Fruquintinib

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Fruquintinib is an onp drug catalogued in DrugCentral. It was first approved by the FDA in 2023. DrugCentral lists 3 molecular targets, including FLT4, FLT1 and KDR. Recorded indications include Metastatic colorectal cancer (mCRC).

• Approval status: onp (first approved 2023 by the FDA).
• Molecular targets: FLT4, FLT1 and KDR (3 listed in DrugCentral).
• Indications: Metastatic colorectal cancer (mCRC).
• ATC code: L01EK04 (Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors).
• Molecular formula: C21H19N3O5; molecular weight 393.40 g/mol.

Indications & contraindications

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

Indications (1)

• Metastatic colorectal cancer (mCRC)

Mechanism & targets

Molecular targets (3)

Target	Gene	Action	Activity
Vascular endothelial growth factor receptor 3	FLT4	inhibitor	IC50 9.30
Vascular endothelial growth factor receptor 1	FLT1	inhibitor	IC50 7.48
Vascular endothelial growth factor receptor 2	KDR	inhibitor	IC50 7.46

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2023-11-08	FDA	—	TAKEDA PHARMS USA

ATC classification

ATC code	Therapeutic hierarchy
L01EK04	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: KRAS
• FDA label: KRAS
• HCSC label: KRAS

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
Myelosuppression	540.5
Death	339.2
Palmar-plantar erythrodysaesthesia syndrome	290.5
Proteinuria	256.1
Hypertension	165.9
Dysphonia	118.0
Decreased appetite	109.8
Hypothyroidism	90.5
Nephrotic syndrome	90.3
Metastases to liver	85.2
Blood pressure increased	73.0
Asthenia	59.7

Chemical structure

• Molecular formula: C₂₁H₁₉N₃O₅
• Molecular weight: 393.40 g/mol
• CAS number: —
• InChIKey: BALLNEJQLSTPIO-UHFFFAOYSA-N
• PubChem CID: 44480399

CNC(=O)C1=C(C)OC2=CC(OC3=C4C=C(OC)C(OC)=CC4=NC=N3)=CC=C12

Frequently asked questions

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

What is Fruquintinib used for?

DrugCentral lists the following indications for Fruquintinib: Metastatic colorectal cancer (mCRC).

How does Fruquintinib work?

Its molecular targets in DrugCentral include FLT4 (inhibitor), FLT1 (inhibitor) and KDR (inhibitor).

When was Fruquintinib first approved?

Fruquintinib was first approved by the FDA in 2023.

What is the chemical formula of Fruquintinib?

Fruquintinib has the molecular formula C21H19N3O5 and a molecular weight of 393.40 g/mol.

Sources

• DrugCentral drug card 5750 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL4303214 — compound record and bioactivity
• PubChem CID 44480399 — chemical identifiers
• DrugBank DB11679 — drug record
• FDA UNII 49DXG3M5ZW — substance identity
• DailyMed: FDA labels for Fruquintinib — current prescribing information (label search)
• UniProt P35916 (FLT4) — target protein
• UniProt P17948 (FLT1) — 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.