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Protein / target

Fibroblast growth factor receptor 2

Encoded byFGFR2P21802Homo sapiensSwiss-Prot
Clinically validated
Therapeutic maturity
11
Approved medicines
Open Targets target-level
View by indication →
30
Clinical trials
Small-molecule tractable
Druggability
Approved Drug

Protein at a glance

Biological role

Fibroblast growth factor receptor

Primary biology

FGFR growth-factor signalling

Strongest disease association

Pfeiffer syndrome

Via encoding gene FGFR2 · Genetic evidence · score 0.97

Therapeutic position

Established drug target

Small molecules and antibodies

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 overview

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.

View complete UniProt function annotation

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.

Cell proliferation & survivalUniProt · GO · ReactomeGrowth-factor signallingUniProt · GOOncogenic signallingReactomeKinase signallingUniProt · GOTranscriptional regulationGOApoptosis & cell deathGO
View supporting evidence

Cell proliferation & survival

  • ·Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth facto…
  • ·fibroblast growth factor receptor signaling pathway involved in positive regulation of c…
  • ·positive regulation of cell population proliferation
  • ·PIP3 activates AKT signaling

Growth-factor signalling

  • ·Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth facto…
  • ·fibroblast growth factor binding
  • ·fibroblast growth factor receptor activity
  • ·fibroblast growth factor receptor signaling pathway

Oncogenic signalling

  • ·Constitutive Signaling by Aberrant PI3K in Cancer

Kinase signalling

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

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…
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.

Approved medicines with mapped indications

4 medicines · 5 areas

Approved therapies targeting this protein, grouped by what they are approved to treat — the disease-first view of the medicines below. Relationships come from the canonical approved-indication graph (ChEMBL phase-4), the same source as the drug cards.

Cholangiocarcinoma2 medicines
Carcinoma, Transitional Cell1 medicine
Colorectal Neoplasms1 medicine
Urinary Bladder Neoplasms1 medicine
Broader indication categories (1)

Broad umbrella indications (e.g. “Neoplasms”). Shown here because every medicine also appears under a more specific disease above — kept for completeness, de-emphasised for clarity.

11 medicines meet Open Targets' target-level approved-medicine definition; the 4 shown here are those on this page with a canonical approved disease indication in the graph. Approved indications from ChEMBL (phase-4), via the canonical drug→disease graph.

Drugs targeting this protein

5

How approved and investigational drugs engage this protein — mechanism and action type, direct vs complex targeting, and how broadly each acts across other targets. A drug-first view (the section above groups the approved ones disease-first); direct binders with few recorded targets are listed first.

bemarituzumab
Narrow target profilePhase 3Inhibitor

Fibroblast growth factor receptor 2 inhibitor

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

pemigatinib
Narrow target profileApprovedInhibitor

Fibroblast growth factor receptor 2 inhibitor

Indicated for Cholangiocarcinoma, Neoplasms

Direct interaction with this protein · 1 of 3 recorded protein targets — narrow recorded profile

regorafenib
ApprovedInhibitor

Fibroblast growth factor receptor 2 inhibitor

Indicated for Colorectal Neoplasms, Neoplasms

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

erdafitinib
ApprovedInhibitor

Fibroblast growth factor receptor inhibitor

Indicated for Carcinoma, Transitional Cell, Urinary Bladder Neoplasms, Neoplasms

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

futibatinib
ApprovedInhibitor

Fibroblast growth factor receptor inhibitor

Indicated for Cholangiocarcinoma, Neoplasms

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

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

Translational evidence

Open Targets 26

Why this target matters therapeutically, strongest evidence first. Disease associations are gene-level (via the gene that encodes this protein) and open into the full confidence synthesis; the development universe, tractability and safety annotations are target-level, from Open Targets.

Strongest disease associations · via encoding gene FGFR2

Gene-level evidence surfaced through the gene FGFR2that encodes this protein — not a direct protein–disease relationship. Ranked by Forefront's causal-directness weighting, so genetically- and clinically-evidenced diseases lead over ones that merely share the literature.

Neoplasms
0.97Well supported

Genetic evidence dominant · Open Targets 0.80

Pfeiffer syndrome
0.97Well supported

Genetic evidence dominant · Open Targets 0.85

Crouzon syndrome
0.96Well supported

Genetic evidence dominant · Open Targets 0.86

Apert syndrome
0.92Well supported

Genetic evidence dominant · Open Targets 0.83

Jackson-Weiss syndrome
0.90Well supported

Genetic evidence dominant · Open Targets 0.81

View evidence synthesis (5)
NeoplasmsWell 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 per-type scores above show the calculation.

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
Neoplasms0.80
Lacrimoauriculodentodigital syndrome0.79
Bent bone dysplasia syndrome 10.78
LADD syndrome 10.78

Drug development

27 compounds recorded · 11 approved · 16 in clinical development

Open Targets' development universe — every compound recorded against the target at any stage, not all approved medicines. Distinct from the 5 drugs that target this protein in Forefront's canonical graph (4 with a mapped approved indication, shown above): these count different sets and are not a subset relation.

View all recorded compounds (10)
ROGARATINIBPhase 2 3
HMPL-453Phase 2
NINTEDANIB ESYLATEApproval
PEMIGATINIBApproval
FGFR INHIBITOR DEBIO 1347Phase 2
LUCITANIBPhase 3
ERDAFITINIBApproval
FEXAGRATINIBPhase 2
APRUTUMAB IXADOTINPhase 1
ENMD-981693Phase 2

Open Targets known-drugs universe. Drug name and highest clinical stage only — the disease relationship is NOT read from this slice (it carries trial-context noise); approved indications come from the canonical graph above.

Tractability

Small moleculesStrong

Approved Drug and Structure with Ligand support this modality.

AntibodiesStrong

Advanced Clinical and GO CC high conf support this modality.

Protein degradersEmerging

Feasibility evidence (literature and uniprot ubiquitination) — no clinical-stage drug of this modality recorded.

Other modalitiesStrong

Approved Drug support this modality.

View underlying tractability evidence (15)
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 UbiquitinationPR · Half-life DataPR · Small Molecule BinderOC · Approved Drug

Raw Open Targets tractability assessment buckets, by modality.

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. Ranked by active status, then clinical phase and recency, and spread across the targeting drugs.

View all trials (26)

ClinicalTrials.gov via the drug-target graph.

What's happening now

12

Recent therapeutic activity around this target — regulatory actions, clinical trials and safety signals for 5 drugs that target this protein, plus publications where such a drug is a genuine subject. Every item is reached indirectly through the drug, not the protein itself; incidental mentions (a paper that merely measures a drug) and press items are excluded.

  1. Trial status changed2026-07-29

    A Phase 1b/2 Study Evaluating the Safety, Tolerability, Efficacy, and Pharmacokinetics of Bemarituzumab in Combination With Other Anti-cancer Therapies in Subjects With Previously Untreated Advanced Gastric or Gastroesophageal Junction Cancer (FORTITUDE-103).

    Status changed to Terminated · ClinicalTrials.gov · via bemarituzumab

  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. Regulatory approval2023-07-04

    Approval: Lytgobi (EMA)

    ema · regulatory · ema · via futibatinib

  6. 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

  7. Regulatory approval2021-03-26

    Approval: Pemazyre (EMA)

    ema · regulatory · ema · via pemigatinib

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

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

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

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

  10. 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

  11. 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

  12. Regulatory approval2013-08-26

    Approval: Stivarga (EMA)

    ema · regulatory · ema · 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.