Regorafenib

ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Regorafenib is an onp drug catalogued in DrugCentral. It was first approved by the FDA in 2012. DrugCentral lists 35 molecular targets, including EPHX2, FGFR1 and FLT1. Recorded indications include Gastrointestinal stromal tumor, Liver cell carcinoma and Metastasis from malignant tumor of colon.

• Approval status: onp (first approved 2012 by the FDA).
• Molecular targets: EPHX2, FGFR1, FLT1 and RAF1 (35 listed in DrugCentral).
• Indications: Gastrointestinal stromal tumor, Liver cell carcinoma and Metastasis from malignant tumor of colon.
• ATC code: L01EX05 (Other protein kinase inhibitors).
• Molecular formula: C21H15ClF4N4O3; molecular weight 482.82 g/mol.

Indications & contraindications

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

Indications (3)

• Gastrointestinal stromal tumor
• Liver cell carcinoma
• Metastasis from malignant tumor of colon

Mechanism & targets

Molecular targets (35)

Target	Gene	Action	Activity
Bifunctional epoxide hydrolase 2	EPHX2	inhibitor	IC50 9.30
Fibroblast growth factor receptor 1	FGFR1	unknown	IC50 8.82
Vascular endothelial growth factor receptor 1	FLT1	unknown	IC50 8.82
RAF proto-oncogene serine/threonine-protein kinase	RAF1	unknown	IC50 8.82
Angiopoietin-1 receptor	TEK	unknown	IC50 8.82
Platelet-derived growth factor receptor beta	PDGFRB	unknown	IC50 8.82
Vascular endothelial growth factor receptor 2	Kdr	unknown	IC50 8.82
Vascular endothelial growth factor receptor 3	Flt4	unknown	IC50 8.82
Platelet-derived growth factor receptor alpha	PDGFRA	unknown	IC50 8.38
Mast/stem cell growth factor receptor Kit	KIT	unknown	IC50 8.21
Ephrin type-A receptor 1	EPHA1	unknown	Kd 8.15
Vascular endothelial growth factor receptor 2	KDR	inhibitor	IC50 7.90
Serine/threonine-protein kinase B-raf	BRAF	inhibitor	IC50 7.55
Vascular endothelial growth factor receptor 3	FLT4	unknown	IC50 7.34
Receptor-type tyrosine-protein kinase FLT3	FLT3	unknown	IC50 7.09
Proto-oncogene tyrosine-protein kinase receptor Ret	RET	unknown	Kd 6.90
Mitogen-activated protein kinase kinase kinase MLT	ZAK	unknown	Kd 6.56
Epithelial discoidin domain-containing receptor 1	DDR1	unknown	Kd 6.45
Receptor-interacting serine/threonine-protein kinase 3	RIPK3	unknown	Kd 6.43
Discoidin domain-containing receptor 2	DDR2	unknown	Kd 6.38

Regulatory approvals (2)

Date	Agency	Marketed as	Applicant	Orphan
2013-08-26	EMA	—	—
2012-09-27	FDA	—	BAYER HLTHCARE

ATC classification

ATC code	Therapeutic hierarchy
L01EX05	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Other protein kinase inhibitors

Pharmacogenomics

Drug-label and guideline annotations from PharmGKB and CPIC.

• EMA label: KRAS · Informative PGx
• 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
Palmar-plantar erythrodysaesthesia syndrome	3948.6
Dysphonia	1154.4
Metastases to lung	692.1
Decreased appetite	620.1
Off label use	500.6
Metastases to liver	429.2
Fatigue	414.8
Diarrhoea	392.5
Blood bilirubin increased	309.1
Carcinoembryonic antigen increased	269.4
Asthenia	257.4
Hypertension	240.0

Chemical structure

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

• Molecular formula: C₂₁H₁₅ClF₄N₄O₃
• Molecular weight: 482.82 g/mol
• CAS number: 755037-03-7
• InChIKey: FNHKPVJBJVTLMP-UHFFFAOYSA-N
• PubChem CID: 11167602

CNC(=O)C1=CC(OC2=CC(F)=C(NC(=O)NC3=CC(=C(Cl)C=C3)C(F)(F)F)C=C2)=CC=N1

Frequently asked questions

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

What is Regorafenib used for?

DrugCentral lists the following indications for Regorafenib: Gastrointestinal stromal tumor, Liver cell carcinoma and Metastasis from malignant tumor of colon.

How does Regorafenib work?

Its molecular targets in DrugCentral include EPHX2 (inhibitor), FGFR1, FLT1 and RAF1.

When was Regorafenib first approved?

Regorafenib was first approved by the FDA in 2012.

What is the chemical formula of Regorafenib?

Regorafenib has the molecular formula C21H15ClF4N4O3 and a molecular weight of 482.82 g/mol.

Sources

• DrugCentral drug card 4654 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1946170 — compound record and bioactivity
• PubChem CID 11167602 — chemical identifiers
• DrugBank DB08896 — drug record
• FDA UNII MGN125FS9D — substance identity
• DailyMed: FDA labels for Regorafenib — current prescribing information (label search)
• UniProt P34913 (EPHX2) — target protein
• UniProt P11362 (FGFR1) — target protein
• UniProt P17948 (FLT1) — target protein
• UniProt P04049 (RAF1) — target protein
• UniProt Q02763 (TEK) — target protein
• UniProt P09619 (PDGFRB) — 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.