Identification

Name
Nintedanib
Accession Number
DB09079
Type
Small Molecule
Groups
Approved
Description

Nintedanib is a drug indicated for the treatment of idiopathic pulmonary fibrosis (IPF) that targets multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs). Nintedanib inhibits the following RTKs: platelet-derived growth factor receptor (PDGFR) α and β, fibroblast growth factor receptor (FGFR) 1-3, vascular endothelial growth factor receptor (VEGFR) 1-3, and Fms-like tyrosine kinase-3 (FLT3). Among them, FGFR, PDGFR, and VEGFR have been implicated in IPF pathogenesis. Nintedanib binds competitively to the adenosine triphosphate (ATP) binding pocket of these receptors and blocks the intracellular signaling which is crucial for the proliferation, migration, and transformation of fibroblasts representing essential mechanisms of the IPF pathology. In addition, nintedanib inhibits the following nRTKs: Lck, Lyn and Src kinases. The contribution of FLT3 and nRTK inhibition to IPF efficacy is unknown.

Idiopathic pulmonary fibrosis (IPF) is a progressive and ultimately fatal lung disease characterized by a progressive loss of lung function with worsening dyspnoea and cough. Development is thought to be instigated by repetitive lung injury (such as by cigarette smoke, industrial dusts, gastrooesophageal reflux and viral infection) leading to destruction of epithelial alveolar cells. Subsequent dysregulation of the repair process results in the proliferation/migration of fibroblasts and their differentiation into myofibroblasts, abnormal extracellular matrix deposition and excessive collagen accumulation in the lung interstitium and alveolar space, leading to progressive fibrosis and stiffening of the lungs. Vascular endothelial growth factor (VEGF), fibroblast growth factor (FGF) and platelet-derived growth factor (PDGF) mediate various processes, including fibrogenesis and angiogenesis, and are implicated in the pathogenesis of IPF. By blocking substrate binding and downstream signalling cascades, nintedanib interferes with processes active in fibrosis such as fibroblast proliferation, migration and differentiation, and the secretion of extracellular matrix.

Structure
Thumb
Synonyms
  • methyl (3Z)-3-[(4-{methyl[(4-methylpiperazin-1-yl)acetyl]amino}anilino)(phenyl)methylidene]-2-oxo-2,3-dihydro-1H-indole-6-carboxylate
External IDs
BIBF 1120 / BIBF-1120 / BIBF1120
Product Ingredients
IngredientUNIICASInChI Key
Nintedanib Esylate42F62RTZ4G656247-18-6MMMVNAGRWOJNMW-FJBFXRHMSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
OfevCapsule100 mgOralBoehringer Ingelheim (Canada) Ltd Ltee2015-06-29Not applicableCanada
OfevCapsule150 mg/1OralBoehringer Ingelheim2014-10-15Not applicableUs
OfevCapsule150 mgOralBoehringer Ingelheim (Canada) Ltd Ltee2015-06-29Not applicableCanada
OfevCapsule100 mg/1OralBoehringer Ingelheim2014-10-15Not applicableUs
International/Other Brands
Vargatef (Boehringer-Ingelheim)
Categories
UNII
G6HRD2P839
CAS number
656247-17-5
Weight
Average: 539.6248
Monoisotopic: 539.253254569
Chemical Formula
C31H33N5O4
InChI Key
XZXHXSATPCNXJR-ZIADKAODSA-N
InChI
InChI=1S/C31H33N5O4/c1-34-15-17-36(18-16-34)20-27(37)35(2)24-12-10-23(11-13-24)32-29(21-7-5-4-6-8-21)28-25-14-9-22(31(39)40-3)19-26(25)33-30(28)38/h4-14,19,32H,15-18,20H2,1-3H3,(H,33,38)/b29-28-
IUPAC Name
methyl (3Z)-2-hydroxy-3-[({4-[N-methyl-2-(4-methylpiperazin-1-yl)acetamido]phenyl}amino)(phenyl)methylidene]-3H-indole-6-carboxylate
SMILES
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

Pharmacology

Indication

Nintedanib is indicated for the treatment of idiopathic pulmonary fibrosis (IPF).

Structured Indications
Pharmacodynamics

By competitively and reversibly inhibiting the adenosine triphosphate binding pocket of the receptor tyrosine kinases VEGFR, FGFR and PDGFR, nintedanib blocks the intracellular signalling needed for the proliferation, migration and transformation of fibroblasts.

Mechanism of action

Nintedanib is a small molecule that targets multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs). Nintedanib inhibits the following RTKs: platelet-derived growth factor receptor (PDGFR) α and β, fibroblast growth factor receptor (FGFR) 1-3, vascular endothelial growth factor receptor (VEGFR) 1-3, and Fms-like tyrosine kinase-3 (FLT3). Among them, FGFR, PDGFR, and VEGFR have been implicated in IPF pathogenesis. Nintedanib binds competitively to the adenosine triphosphate (ATP) binding pocket of these receptors and blocks the intracellular signaling which is crucial for the proliferation, migration, and transformation of fibroblasts representing essential mechanisms of the IPF pathology. In addition, nintedanib inhibits the following nRTKs: Lck, Lyn and Src kinases. The contribution of FLT3 and nRTK inhibition to IPF efficacy is unknown.

TargetActionsOrganism
AVascular endothelial growth factor receptor 1
inhibitor
Human
AVascular endothelial growth factor receptor 2
inhibitor
Human
AVascular endothelial growth factor receptor 3
inhibitor
Human
APlatelet derived growth factor receptor alpha
inhibitor
Human
APlatelet derived growth factor receptor beta
inhibitor
Human
AFibroblast growth factor receptor 1
inhibitor
Human
AFibroblast growth factor receptor 2
inhibitor
Human
AFibroblast growth factor receptor 3
inhibitor
Human
UReceptor-type tyrosine-protein kinase FLT3
inhibitor
Human
UTyrosine-protein kinase Lck
inhibitor
Human
UTyrosine-protein kinase Lyn
inhibitor
Human
UProto-oncogene tyrosine-protein kinase Src
inhibitor
Human
Absorption

Nintedanib reaches maximum plasma concentrations approximately 2 to 4 hours after administration, and absolute bioavailability is 4.7%.

Volume of distribution

1050 L

Protein binding

The in vitro protein binding of nintedanib in human plasma was high, with a bound fraction of 97.8%. Serum albumin is considered to be the major binding protein.

Metabolism

The prevalent metabolic reaction for nintedanib is hydrolytic cleavage by esterases resulting in the free acid moiety BIBF 1202. BIBF 1202 is subsequently glucuronidated by UGT enzymes, namely UGT 1A1, UGT 1A7, UGT 1A8, and UGT 1A10 to BIBF 1202 glucuronide. Only a minor extent of the biotransformation of nintedanib consisted of CYP pathways, with CYP 3A4 being the predominant enzyme involved. In vitro, CYP-dependent metabolism accounted for about 5% compared to about 25% ester cleavage.

Route of elimination

The major route of elimination of drug-related radioactivity after oral administration of [14C] nintedanib was via fecal/biliary excretion (93.4% of dose), and the majority was excreted as BIBF 1202. The contribution of renal excretion to the total clearance was low (0.65% of dose). The overall recovery was considered complete (above 90%) within 4 days after dosing.

Half life

9.5 hours

Clearance

Total plasma clearance after intravenous infusion was found to be 1390 mL/min, while renal clearance was found to be 20 mL/min.

Toxicity

The most common adverse reactions (>5%) reported during clinical trials include diarrhea, nausea, vomiting, abdominal pain, liver enzyme elevation, headache, decreased weight, decreased appetite, and hypertension. The most frequent serious adverse reactions reported in patients treated with nintedanib, more than placebo, were bronchitis (1.2% vs. 0.8%) and myocardial infarction (1.5% vs. 0.4%). The most common adverse events leading to death in patients treated with nintedanib, more than placebo, were pneumonia (0.7% vs. 0.6%), lung neoplasm malignant (0.3% vs. 0%), and myocardial infarction (0.3% vs. 0.2%). Nintedanib can also cause fetal harm when administered to a pregnant woman: if it is used during pregnancy, or if the patient becomes pregnant while taking nintedanib, the patient should be apprised of the potential hazard to a fetus. Women of childbearing potential should be advised to avoid becoming pregnant while receiving treatment.

Affected organisms
Not Available
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Nintedanib.Approved
AcenocoumarolThe risk or severity of adverse effects can be increased when Acenocoumarol is combined with Nintedanib.Approved
AcetaminophenThe serum concentration of Nintedanib can be increased when it is combined with Acetaminophen.Approved
AcetyldigitoxinAcetyldigitoxin may decrease the cardiotoxic activities of Nintedanib.Approved
AcetyldigoxinAcetyldigoxin may decrease the cardiotoxic activities of Nintedanib.Experimental
AmiodaroneThe serum concentration of Nintedanib can be increased when it is combined with Amiodarone.Approved, Investigational
AmlodipineThe serum concentration of Nintedanib can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Nintedanib can be increased when it is combined with Amprenavir.Approved
AncrodThe risk or severity of adverse effects can be increased when Ancrod is combined with Nintedanib.Investigational
Antithrombin III humanThe risk or severity of adverse effects can be increased when Antithrombin III human is combined with Nintedanib.Approved
ApixabanThe risk or severity of adverse effects can be increased when Apixaban is combined with Nintedanib.Approved
ArdeparinThe risk or severity of adverse effects can be increased when Ardeparin is combined with Nintedanib.Approved, Investigational, Withdrawn
ArgatrobanThe risk or severity of adverse effects can be increased when Argatroban is combined with Nintedanib.Approved, Investigational
AstemizoleThe serum concentration of Nintedanib can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of Nintedanib can be increased when it is combined with Atazanavir.Approved, Investigational
AtorvastatinThe serum concentration of Nintedanib can be increased when it is combined with Atorvastatin.Approved
AzelastineThe serum concentration of Nintedanib can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Nintedanib can be increased when it is combined with Azithromycin.Approved
BecaplerminThe risk or severity of adverse effects can be increased when Becaplermin is combined with Nintedanib.Approved, Investigational
BevacizumabBevacizumab may increase the cardiotoxic activities of Nintedanib.Approved, Investigational
BivalirudinThe risk or severity of adverse effects can be increased when Bivalirudin is combined with Nintedanib.Approved, Investigational
BoceprevirThe serum concentration of Nintedanib can be increased when it is combined with Boceprevir.Approved, Withdrawn
BromocriptineThe serum concentration of Nintedanib can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Nintedanib can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
CabazitaxelThe risk or severity of adverse effects can be increased when Cabazitaxel is combined with Nintedanib.Approved
CaffeineThe serum concentration of Nintedanib can be increased when it is combined with Caffeine.Approved
CarbamazepineThe serum concentration of Nintedanib can be decreased when it is combined with Carbamazepine.Approved, Investigational
CaspofunginThe serum concentration of Nintedanib can be increased when it is combined with Caspofungin.Approved
CertoparinThe risk or severity of adverse effects can be increased when Certoparin is combined with Nintedanib.Approved, Investigational
CimetidineThe serum concentration of Nintedanib can be increased when it is combined with Cimetidine.Approved
CiprofloxacinThe serum concentration of Nintedanib can be increased when it is combined with Ciprofloxacin.Approved, Investigational
Citric AcidThe risk or severity of adverse effects can be increased when Citric Acid is combined with Nintedanib.Approved, Nutraceutical, Vet Approved
ClarithromycinThe serum concentration of Nintedanib can be increased when it is combined with Clarithromycin.Approved
ClofazimineThe serum concentration of Nintedanib can be increased when it is combined with Clofazimine.Approved, Investigational
ClotrimazoleThe serum concentration of Nintedanib can be increased when it is combined with Clotrimazole.Approved, Vet Approved
CobicistatThe serum concentration of Nintedanib can be increased when it is combined with Cobicistat.Approved
ColchicineThe serum concentration of Nintedanib can be increased when it is combined with Colchicine.Approved
CrizotinibThe serum concentration of Nintedanib can be increased when it is combined with Crizotinib.Approved
CyclophosphamideCyclophosphamide may increase the cardiotoxic activities of Nintedanib.Approved, Investigational
CyclosporineThe serum concentration of Nintedanib can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
CymarinCymarin may decrease the cardiotoxic activities of Nintedanib.Experimental
Dabigatran etexilateThe risk or severity of adverse effects can be increased when Dabigatran etexilate is combined with Nintedanib.Approved
DalteparinThe risk or severity of adverse effects can be increased when Dalteparin is combined with Nintedanib.Approved
DanaparoidThe risk or severity of adverse effects can be increased when Danaparoid is combined with Nintedanib.Approved, Withdrawn
DarexabanThe risk or severity of adverse effects can be increased when Darexaban is combined with Nintedanib.Investigational
DasatinibThe serum concentration of Nintedanib can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Nintedanib can be increased when it is combined with Daunorubicin.Approved
DesipramineThe serum concentration of Nintedanib can be increased when it is combined with Desipramine.Approved
DesirudinThe risk or severity of adverse effects can be increased when Desirudin is combined with Nintedanib.Approved
DeslanosideDeslanoside may decrease the cardiotoxic activities of Nintedanib.Approved
DexamethasoneThe serum concentration of Nintedanib can be increased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextranThe risk or severity of adverse effects can be increased when Dextran is combined with Nintedanib.Approved, Vet Approved
Dextran 40The risk or severity of adverse effects can be increased when Dextran 40 is combined with Nintedanib.Approved
Dextran 70The risk or severity of adverse effects can be increased when Dextran 70 is combined with Nintedanib.Approved
Dextran 75The risk or severity of adverse effects can be increased when Dextran 75 is combined with Nintedanib.Approved
DicoumarolThe risk or severity of adverse effects can be increased when Dicoumarol is combined with Nintedanib.Approved
DigitoxinDigitoxin may decrease the cardiotoxic activities of Nintedanib.Approved, Investigational
DigoxinDigoxin may decrease the cardiotoxic activities of Nintedanib.Approved
Digoxin Immune Fab (Ovine)Digoxin Immune Fab (Ovine) may decrease the cardiotoxic activities of Nintedanib.Approved
DihydroergotamineThe serum concentration of Nintedanib can be increased when it is combined with Dihydroergotamine.Approved
DiltiazemThe serum concentration of Nintedanib can be increased when it is combined with Diltiazem.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Nintedanib.Approved, Investigational
DoxorubicinThe serum concentration of Nintedanib can be increased when it is combined with Doxorubicin.Approved, Investigational
DronedaroneThe serum concentration of Nintedanib can be increased when it is combined with Dronedarone.Approved
Edetic AcidThe risk or severity of adverse effects can be increased when Edetic Acid is combined with Nintedanib.Approved, Vet Approved
EdoxabanThe risk or severity of adverse effects can be increased when Edoxaban is combined with Nintedanib.Approved
EnasidenibThe serum concentration of Nintedanib can be increased when it is combined with Enasidenib.Approved
EnoxaparinThe risk or severity of adverse effects can be increased when Enoxaparin is combined with Nintedanib.Approved
ErgonovineThe serum concentration of Nintedanib can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Nintedanib can be increased when it is combined with Ergotamine.Approved
ErythromycinThe serum concentration of Nintedanib can be increased when it is combined with Erythromycin.Approved, Vet Approved
Ethyl biscoumacetateThe risk or severity of adverse effects can be increased when Ethyl biscoumacetate is combined with Nintedanib.Withdrawn
EtoposideThe serum concentration of Nintedanib can be increased when it is combined with Etoposide.Approved
FelodipineThe serum concentration of Nintedanib can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Nintedanib can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
Ferulic acidThe risk or severity of adverse effects can be increased when Ferulic acid is combined with Nintedanib.Experimental
FluconazoleThe serum concentration of Nintedanib can be increased when it is combined with Fluconazole.Approved
FluindioneThe risk or severity of adverse effects can be increased when Fluindione is combined with Nintedanib.Investigational
FluoxetineThe serum concentration of Nintedanib can be increased when it is combined with Fluoxetine.Approved, Vet Approved
FluvoxamineThe serum concentration of Nintedanib can be increased when it is combined with Fluvoxamine.Approved, Investigational
FondaparinuxThe risk or severity of adverse effects can be increased when Fondaparinux is combined with Nintedanib.Investigational
Fondaparinux sodiumThe risk or severity of adverse effects can be increased when Fondaparinux sodium is combined with Nintedanib.Approved, Investigational
GabexateThe risk or severity of adverse effects can be increased when Gabexate is combined with Nintedanib.Investigational
GitoformateGitoformate may decrease the cardiotoxic activities of Nintedanib.Experimental
GlyburideThe serum concentration of Nintedanib can be increased when it is combined with Glyburide.Approved
HaloperidolThe serum concentration of Nintedanib can be increased when it is combined with Haloperidol.Approved
HeparinThe risk or severity of adverse effects can be increased when Heparin is combined with Nintedanib.Approved, Investigational
HydrocortisoneThe serum concentration of Nintedanib can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
IdelalisibThe serum concentration of Nintedanib can be increased when it is combined with Idelalisib.Approved
IdraparinuxThe risk or severity of adverse effects can be increased when Idraparinux is combined with Nintedanib.Investigational
ImatinibThe serum concentration of Nintedanib can be increased when it is combined with Imatinib.Approved
IndinavirThe serum concentration of Nintedanib can be increased when it is combined with Indinavir.Approved
IsavuconazoniumThe serum concentration of Nintedanib can be increased when it is combined with Isavuconazonium.Approved, Investigational
ItraconazoleThe serum concentration of Nintedanib can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Nintedanib can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe serum concentration of Nintedanib can be increased when it is combined with Ketoconazole.Approved, Investigational
Lanatoside CLanatoside C may decrease the cardiotoxic activities of Nintedanib.Experimental
LansoprazoleThe serum concentration of Nintedanib can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Nintedanib can be increased when it is combined with Lapatinib.Approved, Investigational
LepirudinThe risk or severity of adverse effects can be increased when Lepirudin is combined with Nintedanib.Approved
LetaxabanThe risk or severity of adverse effects can be increased when Letaxaban is combined with Nintedanib.Investigational
LevofloxacinThe serum concentration of Nintedanib can be increased when it is combined with Levofloxacin.Approved, Investigational
LidocaineThe serum concentration of Nintedanib can be increased when it is combined with Lidocaine.Approved, Vet Approved
LomitapideThe serum concentration of Nintedanib can be increased when it is combined with Lomitapide.Approved
LopinavirThe serum concentration of Nintedanib can be increased when it is combined with Lopinavir.Approved
LoratadineThe serum concentration of Nintedanib can be increased when it is combined with Loratadine.Approved
LosartanThe serum concentration of Nintedanib can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Nintedanib can be increased when it is combined with Lovastatin.Approved, Investigational
LumacaftorThe serum concentration of Nintedanib can be decreased when it is combined with Lumacaftor.Approved
MefloquineThe serum concentration of Nintedanib can be increased when it is combined with Mefloquine.Approved
MelagatranThe risk or severity of adverse effects can be increased when Melagatran is combined with Nintedanib.Experimental
MethadoneThe serum concentration of Nintedanib can be increased when it is combined with Methadone.Approved
MetildigoxinMetildigoxin may decrease the cardiotoxic activities of Nintedanib.Experimental
MibefradilThe serum concentration of Nintedanib can be increased when it is combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe serum concentration of Nintedanib can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Nintedanib can be increased when it is combined with Midazolam.Approved, Illicit
MifepristoneThe serum concentration of Nintedanib can be increased when it is combined with Mifepristone.Approved, Investigational
MitoxantroneThe serum concentration of Nintedanib can be increased when it is combined with Mitoxantrone.Approved, Investigational
NadroparinThe risk or severity of adverse effects can be increased when Nadroparin is combined with Nintedanib.Approved
NafamostatThe risk or severity of adverse effects can be increased when Nafamostat is combined with Nintedanib.Approved, Investigational
NelfinavirThe serum concentration of Nintedanib can be increased when it is combined with Nelfinavir.Approved
NicardipineThe serum concentration of Nintedanib can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Nintedanib can be increased when it is combined with Nifedipine.Approved
NilotinibThe serum concentration of Nintedanib can be increased when it is combined with Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Nintedanib can be increased when it is combined with Nisoldipine.Approved
NitrendipineThe serum concentration of Nintedanib can be increased when it is combined with Nitrendipine.Approved, Investigational
OleandrinOleandrin may decrease the cardiotoxic activities of Nintedanib.Experimental, Investigational
OmeprazoleThe serum concentration of Nintedanib can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OtamixabanThe risk or severity of adverse effects can be increased when Otamixaban is combined with Nintedanib.Investigational
OuabainOuabain may decrease the cardiotoxic activities of Nintedanib.Approved
PaclitaxelThe serum concentration of Nintedanib can be increased when it is combined with Paclitaxel.Approved, Vet Approved
Pentaerythritol TetranitrateThe risk or severity of adverse effects can be increased when Pentaerythritol Tetranitrate is combined with Nintedanib.Approved
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Nintedanib.Approved
PeruvosidePeruvoside may decrease the cardiotoxic activities of Nintedanib.Experimental
PhenindioneThe risk or severity of adverse effects can be increased when Phenindione is combined with Nintedanib.Approved, Investigational
PhenobarbitalThe serum concentration of Nintedanib can be decreased when it is combined with Phenobarbital.Approved
PhenprocoumonThe risk or severity of adverse effects can be increased when Phenprocoumon is combined with Nintedanib.Approved, Investigational
PimozideThe serum concentration of Nintedanib can be increased when it is combined with Pimozide.Approved
PirfenidoneThe serum concentration of Nintedanib can be decreased when it is combined with Pirfenidone.Approved, Investigational
PosaconazoleThe serum concentration of Nintedanib can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Nintedanib can be increased when it is combined with Pravastatin.Approved
PrednisoneThe serum concentration of Nintedanib can be increased when it is combined with Prednisone.Approved, Vet Approved
ProgesteroneThe serum concentration of Nintedanib can be increased when it is combined with Progesterone.Approved, Vet Approved
ProscillaridinProscillaridin may decrease the cardiotoxic activities of Nintedanib.Experimental
Protein CThe risk or severity of adverse effects can be increased when Protein C is combined with Nintedanib.Approved
Protein S humanThe risk or severity of adverse effects can be increased when Protein S human is combined with Nintedanib.Approved
ProtocatechualdehydeThe risk or severity of adverse effects can be increased when Protocatechualdehyde is combined with Nintedanib.Approved
QuinidineThe serum concentration of Nintedanib can be increased when it is combined with Quinidine.Approved
QuinineThe serum concentration of Nintedanib can be increased when it is combined with Quinine.Approved
RanitidineThe serum concentration of Nintedanib can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Nintedanib can be increased when it is combined with Ranolazine.Approved, Investigational
RegorafenibThe serum concentration of Nintedanib can be increased when it is combined with Regorafenib.Approved
ReviparinThe risk or severity of adverse effects can be increased when Reviparin is combined with Nintedanib.Approved, Investigational
RifampicinThe serum concentration of Nintedanib can be decreased when it is combined with Rifampicin.Approved
RilpivirineThe serum concentration of Nintedanib can be increased when it is combined with Rilpivirine.Approved
RitonavirThe serum concentration of Nintedanib can be increased when it is combined with Ritonavir.Approved, Investigational
RivaroxabanThe risk or severity of adverse effects can be increased when Rivaroxaban is combined with Nintedanib.Approved
SaquinavirThe serum concentration of Nintedanib can be increased when it is combined with Saquinavir.Approved, Investigational
SertralineThe serum concentration of Nintedanib can be increased when it is combined with Sertraline.Approved
SimeprevirThe serum concentration of Nintedanib can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Nintedanib can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Nintedanib can be increased when it is combined with Sirolimus.Approved, Investigational
SorafenibThe serum concentration of Nintedanib can be increased when it is combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Nintedanib can be decreased when it is combined with St. John's Wort.Investigational, Nutraceutical
SulfinpyrazoneThe serum concentration of Nintedanib can be increased when it is combined with Sulfinpyrazone.Approved
SulodexideThe risk or severity of adverse effects can be increased when Sulodexide is combined with Nintedanib.Approved, Investigational
TacrolimusThe serum concentration of Nintedanib can be increased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Nintedanib can be increased when it is combined with Tamoxifen.Approved
TelaprevirThe serum concentration of Nintedanib can be increased when it is combined with Telaprevir.Approved, Withdrawn
TemsirolimusThe serum concentration of Nintedanib can be increased when it is combined with Temsirolimus.Approved
TerfenadineThe serum concentration of Nintedanib can be increased when it is combined with Terfenadine.Withdrawn
TesmilifeneThe serum concentration of Nintedanib can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Nintedanib can be increased when it is combined with Testosterone.Approved, Investigational
TicagrelorThe serum concentration of Nintedanib can be increased when it is combined with Ticagrelor.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Nintedanib.Approved, Investigational
TroleandomycinThe serum concentration of Nintedanib can be increased when it is combined with Troleandomycin.Approved
TroxerutinThe risk or severity of adverse effects can be increased when Troxerutin is combined with Nintedanib.Investigational
VenlafaxineThe serum concentration of Nintedanib can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Nintedanib can be increased when it is combined with Verapamil.Approved
VinblastineThe serum concentration of Nintedanib can be increased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Nintedanib can be increased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Nintedanib can be increased when it is combined with Vinorelbine.Approved, Investigational
WarfarinThe risk or severity of adverse effects can be increased when Warfarin is combined with Nintedanib.Approved
XimelagatranThe risk or severity of adverse effects can be increased when Ximelagatran is combined with Nintedanib.Approved, Investigational, Withdrawn
Food Interactions
Not Available

References

General References
  1. Keating GM: Nintedanib: A Review of Its Use in Patients with Idiopathic Pulmonary Fibrosis. Drugs. 2015 Jul;75(10):1131-40. doi: 10.1007/s40265-015-0418-6. [PubMed:26063212]
  2. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]
  3. Mazzei ME, Richeldi L, Collard HR: Nintedanib in the treatment of idiopathic pulmonary fibrosis. Ther Adv Respir Dis. 2015 Jun;9(3):121-9. doi: 10.1177/1753465815579365. Epub 2015 Apr 10. [PubMed:25862013]
  4. Stopfer P, Rathgen K, Bischoff D, Ludtke S, Marzin K, Kaiser R, Wagner K, Ebner T: Pharmacokinetics and metabolism of BIBF 1120 after oral dosing to healthy male volunteers. Xenobiotica. 2011 Apr;41(4):297-311. doi: 10.3109/00498254.2010.545452. Epub 2011 Jan 4. [PubMed:21204634]
External Links
KEGG Drug
D10481
PubChem Compound
9809715
PubChem Substance
310265007
ChemSpider
7985471
BindingDB
50026612
ChEBI
85164
ChEMBL
CHEMBL502835
HET
XIN
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Nintedanib
ATC Codes
L01XE31 — Nintedanib
AHFS Codes
  • 48:02.00 — Antifibrotic Agents
PDB Entries
3c7q / 5te0
FDA label
Download (484 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1CompletedNot AvailableMalignant Solid Tumours1
1CompletedTreatmentGenital Neoplasms, Female1
1CompletedTreatmentHealthy Volunteers6
1CompletedTreatmentHepatic Insufficiency1
1CompletedTreatmentHepatocellular,Carcinoma1
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)5
1CompletedTreatmentMultiple Myeloma (MM)1
1CompletedTreatmentNeoplasms4
1CompletedTreatmentProstatic Neoplasms1
1CompletedTreatmentTumors2
1RecruitingOtherLung Cancer Non-Small Cell Cancer (NSCLC)1
1RecruitingTreatmentCancer, Breast1
1RecruitingTreatmentCervical Carcinoma / Colorectal Adenocarcinoma / Non-Squamous Non-Small Cell Lung Cancer / Platinum-refractory Ovarian Carcinoma / Renal Cell Adenocarcinoma1
1RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
1RecruitingTreatmentLung Cancers1
1RecruitingTreatmentPatients With Any Advanced Solid Tumors1
1TerminatedTreatmentCancer, Ovarian1
1, 2Active Not RecruitingTreatmentColon Adenocarcinoma / Rectal Adenocarcinoma / Recurrent Colon Carcinoma / Recurrent Rectal Carcinoma / Stage IVA Colon Cancer / Stage IVA Rectal Cancer / Stage IVB Colon Cancer / Stage IVB Rectal Cancer1
1, 2Not Yet RecruitingTreatmentCancer of Pancreas1
1, 2RecruitingTreatmentCutaneous Malignant Melanoma1
1, 2RecruitingTreatmentRelapsed/Refractory Acute Myeloid Leukemia1
1, 2TerminatedTreatmentGlioblastoma Multiforme1
1, 2Unknown StatusTreatmentLeukemia Acute Myeloid Leukemia (AML)1
2Active Not RecruitingTreatmentCancer, Breast1
2Active Not RecruitingTreatmentCancer, Ovarian / Fallopian Tube Cancer1
2Active Not RecruitingTreatmentCancer, Ovarian / Fallopian Tube Cancer / Malignant Peritoneal Neoplasm1
2Active Not RecruitingTreatmentCarcinoid Tumors / Metastatic Carcinoid Tumors / Neuroendocrine Neoplasms1
2Active Not RecruitingTreatmentEsophagogastric Adenocarcinoma1
2Active Not RecruitingTreatmentRecurrent Non-small Cell Lung Cancer / Squamous Cell Carcinoma of Lung / Stage III Non-Small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer1
2Active Not RecruitingTreatmentRecurrent or Metastatic Salivary Gland Cancer of the Head and Neck1
2Active Not RecruitingTreatmentRenal Cell Adenocarcinoma1
2Active Not RecruitingTreatmentTransitional Cell Carcinoma1
2CompletedNot AvailableIdiopathic Pulmonary Fibrosis (IPF)1
2CompletedPreventionNeoplasms, Ovarian1
2CompletedTreatmentAnaplastic Astrocytoma (AA) / Anaplastic Oligoastrocytoma / Anaplastic Oligodendroglioma (AO) / Glioblastomas / Gliosarcoma1
2CompletedTreatmentCancer, Ovarian1
2CompletedTreatmentEndometrial Adenocarcinomas / Endometrial Adenosquamous Carcinoma / Endometrial Clear Cell Adenocarcinoma / Endometrial Mucinous Adenocarcinoma / Endometrial Serous Adenocarcinoma / Endometrial Squamous Cell Carcinoma / Endometrial Transitional Cell Carcinoma / Endometrial Undifferentiated Carcinoma / Malignant Uterine Corpus Mixed Epithelial and Mesenchymal Neoplasm / Recurrent Uterine Corpus Carcinoma1
2CompletedTreatmentHepatocellular,Carcinoma2
2CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC) / Refractory Small cell lung cancer1
2CompletedTreatmentNeoplasms, Colorectal2
2CompletedTreatmentProstatic Neoplasms2
2CompletedTreatmentPulmonary Fibrosis2
2CompletedTreatmentRecurrent Glioblastoma1
2Not Yet RecruitingTreatmentAppendix Cancer1
2Not Yet RecruitingTreatmentMalignant Pleural Mesothelioma (MPM)1
2RecruitingPreventionHNSCC / Neoplasms, Head and Neck1
2RecruitingSupportive CareRadiation-Induced Pneumonitis / Stage IIA Non-Small Cell Lung Carcinoma / Stage IIB Non-Small Cell Lung Carcinoma / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIb Non-small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer1
2RecruitingTreatmentCancer, Breast1
2RecruitingTreatmentDifferentiated Thyroid Cancer (DTC) / Medullary Thyroid Cancer (MTC)1
2RecruitingTreatmentEndometrial Clear Cell Carcinoma / Ovarian Clear Cell Carcinoma1
2RecruitingTreatmentAdvanced thymic carcinoma / Lung Cancer Metastatic / Lung Cancer Non-Small Cell Cancer (NSCLC) / Lung Cancer Small Cell Lung Cancer (SCLC) / Lung Cancers / Pleural Mesotheliomas1
2RecruitingTreatmentLymphangioleiomyomatosis1
2RecruitingTreatmentNeoplasms, Lung1
2RecruitingTreatmentRecurrent Pleural Malignant Mesothelioma / Stage IV Pleural Mesothelioma1
2RecruitingTreatmentSoft Tissue Sarcoma (STS)1
2RecruitingTreatmentUterine Cervical Neoplasms1
2TerminatedTreatmentNeoplasms, Colorectal1
2WithdrawnTreatmentEsophagogastric Adenocarcinoma / Metastatic Disease / No Previous Chemotherapy for Metastatic Esophagogastric Cancer1
2WithdrawnTreatmentLung Cancer Small Cell Lung Cancer (SCLC) / Platinum-sensitive1
3Active Not RecruitingTreatmentIdiopathic Pulmonary Fibrosis (IPF)1
3CompletedTreatmentAbdominal wall neoplasm / Neoplasms, Ovarian1
3CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
3CompletedTreatmentNeoplasms, Colorectal1
3CompletedTreatmentPulmonary Fibrosis2
3Not Yet RecruitingTreatmentLung Diseases, Interstitial1
3Not Yet RecruitingTreatmentLung-transplant Recipients1
3RecruitingTreatmentIdiopathic Pulmonary Fibrosis (IPF)1
3RecruitingTreatmentLung Diseases, Interstitial1
3RecruitingTreatmentMesothelioma1
3RecruitingTreatmentScleroderma, Systemic1
3TerminatedTreatmentIdiopathic Pulmonary Fibrosis (IPF)1
3TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
4Active Not RecruitingTreatmentIdiopathic Pulmonary Fibrosis (IPF)1
4CompletedTreatmentIdiopathic Pulmonary Fibrosis (IPF)3
Not AvailableActive Not RecruitingNot AvailableIdiopathic Pulmonary Fibrosis (IPF)1
Not AvailableNo Longer AvailableNot AvailableIdiopathic Pulmonary Fibrosis (IPF)2
Not AvailableRecruitingNot AvailablePulmonary Fibrosis1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
CapsuleOral100 mg
CapsuleOral100 mg/1
CapsuleOral150 mg/1
CapsuleOral150 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US7989474No2004-04-062024-04-06Us
US7119093No2004-02-212024-02-21Us
US6762180No2000-12-102020-12-10Us

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0398 mg/mLALOGPS
logP3.29ALOGPS
logP2.4ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)-6.1ChemAxon
pKa (Strongest Basic)15ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area97.71 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity159.85 m3·mol-1ChemAxon
Polarizability59.7 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as indolecarboxylic acids. These are compounds containing a carboxylic acid group linked to an indole.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Indoles and derivatives
Sub Class
Indolecarboxylic acids and derivatives
Direct Parent
Indolecarboxylic acids
Alternative Parents
Alpha amino acids and derivatives / N-piperazineacetamides / Anilides / Indolines / Aniline and substituted anilines / Secondary alkylarylamines / N-methylpiperazines / Vinylogous amides / Tertiary carboxylic acid amides / Methyl esters
show 10 more
Substituents
Indolecarboxylic acid / Alpha-amino acid or derivatives / N-piperazineacetamide / Dihydroindole / Anilide / Aniline or substituted anilines / Secondary aliphatic/aromatic amine / N-methylpiperazine / N-alkylpiperazine / Monocyclic benzene moiety
show 28 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
methyl ester, aromatic amine, enamine, oxindole, aromatic ester, aromatic amide, N-alkylpiperazine (CHEBI:85164)

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Vegf-b-activated receptor activity
Specific Function
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFB and PGF, and plays an essential role in the development of embryonic vasculature, the regulation of angiogenesis, cell ...
Gene Name
FLT1
Uniprot ID
P17948
Uniprot Name
Vascular endothelial growth factor receptor 1
Molecular Weight
150767.185 Da
References
  1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Vascular endothelial growth factor-activated receptor activity
Specific Function
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and ...
Gene Name
KDR
Uniprot ID
P35968
Uniprot Name
Vascular endothelial growth factor receptor 2
Molecular Weight
151525.555 Da
References
  1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Vascular endothelial growth factor-activated receptor activity
Specific Function
Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFC and VEGFD, and plays an essential role in adult lymphangiogenesis and in the development of the vascular network and the cardi...
Gene Name
FLT4
Uniprot ID
P35916
Uniprot Name
Vascular endothelial growth factor receptor 3
Molecular Weight
152755.94 Da
References
  1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]
4. Platelet derived growth factor receptor alpha
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
References
  1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]
5. Platelet derived growth factor receptor beta
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
References
  1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of embryonic development, cell proliferation, differentiation ...
Gene Name
FGFR1
Uniprot ID
P11362
Uniprot Name
Fibroblast growth factor receptor 1
Molecular Weight
91866.935 Da
References
  1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation, migration and apoptosi...
Gene Name
FGFR2
Uniprot ID
P21802
Uniprot Name
Fibroblast growth factor receptor 2
Molecular Weight
92024.29 Da
References
  1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Inhibitor
General Function
Protein tyrosine kinase activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for fibroblast growth factors and plays an essential role in the regulation of cell proliferation, differentiation and apoptosis. Plays an...
Gene Name
FGFR3
Uniprot ID
P22607
Uniprot Name
Fibroblast growth factor receptor 3
Molecular Weight
87708.905 Da
References
  1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Vascular endothelial growth factor-activated receptor activity
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine FLT3LG and regulates differentiation, proliferation and survival of hematopoietic progenitor cells and of dendritic cells...
Gene Name
FLT3
Uniprot ID
P36888
Uniprot Name
Receptor-type tyrosine-protein kinase FLT3
Molecular Weight
112902.51 Da
References
  1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sh2 domain binding
Specific Function
Non-receptor tyrosine-protein kinase that plays an essential role in the selection and maturation of developing T-cells in the thymus and in the function of mature T-cells. Plays a key role in T-ce...
Gene Name
LCK
Uniprot ID
P06239
Uniprot Name
Tyrosine-protein kinase Lck
Molecular Weight
58000.15 Da
References
  1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Receptor signaling protein tyrosine kinase activity
Specific Function
Non-receptor tyrosine-protein kinase that transmits signals from cell surface receptors and plays an important role in the regulation of innate and adaptive immune responses, hematopoiesis, respons...
Gene Name
LYN
Uniprot ID
P07948
Uniprot Name
Tyrosine-protein kinase Lyn
Molecular Weight
58573.595 Da
References
  1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sh3/sh2 adaptor activity
Specific Function
Non-receptor protein tyrosine kinase which is activated following engagement of many different classes of cellular receptors including immune response receptors, integrins and other adhesion recept...
Gene Name
SRC
Uniprot ID
P12931
Uniprot Name
Proto-oncogene tyrosine-protein kinase Src
Molecular Weight
59834.295 Da
References
  1. Hilberg F, Roth GJ, Krssak M, Kautschitsch S, Sommergruber W, Tontsch-Grunt U, Garin-Chesa P, Bader G, Zoephel A, Quant J, Heckel A, Rettig WJ: BIBF 1120: triple angiokinase inhibitor with sustained receptor blockade and good antitumor efficacy. Cancer Res. 2008 Jun 15;68(12):4774-82. doi: 10.1158/0008-5472.CAN-07-6307. [PubMed:18559524]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da

Drug created on June 24, 2015 05:32 / Updated on November 22, 2017 12:38