Erdafitinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Erdafitinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2019. Its mechanism of action is classified as Cytochrome P450 3A4 Inducers, Cytochrome P450 3A4 Inhibitors and Fibroblast Growth Factor Receptor Inhibitors. DrugCentral lists 6 molecular targets, including Kdr, FGFR1 and FGFR2. Recorded indications include Metastatic urothelial carcinoma.

• Approval status: onp (first approved 2019 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Cytochrome P450 3A4 Inducers; Cytochrome P450 3A4 Inhibitors; Fibroblast Growth Factor Receptor Inhibitors.
• Molecular targets: Kdr, FGFR1, FGFR2 and FGFR3 (6 listed in DrugCentral).
• Indications: Metastatic urothelial carcinoma.
• ATC code: L01EN01 (Fibroblast growth factor receptor (FGFR) tyrosine kinase inhibitors).
• Molecular formula: C25H30N6O2; molecular weight 446.56 g/mol.

Indications & contraindications

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

Indications (1)

• Metastatic urothelial carcinoma

Mechanism & targets

• Mechanism of action (MoA): Cytochrome P450 3A4 Inducers; Cytochrome P450 3A4 Inhibitors; Fibroblast Growth Factor Receptor Inhibitors; Organic Cation Transporter 2 Inhibitors; P-Glycoprotein Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (6)

Target	Gene	Action	Activity
Vascular endothelial growth factor receptor 2	Kdr	unknown	IC50 10.00
Fibroblast growth factor receptor 1	FGFR1	inhibitor	IC50 8.92
Fibroblast growth factor receptor 2	FGFR2	inhibitor	IC50 8.60
Fibroblast growth factor receptor 3	FGFR3	inhibitor	IC50 8.52
Fibroblast growth factor receptor 4	FGFR4	inhibitor	IC50 8.24
Vascular endothelial growth factor receptor 2	KDR	inhibitor	IC50 7.43

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
2019-04-12	FDA	—	JANSSEN BIOTECH

ATC classification

ATC code	Therapeutic hierarchy
L01EN01	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: FGFR3 · Testing Required
• FDA label: FGFR3 · Testing Required
• FDA label: CYP2C9 · Actionable PGx
• HCSC label: FGFR3 · Testing Required
• HCSC label: CYP2C9 · Actionable PGx

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
Onycholysis	250.3
Hyperphosphataemia	188.1
Death	154.1
Nail disorder	99.4
Nail toxicity	99.3
Nail discolouration	97.4
Ocular toxicity	94.5
Mucosal inflammation	91.0
Stomatitis	70.6
Retinal detachment	66.7
Dry eye	60.0
Paronychia	58.6

Chemical structure

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

• Molecular formula: C₂₅H₃₀N₆O₂
• Molecular weight: 446.56 g/mol
• CAS number: 1346242-81-6
• InChIKey: OLAHOMJCDNXHFI-UHFFFAOYSA-N
• PubChem CID: 67462786

COC1=CC(=CC(OC)=C1)N(CCNC(C)C)C1=CC2=NC(=CN=C2C=C1)C1=CN(C)N=C1

Frequently asked questions

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

What is Erdafitinib used for?

DrugCentral lists the following indications for Erdafitinib: Metastatic urothelial carcinoma.

How does Erdafitinib work?

Erdafitinib is classified as Cytochrome P450 3A4 Inducers, Cytochrome P450 3A4 Inhibitors and Fibroblast Growth Factor Receptor Inhibitors; its molecular targets in DrugCentral include Kdr, FGFR1 (inhibitor), FGFR2 (inhibitor) and FGFR3 (inhibitor).

When was Erdafitinib first approved?

Erdafitinib was first approved by the FDA in 2019.

What drug class does Erdafitinib belong to?

Erdafitinib is in the Kinase Inhibitor class.

What is the chemical formula of Erdafitinib?

Erdafitinib has the molecular formula C25H30N6O2 and a molecular weight of 446.56 g/mol.

Sources

• DrugCentral drug card 5327 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3545376 — compound record and bioactivity
• PubChem CID 67462786 — chemical identifiers
• DrugBank DB12147 — drug record
• FDA UNII 890E37NHMV — substance identity
• DailyMed: FDA labels for Erdafitinib — current prescribing information (label search)
• UniProt P11362 (FGFR1) — target protein
• UniProt P21802 (FGFR2) — target protein
• UniProt P22607 (FGFR3) — target protein
• UniProt P22455 (FGFR4) — 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.