FGFR2

FGFR2 is a growth receptor fused in bile-duct cancer and overproduced in gastric cancer.

FGFR2 fusions (~10-15% of intrahepatic cholangiocarcinoma) respond to pemigatinib and futibatinib; FGFR2b overexpression in gastric cancer is targeted by bemarituzumab (FORTITUDE-101 positive on OS in 2025) and FGFR2b ADCs.

FGFR2: what it is and how drugs act on it · animated generic schematic, not to scale

Target · the protein and the cell it sits on
Drug · antibody, small molecule, cell or radioligand
Effect · signal, damage or kill

In plain words · FGFR2 is a growth receptor fused in bile-duct cancer and overproduced in gastric cancer.

1 · What it is
FGFR2 is a growth receptor fused in bile-duct cancer and overproduced in gastric cancer.
2 · What goes wrong in cancer
Receptor tyrosine kinase; FGFR3 alterations are the urothelial counterpart (erdafitinib).
3 · How drugs use it
7 products aim at FGFR2: antibodies and small molecules. Kinases are switched on by binding ATP inside the cell, so most drugs are small molecules shaped to plug that ATP pocket.

Biology

Receptor tyrosine kinase; FGFR3 alterations are the urothelial counterpart (erdafitinib).

Where it is found

Cholangiocarcinoma
Gastric
Endometrial

Class

kinase · FGFR2

How common it is, by cancer

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)

Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.

Products

7top

Phase 3Monoclonal antibody (anti-FGFR2b)

Bemarituzumab

Bemarituzumab is an antibody against FGFR2b, a growth receptor overproduced in about a third of stomach cancers. It improved survival early in its phase 3 trial, but the gain faded with longer follow-up.

ApprovedSmall-molecule kinase inhibitor (pan-FGFR)

Erdafitinib · Balversa

The first targeted pill for bladder cancer, for the roughly 20% of tumours with FGFR3 alterations, used after immunotherapy.

ApprovedSmall-molecule irreversible kinase inhibitor (FGFR1-4)

Futibatinib · Lytgobi

Futibatinib is a covalent FGFR inhibitor for FGFR2-fusion bile duct cancer, with the highest response rate of the first-generation drugs.

ApprovedSmall-molecule multi-kinase inhibitor (VEGFR, FGFR, PDGFR, RET, KIT)

Lenvatinib · Lenvima

An oral anti-angiogenic pill that matched sorafenib in liver cancer with higher response rates, and partners with pembrolizumab in kidney and endometrial cancer.

NegativeSmall-molecule kinase inhibitor (VEGFR/FGFR/PDGFR)

Nintedanib · Ofev (fibrosis); Vargatef (NSCLC, EU)

An anti-angiogenic pill that looked promising in mesothelioma in a small trial but failed in the large one.

ApprovedSmall-molecule kinase inhibitor (FGFR1-3)

Pemigatinib · Pemazyre

Pemigatinib was the first targeted therapy for bile duct cancer, for tumours with an FGFR2 gene fusion.

Phase 3Small-molecule multi-kinase inhibitor (FGFR1-3, VEGFR, Aurora, JAK)

Tinengotinib

A next-generation FGFR inhibitor designed to work after pemigatinib or futibatinib stop working, now in a global phase 3.