Protein / target

Fibroblast growth factor receptor 2

FGFR2P21802Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
11
Approved medicines
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Fibroblast growth factor receptor activity

Primary system

Nervous system

Strongest disease association

Pfeiffer syndrome

Genetic evidence · score 0.97

Therapeutic maturity

Clinically validated target

11 approved medicines against this target

Druggability

Small molecule

Open Targets tractability · Approved Drug

Clinical development

11 approved · 16 in clinical development

30 linked trials

Derived from structured UniProt, Open Targets and literature data on this page.

Protein profile

UniProt 2026_02

Canonical identity and biological annotation from UniProt.

Function

Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosis, and in the regulation of embryonic development. Required for normal embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis and skin development. Plays an essential role in the regulation of osteoblast differentiation, proliferation and apoptosis, and is required for normal skeleton development. Promotes cell proliferation in keratinocytes and immature osteoblasts, but promotes apoptosis in differentiated osteoblasts. Phosphorylates PLCG1, FRS2 and PAK4. Ligand binding leads to the activation of several signaling cascades. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate. Phosphorylation of FRS2 triggers recruitment of GRB2, GAB1, PIK3R1 and SOS1, and mediates activation of RAS, MAPK1/ERK2, MAPK3/ERK1 and the MAP kinase signaling pathway, as well as of the AKT1 signaling pathway. FGFR2 signaling is down-regulated by ubiquitination, internalization and degradation. Mutations that lead to constitutive kinase activation or impair normal FGFR2 maturation, internalization and degradation lead to aberrant signaling. Over-expressed FGFR2 promotes activation of STAT1

Subcellular location

Cell membraneGolgi apparatusCytoplasmic vesicleSecreted
Domains and Gene Ontology detail (117)

Domains & features

Ig-like C2-type 1Ig-like C2-type 2Ig-like C2-type 3Protein kinase

Gene Ontology

  • Ccell cortex
  • Ccell surface
  • Ccytoplasm
  • Ccytoplasmic vesicle
  • Cexcitatory synapse
  • Cextracellular region
  • CGolgi apparatus
  • Cmembrane
  • Cnucleus
  • Cplasma membrane
  • Creceptor complex
  • FATP binding

821 aa · 92 kDa · 17 isoforms

Biological roles

Reactome v97

What this protein does, drawn together from its UniProt function, Gene Ontology terms and Reactome pathways.

Kinase signallingUniProt · GOTranscriptional regulationGOApoptosis & cell deathGOExcitatory neurotransmissionGOSynaptic signallingGO
View supporting evidence

Kinase signalling

  • ·Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth facto…
  • ·protein tyrosine kinase activity
  • ·peptidyl-tyrosine phosphorylation
  • ·protein autophosphorylation

Transcriptional regulation

  • ·negative regulation of transcription by RNA polymerase II
  • ·positive regulation of transcription by RNA polymerase II

Apoptosis & cell death

  • ·apoptotic process
  • ·fibroblast growth factor receptor signaling pathway involved in negative regulation of a…

Excitatory neurotransmission

  • ·excitatory synapse

Synaptic signalling

  • ·excitatory synapse
View underlying pathways (17)

Concepts derived from UniProt GO Reactome — each badge above shows which sources supported that role.

Interaction neighbourhood

STRING v12.0

Proteins with the strongest functional or physical association. Node size and line weight reflect STRING confidence; hover or select a partner to inspect one association.

FGF1FGF4FGF10FGF18FGF3FGF8FGF17FGF9FGF22FGF2FGFR2

10 strongest partners — larger node and heavier line mean higher confidence

Functional and physical associations from STRING v12.0. Only associations with this protein are drawn — partner-to-partner links are not part of this evidence.

Drugs targeting this protein

4

Whether each drug engages this protein directly or through a complex, and how many other targets are recorded for it. Direct binders with few recorded targets are listed first.

bemarituzumab
Narrow target profilePhase 3Inhibitor

Fibroblast growth factor receptor 2 inhibitor

Appears in clinical studies involving gastric cancer, gastric neoplasm, gastric adenocarcinoma, gastroesophageal junction adenocarcinoma

Direct interaction with this protein · 1 of 2 recorded protein targets — narrow recorded profile

regorafenib
ApprovedInhibitor

Fibroblast growth factor receptor 2 inhibitor

Appears in clinical studies involving colorectal cancer, metastatic colorectal cancer, colorectal neoplasm, neoplasm

Direct interaction with this protein · 1 of 18 recorded protein targets — broad pharmacology

erdafitinib
ApprovedInhibitor

Fibroblast growth factor receptor inhibitor

Appears in clinical studies involving cancer, urothelial carcinoma, urinary bladder carcinoma, neoplasm

Acts on a complex — shared with FGFR3, FGFR1, FGFR4 · 1 of 4 recorded protein targets

futibatinib
ApprovedInhibitor

Fibroblast growth factor receptor inhibitor

Appears in clinical studies involving cancer, biliary tract cancer, intrahepatic cholangiocarcinoma, cholangiocarcinoma

Acts on a complex — shared with FGFR3, FGFR1, FGFR4 · 1 of 4 recorded protein targets

ChEMBL mechanism, action type and target identity. Open Targets clinical status and indications.

Translational evidence

Open Targets 26

Why this target matters therapeutically — disease associations, drugs in development, tractability and safety, from Open Targets.

Strongest genetic associations

Human genetic evidence — the most direct causal link between this target and a disease.

Pfeiffer syndrome0.97

Genetic · overall 0.85

Crouzon syndrome0.95

Genetic · overall 0.86

Apert syndrome0.88

Genetic · overall 0.83

Jackson-Weiss syndrome0.87

Genetic · overall 0.81

Beare-Stevenson cutis gyrata syndrome0.86

Genetic · overall 0.82

Highest-confidence therapeutic associations

Diseases where a drug acting on this target has already reached clinical development.

cancer0.93

Clinical · overall 0.80

Highest overall evidence

Remaining associations by Open Targets' aggregated evidence score.

Antley-Bixler syndrome without genital anomalies or disordered steroidogenesis0.81

Genetic

Lacrimoauriculodentodigital syndrome0.79

Genetic

bent bone dysplasia syndrome 10.78

Genetic

LADD syndrome 10.78

Genetic

Show all associations
Crouzon syndrome0.86
Pfeiffer syndrome0.85
Apert syndrome0.83
Beare-Stevenson cutis gyrata syndrome0.82
Jackson-Weiss syndrome0.81
Antley-Bixler syndrome without genital anomalies or disordered steroidogenesis0.81
cancer0.80
Lacrimoauriculodentodigital syndrome0.79
bent bone dysplasia syndrome 10.78
LADD syndrome 10.78

Open Targets ranks 5,541 associations for this target and we store the top 10 by aggregated score. The long tail is largely literature co-mention and RNA-expression evidence, not evidence that this target drives those diseases.

Known drugs · 27 total

ROGARATINIBPhase 2 3

urothelial carcinoma · urinary bladder carcinoma · non-small cell lung carcinoma

HMPL-453Phase 2

malignant mesothelioma · bladder transitional cell carcinoma · cholangiocarcinoma

NINTEDANIB ESYLATEApproval

idiopathic pulmonary fibrosis · systemic sclerosis · non-small cell lung carcinoma

PEMIGATINIBApproval

biliary tract cancer · cholangiocarcinoma · cancer

FGFR INHIBITOR DEBIO 1347Phase 2

breast cancer

LUCITANIBPhase 3

small cell lung carcinoma · breast cancer · lung cancer

ERDAFITINIBApproval

cancer · urothelial carcinoma · urinary bladder carcinoma

FEXAGRATINIBPhase 2

gastric adenocarcinoma · non-small cell lung carcinoma · breast cancer

APRUTUMAB IXADOTINPhase 1

gastric cancer · breast cancer

ENMD-981693Phase 2

colorectal carcinoma · breast carcinoma · exocrine pancreatic carcinoma

Tractability

SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · High-Quality PocketSM · Druggable FamilyAB · Advanced ClinicalAB · GO CC high confAB · UniProt loc med confAB · UniProt SigP or TMHMMPR · LiteraturePR · UniProt UbiquitinationPR · Database Ubiquitination

Clinical trials

30

Trials of drugs that target this protein — reached indirectly through those drugs, so a trial listed here studies the drug, not the protein.

Show remaining trials (24)

ACTIVE_NOT_RECRUITING · via regorafenib · NCT05395741

TERMINATED · via regorafenib · NCT02402036

ClinicalTrials.gov via the drug-target graph.

Forefront confidence

Synthesis

Our own weighting of the evidence behind each disease association. Human genetics and clinical evidence count for most; literature co-mention counts for little, because two entities sharing an abstract is not evidence that one drives the other.

cancerWell supported
0.97
agreement 0.881.00
Genetic41%Clinical34%Pathway19%Literature7%

Open Targets aggregate 0.80 · 4 independent evidence families

Pfeiffer syndromeWell supported
0.97
agreement 0.851.00
Genetic79%Animal model18%Literature4%Genetic literaturedup

Open Targets aggregate 0.85 · 3 independent evidence families · 1 not counted as duplicate

Crouzon syndromeWell supported
0.96
agreement 0.841.00
Genetic76%Animal model19%Literature6%Genetic literaturedup

Open Targets aggregate 0.86 · 3 independent evidence families · 1 not counted as duplicate

Apert syndromeWell supported
0.92
agreement 0.801.00
Genetic71%Animal model18%Literature11%Genetic literaturedup

Open Targets aggregate 0.83 · 3 independent evidence families · 1 not counted as duplicate

Jackson-Weiss syndromeWell supported
0.90
agreement 0.781.00
Genetic78%Animal model21%Literature1%Genetic literaturedup

Open Targets aggregate 0.81 · 3 independent evidence families · 1 not counted as duplicate

This ranking differs from Open Targets' own: re-weighting moves genetically-evidenced diseases above more heavily co-mentioned ones. The evidence agreement range shows how closely the independent evidence families agree — it is not a statistical confidence interval, and nothing here is fitted to outcome data. Derived from Open Targets evidence types under Forefront weighting; the underlying per-type scores are shown above so the calculation can be checked.

What's happening now

13

Recent activity around this target, drawn from one canonical event stream. Every item is reached through 4 drugs that target this protein, so each event is news about that drug rather than about the protein directly.

  1. New publication2025-01-06
    Efficacy of pembrolizumab in microsatellite-stable, tumor mutational burden-high metastatic colorectal cancer: genomic signatures and clinical outcomes.

    ESMO open · 2025 · 10 citations · Europe PMC · via regorafenib

  2. Regulatory approval2024-08-22

    Approval: Balversa (EMA)

    ema · regulatory · ema · via erdafitinib

  3. New publication2024-06-04
    Lenvatinib Plus Pembrolizumab Versus Standard of Care for Previously Treated Metastatic Colorectal Cancer: Final Analysis of the Randomized, Open-Label, Phase III LEAP-017 Study.

    Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2024 · 69 citations · Europe PMC · via regorafenib

  4. New publication2024-02-03
    Bemarituzumab as first-line treatment for locally advanced or metastatic gastric/gastroesophageal junction adenocarcinoma: final analysis of the randomized phase 2 FIGHT trial.

    Gastric cancer : official journal of the International Gastric Cancer Association and the Japanese Gastric Cancer Association · 2024 · 50 citations · Europe PMC · via bemarituzumab

  5. New publication2023-11-01
    Clinical and Genomic Landscape of FGFR3-Altered Urothelial Carcinoma and Treatment Outcomes with Erdafitinib: A Real-World Experience.

    Clinical cancer research : an official journal of the American Association for Cancer Research · 2023 · 49 citations · Europe PMC · via erdafitinib

  6. Regulatory approval2023-07-04

    Approval: Lytgobi (EMA)

    ema · regulatory · ema · via futibatinib

  7. New publication2023-01-01
    Futibatinib for <i>FGFR2</i>-Rearranged Intrahepatic Cholangiocarcinoma.

    The New England journal of medicine · 2023 · 420 citations · Europe PMC · via futibatinib

  8. New publication2020-08-11
    Targeted therapy for hepatocellular carcinoma.

    Signal transduction and targeted therapy · 2020 · 565 citations · Europe PMC · via regorafenib

  9. New publication2019-11-04
    Molecular targeted and immune checkpoint therapy for advanced hepatocellular carcinoma.

    Journal of experimental & clinical cancer research : CR · 2019 · 162 citations · Europe PMC · via regorafenib

  10. New publication2019-07-01
    Erdafitinib in Locally Advanced or Metastatic Urothelial Carcinoma.

    The New England journal of medicine · 2019 · 1,006 citations · Europe PMC · via erdafitinib

  11. New publication2019-04-23
    Randomized Double-Blind Phase II Study of Regorafenib in Patients With Metastatic Osteosarcoma.

    Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2019 · 199 citations · Europe PMC · via regorafenib

  12. New publication2016-12-06
    Regorafenib for patients with hepatocellular carcinoma who progressed on sorafenib treatment (RESORCE): a randomised, double-blind, placebo-controlled, phase 3 trial.

    Lancet (London, England) · 2017 · 2,767 citations · Europe PMC · via regorafenib

Objective event titles are shown unmodified; the event kind and significance line are derived from structured fields. Forefront AttentionEvent stream aggregating Europe PMC Regulatory filings ClinicalTrials.gov.