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FGFR2 is a growth receptor fused in bile-duct cancer and overproduced in gastric cancer. This dossier gathers the 16 products (8 approved), 121 trials, 3 pathways and 0 resistance routes in the corpus that involve it, with external identifiers so it can be joined to UniProt, ChEMBL, Open Targets and the rest of biology.
Receptor tyrosine kinase; FGFR3 alterations are the urothelial counterpart (erdafitinib).
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Bladder & urothelial cancer | 15-20% | FGFR3 alterations (related target) | FGFR3 mutations/fusions; erdafitinib | cBioPortal (TCGA) |
| Biliary tract cancer | 10-15% | Fusion (intrahepatic) | cBioPortal (TCGA) | |
| Gastric & gastro-oesophageal junction cancer | 3-8% | FGFR2b overexpression/amplification | FORTITUDE-101 selected IHC 2+/3+ | cBioPortal (TCGA) |
| Gallbladder cancer | 1% | Fusion, mutation or amplification | No FGFR2 fusion among the structural variants deposited for cBioPortal gbc_mskcc_2022; FGFR2 mutation in 3 of 244, 1.2%, and amplification in 3 of 244, 1.2%; no recurrent structural variants in the cohort (Giraldo 2022). | cBioPortal (TCGA) |
| Pancreatic ductal adenocarcinoma | 0.2% | Gene fusion | cBioPortal structural variants: 4 of 2,336, 0.17% (FGFR2-CAT 2, FGFR2-SHTN1), in pdac_msk_2024; 5.2% of 266 KRAS wild-type tumours (Philip 2022). Other receptor kinase fusions in pdac_msk_2024: ROS1 5 (GOPC-ROS1), RAF1 4, RET 2 (NCOA4-RET), MET 2 (KANK1-MET), ERBB2 2, EGFR 3, FGFR1 2, FGFR3 1 (cBioPortal). | cBioPortal (TCGA) |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
| Residue | Kind | How common | What it does | Addressed by | Defeats | Source |
|---|---|---|---|---|---|---|
| Fusions (FGFR2::BICC1 and many partners) 768 to 821 | Activating | About 10 to 15% of intrahepatic cholangiocarcinoma | Breakpoints in the last exon keep the kinase intact and add a dimerising partner. Pemigatinib and futibatinib are approved. | - | Goyal et al., Cancer Discov 2017 | |
| N550K / N550H 550 | Activating | not sourced | Molecular-brake mutation: primary driver in endometrial cancer and an acquired resistance allele after reversible FGFR inhibitors. | - | Goyal et al., Cancer Discov 2017 | |
| V565I / V565F (gatekeeper) and E566A, L618V 565 | Resistance | not sourced | Polyclonal secondary kinase-domain mutations after pemigatinib or infigratinib; the covalent inhibitor futibatinib and newer FGFR2-selective agents retain activity against several of them. | Goyal et al., Cancer Discov 2017 |
Frequencies are quoted from the source on each row; a blank means no figure was sourced, not that it is rare. Domain boundaries are approximate. Sources for the map: Cancer Hotspots (MSK) · COSMIC: FGFR2.
| Modality | Approved | Phase 3 | Phase 2 | Withdrawn or failed |
|---|---|---|---|---|
| Small molecule 14 | ||||
| Antibody 1 | - | - | - | |
| Test or device 1 | - | - | - |
| Trial | Setting | Result | Products | ||
|---|---|---|---|---|---|
| 3 | Active | A Multi-Center, Double-Blind, Randomized, Phase III Study to Investigate the Efficacy and Safety of Nofazinlimab (CS1003) in Combination With Lenvatinib Compared to Placebo in Combination With Lenvatinib as First-Line Therapy in Subjects With Advanced Hepatocellular Carcinoma (HCC) | - | ||
EMERALD-3 NCT05301842 | 3 | Positive | Embolisation-eligible unresectable HCC: STRIDE (durvalumab + tremelimumab) + lenvatinib + TACE vs TACE | PFS HR ~0.70 (interim); OS immature. | |
FIGHT-302 NCT03656536 | 3 | Withdrawn | Untreated advanced cholangiocarcinoma with an FGFR2 rearrangement: pemigatinib against gemcitabine and cisplatin | - | |
LITESPARK-011 NCT04586231 | 3 | Positive | Advanced clear-cell renal cell carcinoma that has progressed after anti-PD-1 or anti-PD-L1 therapy: belzutifan 120 mg plus lenvatinib 20 mg versus cabozantinib 60 mg, all oral once daily, open label, randomised 1:1 | Final progression-free survival 14.8 vs 10.7 months (hazard ratio 0.70, 95% CI 0.59 to 0.84; one-sided p<0.0001). Interim overall survival 34.9 vs 27.6 months (hazard ratio 0.85, 0.68 to 1.05; one-sided p 0.061), not statistically significant. Data cutoff 9 April 2025. | |
LITESPARK-012 NCT04736706 | 3 | Negative | Untreated advanced clear-cell RCC: pembrolizumab + lenvatinib ± belzutifan (or ± quavonlimab) | Primary endpoint not met (ASCO GU 2026). | |
FORTITUDE-101 NCT05052801 | 3 | Mixed | First-line FGFR2b-overexpressing (≥10% 2+/3+), HER2-negative advanced gastric/GEJ cancer: bemarituzumab + mFOLFOX6 vs placebo + mFOLFOX6 | Interim OS 17.9 vs 12.5 months (HR 0.61); benefit attenuated on follow-up. | |
LEAP-012 NCT04246177 | 3 | Mixed | Unresectable non-metastatic HCC: TACE + lenvatinib + pembrolizumab vs TACE + placebo | PFS HR 0.66; final OS HR 0.98. | |
THOR NCT03390504 | 3 | Positive | Advanced urothelial cancer with FGFR3/2 alterations after chemotherapy and a checkpoint inhibitor: erdafitinib vs chemotherapy (cohort 1) | OS 12.1 vs 7.8 months, HR 0.64 (cohort 1). | |
LEAP-002 NCT03713593 | 3 | Negative | First-line unresectable HCC: lenvatinib + pembrolizumab vs lenvatinib | OS HR 0.84, not significant. | |
CLEAR (KEYNOTE-581) NCT02811861 | 3 | Positive | Untreated advanced clear-cell RCC: lenvatinib + pembrolizumab vs sunitinib (and lenvatinib + everolimus arm) | PFS 23.9 vs 9.2 months (HR 0.39); OS HR 0.79. | |
KEYNOTE-775 / Study 309 NCT03517449 | 3 | Positive | Advanced endometrial cancer after platinum: lenvatinib + pembrolizumab vs doxorubicin or weekly paclitaxel | OS 18.3 vs 11.4 months (HR 0.62). | |
REFLECT NCT01761266 | 3 | Positive | First-line unresectable HCC: lenvatinib vs sorafenib (non-inferiority) | OS 13.6 vs 12.3 months, non-inferior (HR 0.92). | |
LUME-Lung 1 NCT00805194 | 3 | Mixed | Stage IIIB or IV recurrent non-small-cell lung cancer progressing after first-line chemotherapy: docetaxel 75 mg/m2 on day 1 with nintedanib 200 mg twice daily or placebo on days 2 to 21, every three weeks, with progression-free survival by independent central review as the primary endpoint and a stepwise overall survival hierarchy | Median progression-free survival 3.4 against 2.7 months (hazard ratio 0.79, p=0.0019); overall survival significant in the adenocarcinoma populations of the prespecified hierarchy but not overall. | |
| 3 | Planned | A Randomized, Double-blind, Placebo-controlled Phase III Clinical Trial to Evaluate the Efficacy and Safety of TQB2450 Combined With Anlotinib as Maintenance Therapy in Patients With Limited-stage Small Cell Lung Cancer | - | ||
| 3 | Planned | A Single Center, Single Arm Clinical Study on the Treatment of Advanced Non-small Cell | - | ||
| 3 | Planned | A Single-arm, Exploratory Clinical Study Evaluating the Efficacy and Safety of Bevacizumab in Combination With Anlotinib and Etoposide as First-line Therapy for Elderly Patients With Small-cell Lung Cancer or Those Who Are Intolerant to Intensive Chemotherapy | - | ||
| 3 | Recruiting | A Phase III, Randomized, Double-blinded, Multicenter Study of Cadonilimab (AK104) + Lenvatinib in Combination With Transarterial Chemoembolization (TACE) Versus TACE in Participants With Incurable/Non-metastatic Hepatocellular Carcinoma | - | ||
| 3 | Active | A Randomized, Open-label, Parallel Controlled, Multi-center Phase III Study of Anlotinib Hydrochloride Capsule Combined With Chemotherapy as First-line Treatment in Subjects With RAS/BRAF Wild Metastatic Colorectal Cancer | - | ||
| 3 | Active | An Open-label, Randomized Phase 3 Study to Evaluate Efficacy and Safety of Pembrolizumab (MK-3475) in Combination With Belzutifan (MK-6482) and Lenvatinib (MK-7902), or MK-1308A in Combination With Lenvatinib, Versus Pembrolizumab and Lenvatinib, as First-Line Treatment in Participants With Advanced Clear Cell Renal Cell Carcinoma (ccRCC) | - | ||
| 3 | Recruiting | A Phase 3, Randomized, Open-label, Multicenter Study Evaluating the Efficacy and Safety of TAR-210 Erdafitinib Intravesical Delivery System Versus Investigator's Choice of Intravesical Chemotherapy in Participants With High-risk Non-muscle-invasive Bladder Cancer With Susceptible FGFR Alterations Who Had Received Intravesical Bacillus Calmette-Guérin (BCG) | - | ||
| 3 | Recruiting | A Phase 3, Randomized Study Evaluating the Efficacy and Safety of TAR-210 Erdafitinib Intravesical Delivery System Versus Single Agent Intravesical Chemotherapy in Participants With Intermediate-risk Non-muscle Invasive Bladder Cancer (IR-NMIBC) and Susceptible FGFR Alterations | - | ||
| 3 | Recruiting | A Randomized, Double-blind, Placebo-controlled, Multicenter Phase 3 Study of Anlotinib Hydrochloride Capsules Combined With Penpulimab Injection in Patients With High Risk of Relapse After Radical Surgery or Ablation of Hepatocellular Carcinoma (HCC). | - | ||
| 3 | Recruiting | Anlotinib Plus Whole-Brain Radiotherapy for Brain Metastases in Small Cell Lung Cancer Patients: A Multicenter Phase III Trail. | - | ||
| 3 | Recruiting | A Multicenter, Open-label, Phase 3 Extension Study to Evaluate the Long-term Efficacy and Safety in Participants Who Are Currently on Treatment in a Belzutifan Study (LITESPARK-043) | - | ||
| FIRST-308 | 3 | Recruiting | FGFR-altered cholangiocarcinoma refractory to chemotherapy and a first-generation FGFR inhibitor: tinengotinib vs FOLFOX/FOLFIRI | - | |
| 3 | Recruiting | A Phase 3, Randomized-Controlled, Open-Label, Multi-Regional, International Study of Futibatinib (TAS-120) and Zimberelimab (AB122) in Combination With Gemcitabine Plus Cisplatin Versus Durvalumab or Pembrolizumab in Combination With Gemcitabine Plus Cisplatin for Patients With First-Line Advanced Biliary Tract Cancers | - | ||
| 3 | Planned | Investigating Precision Medicine in the Adjuvant Setting: a Phase 3 Clinical Trial in Biliary Tract Cancer | - | ||
| 3 | Recruiting | A Phase III Study of AL3818 (Anlotinib, Catequentinib) Hydrochloride Monotherapy in Subjects With Metastatic or Advanced Alveolar Soft Part Sarcoma, Leiomyosarcoma and Synovial Sarcoma | - | ||
SAFIR-ABC10 NCT05615818 | 3 | Recruiting | Advanced biliary cancer (intrahepatic, perihilar or distal cholangiocarcinoma, or gallbladder carcinoma) after induction gemcitabine and cisplatin: molecular targeted maintenance therapy matched to the tumour's alteration versus standard of care, international platform phase 3 | - | |
| 3 | Active | A Phase III, Randomized, Controlled, Global Multicenter Study to Evaluate the Efficacy and Safety of Oral Tinengotinib VS Physician's Choice in Subjects With FGFR-altered, Chemotherapy- and FGFR Inhibitor-Cholangiocarcinoma | - |
No recorded escape route names this target.
Fibroblast growth factor receptors are growth antennas on the cell surface. Bladder cancer mutates FGFR3, bile duct cancer fuses FGFR2 to other genes, and stomach cancer overproduces FGFR2b; each has its own drug, and each brings a tell-tale side effect (high phosphate) because the same receptors control phosphate in the kidney.
Which nodes have drugs →This KEGG map splits stomach cancer into two routes: the intestinal type that accumulates TP53, APC and HER2 changes step by step, and the diffuse type driven by loss of the cell glue E-cadherin plus MET or FGFR2 amplification. It matters because HER2, FGFR2, claudin 18.2 and PD-1 status now decide first-line treatment.
Which nodes have drugs →This KEGG map shows how sugar-coated proteins on the cell surface and in the surrounding matrix (proteoglycans such as syndecans, glypicans, CD44 and decorin) catch growth factors and hand signals to receptors. It matters because these molecules set how loudly growth signals reach the tumour cell and how easily it invades.
Which nodes have drugs →| Assay | Platform | Cut-off | Gates |
|---|---|---|---|
| FoundationOne CDx Foundation Medicine (Roche) · FDA CDx 2017 | NGS tissue | Per companion claim: EGFR, ALK, BRAF V600, ERBB2 amplification, KRAS wild-type, BRCA1/2 and HRR genes, PIK3CA, MET exon 14, RET, FGFR2 fusions, IDH1, NTRK fusions; MSI-high; TMB at least 10 mutations per megabase | |
| FoundationOne Liquid CDx Foundation Medicine (Roche) · FDA CDx 2020 | NGS plasma | Per companion claim: EGFR (osimertinib, erlotinib, gefitinib), ALK (alectinib), BRCA1/2 and ATM (olaparib, rucaparib), PIK3CA (alpelisib), FGFR3 (erdafitinib), NTRK and RET; negative plasma results reflex to tissue | |
| therascreen FGFR RGQ RT-PCR Kit QIAGEN · FDA CDx 2019 | PCR | Alteration detected (erdafitinib, urothelial carcinoma) |
No model entry for this target yet; check the cancer entries on the models page.
Why unresolved. Resistance in cholangiocarcinoma is polyclonal (N550, V565, E566, L618) and varies between lesions; covalent and next-generation FGFR2-selective agents cover subsets, and hyperphosphataemia from FGFR1 limits dosing of pan-FGFR drugs.
What would answer it. Trials of FGFR2-selective inhibitors after FGFR-inhibitor progression with ctDNA-defined resistance profiles.
Source: Goyal et al., Cancer Discov 2017Query for this target: (TITLE:"FGFR2" OR ABSTRACT:"FGFR2") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about FGFR2, not a curated reading list.
The dossier as machine-readable JSON, at /api/v1/dossiers/fgfr2.json: identifiers from HGNC, Ensembl, UniProt and ChEMBL, products with status, trials, pathways, hotspots, open questions and assays. The full entity record is in the open API at /api/v1/entities/fgfr2.json. Licence CC BY-NC 4.0.