Futibatinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Futibatinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2022. Its mechanism of action is classified as Breast Cancer Resistance Protein Inhibitors, Fibroblast Growth Factor Receptor Inhibitors and P-Glycoprotein Inhibitors. DrugCentral lists 6 molecular targets, including FGFR2, FGFR4 and FGFR3. Recorded indications include Biliary tract cancer and Intrahepatic cholangiocarcinoma.

• Approval status: onp (first approved 2022 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Breast Cancer Resistance Protein Inhibitors; Fibroblast Growth Factor Receptor Inhibitors; P-Glycoprotein Inhibitors.
• Molecular targets: FGFR2, FGFR4, FGFR3 and FGFR1 (6 listed in DrugCentral).
• Indications: Biliary tract cancer and Intrahepatic cholangiocarcinoma.
• ATC code: L01EN04 (Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors).
• Molecular formula: C22H22N6O3; molecular weight 418.46 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (2)

• Biliary tract cancer
• Intrahepatic cholangiocarcinoma

Mechanism & targets

• Mechanism of action (MoA): Breast Cancer Resistance Protein Inhibitors; Fibroblast Growth Factor Receptor Inhibitors; P-Glycoprotein Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (6)

Target	Gene	Action	Activity
Fibroblast growth factor receptor 2	FGFR2	inhibitor	IC50 8.85
Fibroblast growth factor receptor 4	FGFR4	inhibitor	IC50 8.79
Fibroblast growth factor receptor 3	FGFR3	inhibitor	IC50 8.79
Fibroblast growth factor receptor 1	FGFR1	inhibitor	IC50 8.74
Tyrosine-protein kinase BTK	BTK	unknown	IC50 7.02
Vascular endothelial growth factor receptor 2	KDR	unknown	IC50 5.63

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2023-07-04	EMA	—	TAIHO PHARMA NETHERLANDS B.V.
2023-06-26	PMDA	—	Taiho Pharmaceutical Co., Ltd.
2022-09-30	FDA	—	TAIHO ONCOLOGY	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EN04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: FGFR2 · Testing Required
• FDA label: FGFR2 · Testing Required
• HCSC label

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Hyperphosphataemia	134.6

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Futibatinib is on its molecule page.

• Molecular formula: C₂₂H₂₂N₆O₃
• Molecular weight: 418.46 g/mol
• CAS number: 1448169-71-8
• InChIKey: KEIPNCCJPRMIAX-HNNXBMFYSA-N
• PubChem CID: 71621331

COC1=CC(=CC(OC)=C1)C#CC1=NN([C@H]2CCN(C2)C(=O)C=C)C2=NC=NC(N)=C12

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Futibatinib used for?

DrugCentral lists the following indications for Futibatinib: Biliary tract cancer and Intrahepatic cholangiocarcinoma.

How does Futibatinib work?

Futibatinib is classified as Breast Cancer Resistance Protein Inhibitors, Fibroblast Growth Factor Receptor Inhibitors and P-Glycoprotein Inhibitors; its molecular targets in DrugCentral include FGFR2 (inhibitor), FGFR4 (inhibitor), FGFR3 (inhibitor) and FGFR1 (inhibitor).

When was Futibatinib first approved?

Futibatinib was first approved by the FDA in 2022.

What drug class does Futibatinib belong to?

Futibatinib is in the Kinase Inhibitor class.

What is the chemical formula of Futibatinib?

Futibatinib has the molecular formula C22H22N6O3 and a molecular weight of 418.46 g/mol.

Sources

• DrugCentral drug card 5680 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3701238 — compound record and bioactivity
• PubChem CID 71621331 — chemical identifiers
• DrugBank DB15149 — drug record
• FDA UNII 4B93MGE4AL — substance identity
• DailyMed: FDA labels for Futibatinib — current prescribing information (label search)
• UniProt P21802 (FGFR2) — target protein
• UniProt P22455 (FGFR4) — target protein
• UniProt P22607 (FGFR3) — target protein
• UniProt P11362 (FGFR1) — target protein
• UniProt Q06187 (BTK) — target protein
• UniProt P35968 (KDR) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral
• PharmGKB / CPIC — pharmacogenomic label annotations

How this page is built: methodology · editorial policy & corrections.