Nintedanib

Highest phase reached

Approved

www.ebi.ac.uk

Drug type

Small molecule

www.ebi.ac.uk

First approval year

2014

www.ebi.ac.uk

First approval year: 2014
www.ebi.ac.uk

Listing at source: Listed

Highest phase reached: Approved
www.ebi.ac.uk

Drug type: Small molecule
www.ebi.ac.uk

Drug name: Nintedanib
www.ebi.ac.uk

Molecular weight: 539.64
www.ebi.ac.uk

Structure (SMILES): COC(=O)c1ccc2c(c1)NC(=O)/C2=C(\Nc1ccc(N(C)C(=O)CN2CCN(C)CC2)cc1)c1ccccc1
www.ebi.ac.uk

nintedanib component of ofev
Nintedanib component of ofev
ofev
Ofev
vargatef
Vargatef

alks 9072 low
bibf 1120
BIBF 1120
BIBF 1120 (high)
BIBF 1120 (low)
BIBF 1120 (medium)
bibf 1120 and bibw 2992
bibf 1120 high
bibf 1120 intravenous solution
BIBF 1120 intravenous solution
bibf 1120 low
bibf 1120 m
BIBF 1120 M
bibf 1120 m docetaxel m
bibf 1120 m pemetrexed
bibf 1120 medium
bibf 1120 plus docetaxel
bibf 1120 rd
BIBF 1120 RD
bibf 1120 rd pemetrexed
Bibf-1120
BIBF-1120
bibf1120
BIBF1120
egcg 300 mg nintedanib

And 39 more, listed on the interactive page.

CAS registry numbers

656247-17-5

ChEMBL ID: CHEMBL502835
www.ebi.ac.uk

InChIKey: XZXHXSATPCNXJR-ZIADKAODSA-N
www.ebi.ac.uk

PubChem compound IDs

9809715

RxNorm IDs (RxCUI)

1592737

FDA ingredient codes (UNII)

G6HRD2P839

L01EX09
L01XE3

Sources for recorded values

www.ebi.ac.uk

Applicant: CIPLA
Approval date: 2 Apr 2026
Application number: ANDA212609

Status: Authorised
Status date: 21 Nov 2014
Authorisation date: 21 Nov 2014
Approved indications: Vargatef is indicated in combination with docetaxel for the treatment of adult patients with locally advanced, metastatic or locally recurrent non-small cell lung cancer (NSCLC) of adenocarcinoma tumour histology after first line chemotherapy.
Product number: EMEA/H/C/002569
Authorisation holder: Boehringer Ingelheim International GmbH
Priority medicines scheme: No
Generic: No
Biosimilar: No
Generic medicines: 2
Biosimilar medicines: 0
Advanced therapy: No
Conditional approval: No
Additional monitoring: No
Accelerated assessment: No
Exceptional circumstances: No

Therapeutic areas

Carcinoma, Non-Small-Cell Lung

European medicines record

www.ema.europa.eu

Patents: 0
Designations: 7
First in class: Yes
Fast track: Yes
Breakthrough designation: Yes
Orphan designation: No
Priority review: Yes
Orphan exclusivity: No
Accelerated approval: No
Availability: Prescription only

United States (FDA): Approved
European Union (EMA): Authorised

Pharmacology name: nintedanib
Type: Synthetic organic
Drug name stem: -anib
Approval recorded by Guide to Pharmacology: Yes

Administration routes

Oral

Action
Inhibition
Action type
Inhibitor
Target
large tumor suppressor kinase 1
Gene symbol
LATS1
Protein identifier
O95835
Median affinity
4.97
Affinity units
pKd
Action
Inhibition
Action type
Inhibitor
Target
platelet derived growth factor receptor beta
Gene symbol
PDGFRB
Protein identifier
P09619
Median affinity
7.19
Affinity units
pIC50
Action
Inhibition
Action type
Inhibitor
Target
fibroblast growth factor receptor 1
Gene symbol
FGFR1
Protein identifier
P11362
Median affinity
7.16
Affinity units
pIC50
Action
Inhibition
Action type
Inhibitor
Target
platelet derived growth factor receptor alpha
Gene symbol
PDGFRA
Protein identifier
P16234
Median affinity
7.23
Affinity units
pIC50
Action
Inhibition
Action type
Inhibitor
Target
fms related receptor tyrosine kinase 1
Gene symbol
FLT1
Protein identifier
P17948
Median affinity
7.51
Affinity units
pIC50
Action
Inhibition
Action type
Inhibitor
Target
fibroblast growth factor receptor 2
Gene symbol
FGFR2
Protein identifier
P21802
Median affinity
7.43
Affinity units
pIC50
Action
Inhibition
Action type
Inhibitor
Target
fibroblast growth factor receptor 4
Gene symbol
FGFR4
Protein identifier
P22455
Median affinity
6.21
Affinity units
pIC50
Action
Inhibition
Action type
Inhibitor
Target
fibroblast growth factor receptor 3
Gene symbol
FGFR3
Protein identifier
P22607
Median affinity
6.97
Affinity units
pIC50
Action
Inhibition
Action type
Inhibitor
Target
fms related receptor tyrosine kinase 4
Gene symbol
FLT4
Protein identifier
P35916
Median affinity
7.89
Affinity units
pIC50
Primary target
Yes
Action
Inhibition
Action type
Inhibitor
Target
kinase insert domain receptor
Gene symbol
KDR
Protein identifier
P35968
Median affinity
7.68
Affinity units
pIC50

Mechanism
Fibroblast growth factor receptor inhibitor
Action type
Inhibitor
Target
Fibroblast growth factor receptor
Mechanism
Platelet-derived growth factor receptor inhibitor
Action type
Inhibitor
Target
Platelet-derived growth factor receptor
Mechanism
Vascular endothelial growth factor receptor inhibitor
Action type
Inhibitor
Target
Vascular endothelial growth factor receptor

Action type
Agonist
Gene symbol
INSR
Protein identifier
P06213
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
PDGFRB
Protein identifier
P09619
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
FGFR1
Protein identifier
P11362
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
PDGFRA
Protein identifier
P16234
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
FLT1
Protein identifier
P17948
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
FGFR2
Protein identifier
P21802
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
FGFR4
Protein identifier
P22455
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
FGFR3
Protein identifier
P22607
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
FLT4
Protein identifier
P35916
Organism
Homo sapiens
Target development level
Clinical
Action type
Inhibitor
Gene symbol
KDR
Protein identifier
P35968
Organism
Homo sapiens
Target development level
Clinical

Condition
Carcinoma, Hepatocellular
Highest recorded phase
2
Condition identifier
EFO:0000182
Subject identifier
D006528
Condition
Leukemia, Myeloid, Acute
Highest recorded phase
2
Condition identifier
EFO:0000222
Subject identifier
D015470
Condition
Colorectal Neoplasms
Highest recorded phase
3
Condition identifier
EFO:0000365
Subject identifier
D015179
Condition
Melanoma
Highest recorded phase
1
Condition identifier
EFO:0000389
Subject identifier
D008545
Condition
Stomach Neoplasms
Highest recorded phase
2
Condition identifier
EFO:0000503
Subject identifier
D013274
Condition
Glioblastoma
Highest recorded phase
2
Condition identifier
EFO:0000519
Subject identifier
D005909
Condition
Adenocarcinoma of Lung
Highest recorded phase
1
Condition identifier
EFO:0000571
Subject identifier
D000077192
Condition
Mesothelioma
Highest recorded phase
2
Condition identifier
EFO:0000588
Subject identifier
D008654
Condition
Neoplasms
Highest recorded phase
3
Condition identifier
EFO:0000616
Subject identifier
D009369
Condition
Prostatic Neoplasms
Highest recorded phase
2
Condition identifier
EFO:0000673
Subject identifier
D011471
Condition
Carcinoma, Renal Cell
Highest recorded phase
2
Condition identifier
EFO:0000681
Subject identifier
D002292
Condition
Sarcoma
Highest recorded phase
2
Condition identifier
EFO:0000691
Subject identifier
D012509
Condition
Small Cell Lung Carcinoma
Highest recorded phase
2
Condition identifier
EFO:0000702
Subject identifier
D055752
Condition
Carcinoma, Squamous Cell
Highest recorded phase
2
Condition identifier
EFO:0000708
Subject identifier
D002294
Condition
Scleroderma, Systemic
Highest recorded phase
3
Condition identifier
EFO:0000717
Subject identifier
D012595
Condition
Idiopathic Pulmonary Fibrosis
Highest recorded phase
3
Condition identifier
EFO:0000768
Subject identifier
D054990
Condition
Mesothelioma
Highest recorded phase
2
Condition identifier
EFO:0000770
Subject identifier
D008654
Condition
Multiple Myeloma
Highest recorded phase
1
Condition identifier
EFO:0001378
Subject identifier
D009101
Condition
Uterine Cervical Neoplasms
Highest recorded phase
2
Condition identifier
EFO:0001416
Subject identifier
D002583
Condition
Astrocytoma
Highest recorded phase
2
Condition identifier
EFO:0002499
Subject identifier
D001254
Condition
Oligodendroglioma
Highest recorded phase
2
Condition identifier
EFO:0002501
Subject identifier
D009837
Condition
Pancreatic Neoplasms
Highest recorded phase
1
Condition identifier
EFO:0002618
Subject identifier
D010190
Condition
Carcinoma, Non-Small-Cell Lung
Highest recorded phase
3
Condition identifier
EFO:0003060
Subject identifier
D002289
Condition
Ovarian Neoplasms
Highest recorded phase
2
Condition identifier
EFO:0003893
Subject identifier
D010051
Condition
Colorectal Neoplasms
Highest recorded phase
3
Condition identifier
EFO:0004142
Subject identifier
D015179

And 25 more, listed on the interactive page.

Condition identifier
EFO_0000182
Highest recorded phase
2
Condition identifier
EFO_0000222
Highest recorded phase
2
Condition identifier
EFO_0000503
Highest recorded phase
2
Condition identifier
EFO_0000519
Highest recorded phase
2
Condition identifier
EFO_0000571
Condition identifier
EFO_0000588
Highest recorded phase
3
Condition identifier
EFO_0000616
Condition identifier
EFO_0000673
Highest recorded phase
2
Condition identifier
EFO_0000681
Highest recorded phase
2
Condition identifier
EFO_0000702
Highest recorded phase
2
Condition identifier
EFO_0000717
Condition identifier
EFO_0000768
Condition identifier
EFO_0000768
Highest recorded phase
4
Condition identifier
EFO_0000770
Highest recorded phase
2
Condition identifier
EFO_0001378
Highest recorded phase
1
Condition identifier
EFO_0001416
Highest recorded phase
2
Condition identifier
EFO_0002618
Condition identifier
EFO_0003060
Condition identifier
EFO_0003893
Highest recorded phase
2
Condition identifier
EFO_0003895
Highest recorded phase
2
Condition identifier
EFO_0004142
Highest recorded phase
3
Condition identifier
EFO_0004243
Highest recorded phase
2
Condition identifier
EFO_0004244
Condition identifier
EFO_0006890
Condition identifier
EFO_0007183
Highest recorded phase
2

And 68 more, listed on the interactive page.

Event
abdominal discomfort
Reports
151
Reporting signal score
81.2214
Event
abnormal loss of weight
Reports
48
Reporting signal score
98.581
Event
constipation
Reports
223
Reporting signal score
107.471
Event
cough
Reports
279
Reporting signal score
125.049
Event
decreased appetite
Reports
464
Reporting signal score
502.594
Event
diarrhoea
Reports
1,586
Reporting signal score
1,853.09
Event
drug hypersensitivity
Reports
5
Reporting signal score
91.8867
Event
dyspnoea
Reports
518
Reporting signal score
172.993
Event
dyspnoea exertional
Reports
88
Reporting signal score
82.234
Event
faeces soft
Reports
45
Reporting signal score
105.651
Event
flatulence
Reports
89
Reporting signal score
99.9065
Event
forced vital capacity decreased
Reports
26
Reporting signal score
88.9126
Event
idiopathic pulmonary fibrosis
Reports
355
Reporting signal score
1,739.8
Event
interstitial lung disease
Reports
123
Reporting signal score
101.363
Event
liver disorder
Reports
108
Reporting signal score
103.347
Event
lung transplant
Reports
52
Reporting signal score
124.985
Event
malignant neoplasm progression
Reports
236
Reporting signal score
287.966
Event
nausea
Reports
726
Reporting signal score
255.538
Event
oxygen saturation decreased
Reports
104
Reporting signal score
82.6226
Event
pneumothorax
Reports
130
Reporting signal score
262.286
Event
productive cough
Reports
101
Reporting signal score
111.508
Event
pulmonary embolism
Reports
162
Reporting signal score
97.5831
Event
pulmonary hypertension
Reports
74
Reporting signal score
95.7615
Event
vomiting
Reports
440
Reporting signal score
131.469
Event
weight decreased
Reports
430
Reporting signal score
388.496

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And 75 more, listed on the interactive page.

Dose: 150mg
Route: Oral
How often: Twice daily approximately 12 hours apart

Do not chew or crush
Swallow whole with liquid
Take with food

Hydrogen bond acceptors: 7
Hydrogen bond donors: 2
Polar surface area: 94.22
Calculated partition coefficient (ALogP): 3.62
Calculated partition coefficient (XLogP): 3.3
Prodrug: No
Chirality: Achiral
Inorganic: No
Rule-of-five violations: 1
Rotatable bonds: 7
Heavy atoms: 40
Molecular formula: C31H33N5O4
Monoisotopic mass: 539.25325455
Natural product: Yes

These details could not be displayed.

Related records

Trials (176)

A Dose Escalation Study of BIBF 1120 Together With Paclitaxel and Carboplatin in Patients With Advanced Stage Non-small-cell Lung Cancer
A Dose-escalation Study of BIBF 1120 in Japanese Patients With Advanced Solid Tumours
A Drug-Drug Interaction Study of ENV-101 (Taladegib) on Nintedanib Pharmacokinetics in Healthy Subjects
A Follow-up Study Investigating Long Term Treatment With Nintedanib in Patients With Progressive Fibrosing Interstitial Lung Disease (PF-ILD)
A Multi-centre 3-arm Randomised Phase II Trial of BIBF 1120 Versus BIBW 2992 Versus Sequential Administration of BIBF 1120 and BIBW 2992 in Patients With Hormone-resistant Prostate Cancer
A Phase I / II Trial of Nintedanib in Asian Hepatocellular Carcinoma Patients
A Phase I/II Open Label Extension Study of BIBF 1120 Administered Orally Once or Twice Daily to Establish Safety, Pharmacokinetics and Efficacy in Patients With Advanced Solid Tumours and Clinical Benefit From Previous Therapy With BIBF 1120
A Phase I/II Study of Continuous Oral Treatment With BIBF 1120 Added to Standard Gemcitabine/Cisplatin Therapy in First Line NSCLC Patients With Squamous Cell Histology.
A Phase II Trial of Weekly Alternating Sequential Administration of BIBF 1120 and BIBW 2992 in Patients With Advanced Colorectal Cancer
A Prospective, Multicenter Exploratory Clinical Study on Consolidation Therapy With Tislelizumab Combined With Nintedanib for Limited-stage Small Cell Lung Cancer
A Randomised Placebo-Controlled Phase II Study of Continuous Maintenance Treatment With BIBF 1120 Following Chemotherapy in Patients With Relapsed Ovarian Cancer
A Study Based on Medical Records in Spain That Looks at Diarrhoea Control in People With Pulmonary Fibrosis Who Are Taking Nintedanib
A Study Based on Medical Records That Looks at the Characteristics of Idiopathic Pulmonary Fibrosis Patients Grouped by the Type of Medication They Are Taking
A Study in Healthy Men to Find the Best Formulation for Once Daily Intake of Nintedanib
A Study in Healthy Men to Test Whether BI 1015550 Influences the Amount of Nintedanib and Pirfenidone in the Blood
A Study in Healthy Men to Test Whether Four Capsules of 25 mg Nintedanib Are Taken up in the Body in the Same Way as One 100 mg Capsule
A Study of Nintedanib for LymphAngioleioMyomatosis (LAM)
A Study of the Pharmacokinetic Interaction Between Pirfenidone, Nintedanib, and Nalbuphine Extended Release (NAL ER) in Healthy Participants
A Study to Assess the Effect of AZD5055 on the Pharmacokinetics (PK) of Nintedanib in Healthy Participants.
A Study to Assess the Extent of Drug Interaction Between BMS-986278 and Nintedanib, the Relative Bioavailability of BMS-986278 in Tablet and the Effect That Food Has on BMS-986278 in Tablet Formulations in Healthy Participants

In development for (78)

Acute myeloid leukemia Phase 2
Adenocarcinoma Phase 3
Adenomyosis Phase 3
Anaplastic astrocytoma Phase 2
Anaplastic oligodendroglioma Phase 2
Anthracosis Phase 2
Appendix cancer Phase 2
Asbestosis Phase 2
Breast cancer Phase 2
Breast carcinoma Phase 2
Bronchiolitis obliterans syndrome Phase 2
Cancer Phase 1
Carcinoid tumor Phase 2
Castleman disease Phase 2
Cervical adenocarcinoma Phase 2
Cervical cancer Phase 2
Colon adenocarcinoma Phase 1
Colorectal adenocarcinoma Phase 3
Colorectal cancer Phase 3
Colorectal neoplasm Phase 3

Targets (11)

FGFR1 Fibroblast growth factor receptor inhibitor
FGFR2 Fibroblast growth factor receptor inhibitor
FGFR3 Fibroblast growth factor receptor inhibitor
FGFR4 Fibroblast growth factor receptor inhibitor
FLT1 Vascular endothelial growth factor receptor inhibitor
FLT4 Vascular endothelial growth factor receptor inhibitor
INSR
KDR Vascular endothelial growth factor receptor inhibitor
LATS1
PDGFRA Platelet-derived growth factor receptor inhibitor
PDGFRB Platelet-derived growth factor receptor inhibitor

Nintedanib

Development status

Names and chemistry

Brand names (6)

Other names (64)

Identifiers

ATC classification codes (2)

Regulatory information

United States

European Union

Therapeutic areas

Other regulatory facts

Approval status

Pharmacology

Drug classification

Administration routes

Mechanisms of action (10)

Open Targets mechanisms (3)

DrugCentral mechanisms (10)

Investigated indications (50)

Open Targets indications (93)

Reported adverse events (25)

Trial references (100)

Dosing

Conditions of use (3)

Chemical properties

Biological measurements

Related records

Trials (176)

In development for (78)

Targets (11)