Protein / target

Fibroblast growth factor receptor 3

FGFR3P22607Homo 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

Musculoskeletal system

Strongest disease association

thanatophoric dysplasia type 1

Genetic evidence · score 0.90

Therapeutic maturity

Clinically validated target

11 approved medicines against this target

Druggability

Small molecule

Open Targets tractability · Approved Drug

Clinical development

11 approved · 14 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 and apoptosis. Plays an essential role in the regulation of chondrocyte differentiation, proliferation and apoptosis, and is required for normal skeleton development. Regulates both osteogenesis and postnatal bone mineralization by osteoblasts. Promotes apoptosis in chondrocytes, but can also promote cancer cell proliferation. Required for normal development of the inner ear. Phosphorylates PLCG1, CBL and FRS2. 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. Plays a role in the regulation of vitamin D metabolism. Mutations that lead to constitutive kinase activation or impair normal FGFR3 maturation, internalization and degradation lead to aberrant signaling. Over-expressed or constitutively activated FGFR3 promotes activation of PTPN11/SHP2, STAT1, STAT5A and STAT5B. Secreted isoform 3 retains its capacity to bind FGF1 and FGF2 and hence may interfere with FGF signaling

Subcellular location

Cell membraneCytoplasmic vesicleEndoplasmic reticulumSecreted
Domains and Gene Ontology detail (34)

Domains & features

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

Gene Ontology

  • Cendoplasmic reticulum
  • Cextracellular region
  • CGolgi apparatus
  • Cplasma membrane
  • Creceptor complex
  • Ctransport vesicle
  • FATP binding
  • Ffibroblast growth factor binding
  • Ffibroblast growth factor receptor activity
  • Fidentical protein binding
  • Fprotein tyrosine kinase activity
  • Pbone maturation

806 aa · 88 kDa · 4 isoforms

Biological roles

Reactome v97

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

Kinase signallingUniProt · GO
View supporting evidence

Kinase signalling

  • ·Tyrosine-protein kinase that acts as a cell-surface receptor for fibroblast growth facto…
  • ·protein tyrosine kinase activity
  • ·positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction
  • ·positive regulation of tyrosine phosphorylation of STAT protein
View underlying pathways (16)

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.

FGF8FGF9FGF2FGF1FGF18FGF13FGFR2FGF17GRB2HRASFGFR3

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

2

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.

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 FGFR1, FGFR4, FGFR2 · 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 FGFR1, FGFR4, FGFR2 · 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.

thanatophoric dysplasia type 10.90

Genetic · overall 0.82

achondroplasia0.89

Genetic · overall 0.82

Severe achondroplasia - developmental delay - acanthosis nigricans0.89

Genetic · overall 0.81

hypochondroplasia0.87

Genetic · overall 0.80

urinary bladder carcinoma0.86

Genetic · overall 0.80

Highest-confidence therapeutic associations

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

urinary bladder cancer0.56

Clinical · overall 0.79

Highest overall evidence

Remaining associations by Open Targets' aggregated evidence score.

Muenke syndrome0.80

Genetic

thanatophoric dysplasia type 20.79

Genetic

Crouzon syndrome-acanthosis nigricans syndrome0.78

Genetic

camptodactyly-tall stature-scoliosis-hearing loss syndrome0.77

Genetic

Show all associations
achondroplasia0.82
thanatophoric dysplasia type 10.82
Severe achondroplasia - developmental delay - acanthosis nigricans0.81
urinary bladder carcinoma0.80
hypochondroplasia0.80
Muenke syndrome0.80
urinary bladder cancer0.79
thanatophoric dysplasia type 20.79
Crouzon syndrome-acanthosis nigricans syndrome0.78
camptodactyly-tall stature-scoliosis-hearing loss syndrome0.77

Open Targets ranks 5,225 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 · 25 total

FEXAGRATINIBPhase 2

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

NINTEDANIB ESYLATEApproval

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

HMPL-453Phase 2

malignant mesothelioma · bladder transitional cell carcinoma · cholangiocarcinoma

PAZOPANIBApproval

renal cell carcinoma · neoplasm · renal cell carcinoma

XL-999Phase 2

ovarian cancer · colorectal cancer · renal cell carcinoma

INFIGRATINIB PHOSPHATEApproval

cholangiocarcinoma · neoplasm

E-7090Approval

cancer · biliary tract cancer · cholangiocarcinoma

FGFR INHIBITOR DEBIO 1347Phase 2

breast cancer

ENMD-2076Phase 2

acute myeloid leukemia by FAB classification · triple-negative breast carcinoma · ovarian cancer

ORANTINIBPhase 3

hepatocellular carcinoma

Tractability

SM · Approved DrugSM · Structure with LigandSM · High-Quality LigandSM · Druggable FamilyAB · Phase 1 ClinicalAB · GO CC high confAB · UniProt loc med confAB · UniProt SigP or TMHMMPR · UniProt UbiquitinationPR · Database UbiquitinationPR · Small Molecule BinderOC · Advanced Clinical

Safety liabilities

regulation of catalytic activity

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 erdafitinib · NCT02465060

TERMINATED · via futibatinib · NCT04189445

ACTIVE_NOT_RECRUITING · via erdafitinib · NCT03155620

RECRUITING · via futibatinib · NCT02693535

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.

urinary bladder carcinomaWell supported
0.98
agreement 0.891.00
Genetic38%Somatic mutation22%Clinical22%Pathway12%Literature6%Genetic literaturedup

Open Targets aggregate 0.80 · 5 independent evidence families · 1 not counted as duplicate

urinary bladder cancerWell supported
0.96
agreement 0.871.00
Genetic42%Somatic mutation30%Clinical21%Literature7%

Open Targets aggregate 0.79 · 4 independent evidence families

achondroplasiaWell supported
0.96
agreement 0.861.00
Genetic55%Clinical26%Animal model15%Literature5%Genetic literaturedup

Open Targets aggregate 0.82 · 4 independent evidence families · 1 not counted as duplicate

hypochondroplasiaWell supported
0.93
agreement 0.831.00
Genetic60%Animal model19%Clinical17%Literature4%Genetic literaturedup

Open Targets aggregate 0.80 · 4 independent evidence families · 1 not counted as duplicate

thanatophoric dysplasia type 1Well supported
0.93
agreement 0.811.00
Genetic77%Animal model20%Literature2%Genetic literaturedup

Open Targets aggregate 0.82 · 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

5

Recent activity around this target, drawn from one canonical event stream. Every item is reached through 2 drugs that target this protein, so each event is news about that drug rather than about the protein directly.

  1. Regulatory approval2024-08-22

    Approval: Balversa (EMA)

    ema · regulatory · ema · via erdafitinib

  2. 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

  3. Regulatory approval2023-07-04

    Approval: Lytgobi (EMA)

    ema · regulatory · ema · via futibatinib

  4. 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

  5. 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

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.