Lenvatinib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Lenvatinib is an onp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2015. Its mechanism of action is classified as Receptor Tyrosine Kinase Inhibitors. DrugCentral lists 33 molecular targets, including RET, FGFR4 and KDR. Recorded indications include Endometrial carcinoma progressing after chemotherapy, Follicular thyroid carcinoma, Hurthle cell carcinoma of thyroid and Liver cell carcinoma.

• Approval status: onp (first approved 2015 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Receptor Tyrosine Kinase Inhibitors.
• Molecular targets: RET, FGFR4, KDR and FLT4 (33 listed in DrugCentral).
• Indications: Endometrial carcinoma progressing after chemotherapy, Follicular thyroid carcinoma, Hurthle cell carcinoma of thyroid, Liver cell carcinoma and Papillary thyroid carcinoma and others.
• ATC code: L01EX08 (Other protein kinase inhibitors).
• Molecular formula: C21H19ClN4O4; molecular weight 426.86 g/mol.

Indications & contraindications

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

Indications (7)

• Endometrial carcinoma progressing after chemotherapy
• Follicular thyroid carcinoma
• Hurthle cell carcinoma of thyroid
• Liver cell carcinoma
• Papillary thyroid carcinoma
• Renal cell carcinoma
• Thymic carcinoma

Contraindications (1)

• Breastfeeding (mother)

Mechanism & targets

• Mechanism of action (MoA): Receptor Tyrosine Kinase Inhibitors
• Established pharmacologic class: Kinase Inhibitor

Molecular targets (33)

Target	Gene	Action	Activity
Proto-oncogene tyrosine-protein kinase receptor Ret	RET	inhibitor	Ki 8.82
Fibroblast growth factor receptor 4	FGFR4	unknown	IC50 8.72
Vascular endothelial growth factor receptor 2	KDR	inhibitor	IC50 8.40
Vascular endothelial growth factor receptor 3	FLT4	inhibitor	IC50 8.28
Fibroblast growth factor receptor 2	FGFR2	unknown	IC50 7.96
Receptor-interacting serine/threonine-protein kinase 2	RIPK2	unknown	Kd 7.96
Vascular endothelial growth factor receptor 1	FLT1	inhibitor	IC50 7.66
Fibroblast growth factor receptor 3	FGFR3	unknown	IC50 7.57
Platelet-derived growth factor receptor beta	PDGFRB	inhibitor	IC50 7.41
Epithelial discoidin domain-containing receptor 1	DDR1	unknown	Kd 7.34
Fibroblast growth factor receptor 1	FGFR1	inhibitor	IC50 7.34
Platelet-derived growth factor receptor alpha	PDGFRA	inhibitor	IC50 7.29
MAP kinase-activated protein kinase 2	MAPKAPK2	unknown	Kd 7.20
Mast/stem cell growth factor receptor Kit	KIT	inhibitor	IC50 7.00
Carbonic anhydrase 5A, mitochondrial	CA5A	unknown	Ki 6.88
Protein-tyrosine kinase 6	PTK6	unknown	Kd 6.76
Discoidin domain-containing receptor 2	DDR2	unknown	Kd 6.66
Mitogen-activated protein kinase 14	MAPK14	unknown	Kd 6.66
Receptor-interacting serine/threonine-protein kinase 3	RIPK3	unknown	Kd 6.50
TRAF2 and NCK-interacting protein kinase	TNIK	unknown	Kd 6.25

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2015-05-28	EMA	—	Eisai Europe Ltd	Yes
2015-03-26	PMDA	—	Eisai Co., Ltd.	Yes
2015-02-13	FDA	—	EISAI INC	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EX08	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
• FDA label · Testing Required
• HCSC label · Testing Required

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
Malignant neoplasm progression	6075.8
Hypertension	4325.4
Proteinuria	3853.9
Hypothyroidism	3659.7
Palmar-plantar erythrodysaesthesia syndrome	3440.2
Decreased appetite	2033.3
Platelet count decreased	1389.3
Hepatic encephalopathy	1182.3
Diarrhoea	1142.8
Adrenal insufficiency	1117.1
Interstitial lung disease	947.3
Immune-mediated hypothyroidism	846.8

Chemical structure

• Molecular formula: C₂₁H₁₉ClN₄O₄
• Molecular weight: 426.86 g/mol
• CAS number: —
• InChIKey: WOSKHXYHFSIKNG-UHFFFAOYSA-N
• PubChem CID: 9823820

COC1=CC2=C(C=C1C(N)=O)C(OC1=CC=C(NC(=O)NC3CC3)C(Cl)=C1)=CC=N2

Frequently asked questions

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

What is Lenvatinib used for?

DrugCentral lists the following indications for Lenvatinib: Endometrial carcinoma progressing after chemotherapy, Follicular thyroid carcinoma, Hurthle cell carcinoma of thyroid, Liver cell carcinoma, Papillary thyroid carcinoma, Renal cell carcinoma and Thymic carcinoma.

How does Lenvatinib work?

Lenvatinib is classified as Receptor Tyrosine Kinase Inhibitors; its molecular targets in DrugCentral include RET (inhibitor), FGFR4, KDR (inhibitor) and FLT4 (inhibitor).

When was Lenvatinib first approved?

Lenvatinib was first approved by the FDA in 2015.

What drug class does Lenvatinib belong to?

Lenvatinib is in the Kinase Inhibitor class.

What is the chemical formula of Lenvatinib?

Lenvatinib has the molecular formula C21H19ClN4O4 and a molecular weight of 426.86 g/mol.

Sources

• DrugCentral drug card 4942 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL1289601 — compound record and bioactivity
• PubChem CID 9823820 — chemical identifiers
• DrugBank DB09078 — drug record
• FDA UNII EE083865G2 — substance identity
• DailyMed: FDA labels for Lenvatinib — current prescribing information (label search)
• UniProt P07949 (RET) — target protein
• UniProt P22455 (FGFR4) — target protein
• UniProt P35968 (KDR) — target protein
• UniProt P35916 (FLT4) — target protein
• UniProt P21802 (FGFR2) — target protein
• UniProt O43353 (RIPK2) — 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.