Nintedanib

Kinase Inhibitor — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Key facts

Nintedanib is an ofp drug in the Kinase Inhibitor class catalogued in DrugCentral. It was first approved by the FDA in 2014. Its mechanism of action is classified as Protein Kinase Inhibitors. DrugCentral lists 225 molecular targets, including FLT3, MAP2K5 and BMP2K. Recorded indications include Idiopathic pulmonary fibrosis, Interstitial fibrosis, Non-small cell lung cancer and Systemic sclerosis associated interstitial lung disease.

• Approval status: ofp (first approved 2014 by the FDA).
• Drug class: Kinase Inhibitor.
• Mechanism of action: Protein Kinase Inhibitors.
• Molecular targets: FLT3, MAP2K5, BMP2K and KCNH2 (225 listed in DrugCentral).
• Indications: Idiopathic pulmonary fibrosis, Interstitial fibrosis, Non-small cell lung cancer and Systemic sclerosis associated interstitial lung disease.
• ATC code: L01EX09 (Other protein kinase inhibitors).
• Molecular formula: C31H33N5O4; molecular weight 539.64 g/mol.

Indications & contraindications

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

Indications (4)

• Idiopathic pulmonary fibrosis
• Interstitial fibrosis
• Non-small cell lung cancer
• Systemic sclerosis associated interstitial lung disease

Mechanism & targets

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

Molecular targets (225)

Target	Gene	Action	Activity
Receptor-type tyrosine-protein kinase FLT3	FLT3	unknown	Kd 9.38
Dual specificity mitogen-activated protein kinase kinase 5	MAP2K5	unknown	Kd 8.74
BMP-2-inducible protein kinase	BMP2K	unknown	Kd 8.66
Potassium voltage-gated channel subfamily H member 2	KCNH2	unknown	IC50 8.59
Mast/stem cell growth factor receptor Kit	KIT	unknown	Kd 8.57
Serine/threonine-protein kinase PknB	pknB	unknown	Kd 8.44
Mitogen-activated protein kinase kinase kinase 7	MAP3K7	unknown	Kd 8.39
High affinity nerve growth factor receptor	NTRK1	unknown	Kd 8.35
Tyrosine-protein kinase JAK1	JAK1	unknown	Kd 8.32
Maternal embryonic leucine zipper kinase	MELK	unknown	Kd 8.31
Vascular endothelial growth factor receptor 3	FLT4	inhibitor	IC50 8.30
Vascular endothelial growth factor receptor 2	KDR	inhibitor	IC50 8.30
Mitogen-activated protein kinase kinase kinase 19	MAP3K19	unknown	Kd 8.28
Tyrosine-protein kinase Lck	LCK	unknown	Kd 8.21
Tyrosine-protein kinase JAK3	JAK3	unknown	Kd 8.09
Serine/threonine-protein kinase PRP4 homolog	PRPF4B	unknown	Kd 8.08
Tyrosine-protein kinase Mer	MERTK	unknown	Kd 8.07
Dual specificity protein kinase CLK1	CLK1	unknown	Kd 8.06
Serine/threonine-protein kinase 4	STK4	unknown	Kd 8.05
Mitogen-activated protein kinase kinase kinase 2	MAP3K2	unknown	Kd 8.03

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2015-07-03	PMDA	—	Boehringer Ingelheim	Yes
2014-11-20	EMA	—	Boehringer Ingelheim International GmbH	Yes
2014-10-15	FDA	—	BOEHRINGER INGELHEIM	Yes

ATC classification

ATC code	Therapeutic hierarchy
L01EX09	ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Other protein kinase inhibitors

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
Diarrhoea	3438.3
Death	1460.6
Malignant neoplasm progression	843.4
Decreased appetite	718.8
Weight decreased	522.8
Nausea	489.4
Pneumothorax	438.0
Dyspnoea	353.0
Lung transplant	318.5
Cough	309.5
Respiratory failure	278.8
Idiopathic pulmonary fibrosis	255.6

Chemical structure

• Molecular formula: C₃₁H₃₃N₅O₄
• Molecular weight: 539.64 g/mol
• CAS number: 656247-17-5
• InChIKey: XZXHXSATPCNXJR-ZIADKAODSA-N
• PubChem CID: 135423438

COC(=O)C1=CC2=C(C=C1)\C(=C(\NC1=CC=C(C=C1)N(C)C(=O)CN1CCN(C)CC1)C1=CC=CC=C1)C(=O)N2

Frequently asked questions

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

What is Nintedanib used for?

DrugCentral lists the following indications for Nintedanib: Idiopathic pulmonary fibrosis, Interstitial fibrosis, Non-small cell lung cancer and Systemic sclerosis associated interstitial lung disease.

How does Nintedanib work?

Nintedanib is classified as Protein Kinase Inhibitors; its molecular targets in DrugCentral include FLT3, MAP2K5, BMP2K and KCNH2.

When was Nintedanib first approved?

Nintedanib was first approved by the FDA in 2014.

What drug class does Nintedanib belong to?

Nintedanib is in the Kinase Inhibitor class.

What is the chemical formula of Nintedanib?

Nintedanib has the molecular formula C31H33N5O4 and a molecular weight of 539.64 g/mol.

Sources

• DrugCentral drug card 4903 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL3039504 — compound record and bioactivity
• PubChem CID 135423438 — chemical identifiers
• DrugBank DB09079 — drug record
• FDA UNII G6HRD2P839 — substance identity
• DailyMed: FDA labels for Nintedanib — current prescribing information (label search)
• UniProt P36888 (FLT3) — target protein
• UniProt Q13163 (MAP2K5) — target protein
• UniProt Q9NSY1 (BMP2K) — target protein
• UniProt Q12809 (KCNH2) — target protein
• UniProt P10721 (KIT) — target protein
• UniProt O43318 (MAP3K7) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

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