386PHASE2UNKNOWNA Single-Arm Phase II Clinical Study of Pemigatinib in the Treatment of Advanced Non-Small Cell Lung Cancer Patients With FGFR Alterations Who Have Failed Standard Therapy
NCT05529667PHASE1/PHASE2COMPLETEDFibroblast Growth Factor (FGFs) / Fibroblast Growth Factor Receptor (FGFRs) Genetic as a Second-line Therapy for Recurrent / Progressive Gastric Cancer With INCB054828 and Paclitaxel a Study to Evaluate the Safety and Efficacy of Combination Therapy.
NCT05559775PHASE2UNKNOWNA Single-Arm Phase II Exploratory Clinical Study of Pemigatinib in the Treatment of Advanced Gastrointestinal Cancer (Excluding Biliary Tract Cancer) Patients With FGFR Alterations Who Have Failed Standard Therapy
NCT05560334PHASE2UNKNOWNA Single-Arm, Open, Exploratory Clinical Study of Pemigatinib in the Treatment of HER2-negative Advanced Breast Cancer Patients With FGFR Alterations
NCT05565794PHASE2TERMINATEDPemigatinib After Curative Local Therapy in Advanced iCCA With FGFR2 Fusion/Rearrangements
NCT05913661PHASE2UNKNOWNPemigatinib Combined With PD-1 Inhibitor in Unresectable or Metastatic Intrahepatic Cholangiocarcinoma
NCT05997459PHASE2UNKNOWNA Single Arm, Phase II Exploratory Clinical Study of Pemitinib in Advanced Gastric Cancer With Previous Standard Therapy Failure the FGFR Variant

Clinical evidence (CIViC)

Variant × indication × effect (6 predictive associations from 6 curated evidence items):

VariantIndicationEffectTherapyLevelCIViC
FGFR2::v Fusion OR FGFR2::? FusionCholangiolocellular CarcinomaSensitivity/ResponsePemigatinibCIViC AEID8173
ZMYM2::FGFR1 Fusion OR BCR::FGFR1 Fusion OR CEP43::FGFR1 Fusion OR TRIM24::FGFR1 Fusion OR FGFR1 TranslocationMyeloid NeoplasmSensitivity/ResponsePemigatinibCIViC AEID11324
ZMYM2::FGFR1 Fusion OR BCR::FGFR1 Fusion OR CEP43::FGFR1 Fusion OR TRIM24::FGFR1 Fusion OR FGFR1 TranslocationLymphoid LeukemiaSensitivity/ResponsePemigatinibCIViC AEID12241
ZMYM2::FGFR1 Fusion OR BCR::FGFR1 Fusion OR CEP43::FGFR1 Fusion OR TRIM24::FGFR1 Fusion OR FGFR1 TranslocationLymphomaSensitivity/ResponsePemigatinibCIViC AEID12242
FGFR1 AmplificationBreast CancerSensitivity/ResponsePemigatinibCIViC CEID12542
FGFR1 N546KPilocytic AstrocytomaSensitivity/ResponsePemigatinibCIViC CEID10325

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.

89 molecules share ≥1 primary target. Top 60 by shared-target count:

MoleculeSourceStatusShared targets
CrizotinibChEMBL + PubChemPhase 4 (approved)FGFR1, FGFR2, FGFR3
PAZOPANIBChEMBL + PubChemPhase 4 (approved)FGFR1, FGFR2, FGFR3
AXITINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
BRIGATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
DASATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
ERDAFITINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
FEDRATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
FUTIBATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
INFIGRATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
LENVATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
MIDOSTAURINChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
NINTEDANIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
NINTEDANIB ESYLATEChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
PONATINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
SORAFENIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
SUNITINIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
VANDETANIBChEMBLPhase 4 (approved)FGFR1, FGFR2, FGFR3
BRIVANIBChEMBLPhase 3FGFR1, FGFR2, FGFR3
CEDIRANIBChEMBLPhase 3FGFR1, FGFR2, FGFR3
DOVITINIBChEMBLPhase 3FGFR1, FGFR2, FGFR3
LESTAURTINIBChEMBLPhase 3FGFR1, FGFR2, FGFR3
LINIFANIBChEMBLPhase 3FGFR1, FGFR2, FGFR3
SEMAXANIBChEMBLPhase 3FGFR1, FGFR2, FGFR3
AT-9283ChEMBLPhase 2FGFR1, FGFR2, FGFR3
BMS-754807ChEMBLPhase 2FGFR1, FGFR2, FGFR3
DERAZANTINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
E-7090ChEMBLPhase 2FGFR1, FGFR2, FGFR3
FEXAGRATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
FGFR INHIBITOR DEBIO 1347ChEMBLPhase 2FGFR1, FGFR2, FGFR3
FISOGATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
FORETINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
LIRAFUGRATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
LUCITANIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
MK-2461ChEMBLPhase 2FGFR1, FGFR2, FGFR3
OSI-632ChEMBLPhase 2FGFR1, FGFR2, FGFR3
R-406ChEMBLPhase 2FGFR1, FGFR2, FGFR3
REBASTINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
RESIGRATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
SEGIGRATINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
SU-014813ChEMBLPhase 2FGFR1, FGFR2, FGFR3
TANDUTINIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
TOZASERTIBChEMBLPhase 2FGFR1, FGFR2, FGFR3
AfatinibPubChemApprovedFGFR1, FGFR2, FGFR3
GefitinibPubChemApprovedFGFR1, FGFR2, FGFR3
IdelalisibPubChemApprovedFGFR1, FGFR2, FGFR3
SelumetinibPubChemApprovedFGFR1, FGFR2, FGFR3
CERITINIBChEMBLPhase 4 (approved)FGFR2, FGFR3
ENTRECTINIBChEMBLPhase 4 (approved)FGFR1, FGFR3
ALISERTIBChEMBLPhase 3FGFR1, FGFR3
CENISERTIBChEMBLPhase 2FGFR1, FGFR3
CEP-11981ChEMBLPhase 2FGFR1, FGFR3
DORAMAPIMODChEMBLPhase 2FGFR1, FGFR2
ILORASERTIBChEMBLPhase 2FGFR1, FGFR3
ROGARATINIBChEMBLPhase 2FGFR1, FGFR3
RX-518ChEMBLPhase 2FGFR1, FGFR2
REGORAFENIBChEMBL + PubChemPhase 4 (approved)FGFR1
CABOZANTINIBChEMBLPhase 4 (approved)FGFR1
CAPIVASERTIBChEMBLPhase 4 (approved)FGFR1
ERLOTINIBChEMBLPhase 4 (approved)FGFR2
IBRUTINIBChEMBLPhase 4 (approved)FGFR2

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
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Sources 30

This page pulls from 30 datasets indexed by BioBTree:

chebichembl_activitychembl_moleculechembl_targetcivic_evidenceclingen_dosageclinical_trialsdepmapefoensemblentrezgogoparentgtopdbgtopdb_interactiongtopdb_ligandhgncmeshmondomsigdbpatent_compoundpharmgkbpharmgkb_guidelinepubchempubchem_activityreactomereactomeparentrefseqtranscriptuniprot