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Identification
NameNintedanib
Accession NumberDB09079
TypeSmall Molecule
GroupsApproved
DescriptionNintedanib 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 Identifiers
  • BIBF 1120
  • BIBF-1120
  • BIBF1120
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
OfevCapsule100 mgOralBoehringer Ingelheim (Canada) Ltd Ltee2015-06-29Not applicableCanada
OfevCapsule150 mgOralBoehringer Ingelheim (Canada) Ltd Ltee2015-06-29Not applicableCanada
OfevCapsule100 mg/1OralBoehringer Ingelheim Pharmaceuticals, Inc.2014-10-15Not applicableUs
OfevCapsule150 mg/1OralBoehringer Ingelheim Pharmaceuticals, Inc.2014-10-15Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
VargatefBoehringer-Ingelheim
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Nintedanib Esylate
ThumbNot applicableDBSALT001111
Categories
UNIIG6HRD2P839
CAS number656247-17-5
WeightAverage: 539.6248
Monoisotopic: 539.253254569
Chemical FormulaC31H33N5O4
InChI KeyXZXHXSATPCNXJR-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
IndicationNintedanib is indicated for the treatment of idiopathic pulmonary fibrosis (IPF).
Structured Indications
PharmacodynamicsBy 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 actionNintedanib 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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Vascular endothelial growth factor receptor 1Proteinyes
Inhibitor
HumanP17948 details
Vascular endothelial growth factor receptor 2Proteinyes
Inhibitor
HumanP35968 details
Vascular endothelial growth factor receptor 3Proteinyes
Inhibitor
HumanP35916 details
Platelet derived growth factor receptor alphaProteinyes
Inhibitor
Humannot applicabledetails
Platelet derived growth factor receptor betaProteinyes
Inhibitor
Humannot applicabledetails
Fibroblast growth factor receptor 1Proteinyes
Inhibitor
HumanP11362 details
Fibroblast growth factor receptor 2Proteinyes
Inhibitor
HumanP21802 details
Fibroblast growth factor receptor 3Proteinyes
Inhibitor
HumanP22607 details
Receptor-type tyrosine-protein kinase FLT3Proteinunknown
Inhibitor
HumanP36888 details
Tyrosine-protein kinase LckProteinunknown
Inhibitor
HumanP06239 details
Tyrosine-protein kinase LynProteinunknown
Inhibitor
HumanP07948 details
Proto-oncogene tyrosine-protein kinase SrcProteinunknown
Inhibitor
HumanP12931 details
Related Articles
AbsorptionNintedanib reaches maximum plasma concentrations approximately 2 to 4 hours after administration, and absolute bioavailability is 4.7%.
Volume of distribution

1050 L

Protein bindingThe 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.

SubstrateEnzymesProduct
Nintedanib
Not Available
BIBF 1202Details
BIBF 1202
BIBF 1202 glucuronideDetails
Route of eliminationThe 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 life9.5 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.

ToxicityThe 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 organismsNot Available
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot 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
AfatinibThe serum concentration of Nintedanib can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Nintedanib can be increased when it is combined with Albendazole.Approved, Vet Approved
AldosteroneThe serum concentration of Nintedanib can be decreased when it is combined with Aldosterone.Experimental
AlectinibThe serum concentration of Nintedanib can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Nintedanib can be increased when it is combined with Alfentanil.Approved, Illicit
AmantadineThe serum concentration of Nintedanib can be increased when it is combined with Amantadine.Approved
Aminohippuric acidThe serum concentration of Nintedanib can be increased when it is combined with Aminohippuric acid.Approved
AmiodaroneThe serum concentration of Nintedanib can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Nintedanib can be increased when it is combined with Amitriptyline.Approved
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
AmsacrineThe serum concentration of Nintedanib can be increased when it is combined with Amsacrine.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
AnvirzelAnvirzel may decrease the cardiotoxic activities of Nintedanib.Investigational
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, 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
AtenololThe serum concentration of Nintedanib can be increased when it is combined with Atenolol.Approved
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
BenzocaineThe serum concentration of Nintedanib can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Nintedanib can be increased when it is combined with Bepridil.Approved, Withdrawn
BevacizumabBevacizumab may increase the cardiotoxic activities of Nintedanib.Approved, Investigational
BiperidenThe serum concentration of Nintedanib can be increased when it is combined with Biperiden.Approved
BivalirudinThe risk or severity of adverse effects can be increased when Bivalirudin is combined with Nintedanib.Approved, Investigational
BosutinibThe serum concentration of Nintedanib can be increased when it is combined with Bosutinib.Approved
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
BuspironeThe serum concentration of Nintedanib can be increased when it is combined with Buspirone.Approved, Investigational
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
CanagliflozinThe serum concentration of Nintedanib can be increased when it is combined with Canagliflozin.Approved
CandesartanThe serum concentration of Nintedanib can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Nintedanib can be increased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Nintedanib can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarvedilolThe serum concentration of Nintedanib can be increased when it is combined with Carvedilol.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
ChloroquineThe serum concentration of Nintedanib can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorpromazineThe serum concentration of Nintedanib can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Nintedanib can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Nintedanib can be increased when it is combined with Chlorprothixene.Approved, Withdrawn
CholesterolThe serum concentration of Nintedanib can be increased when it is combined with Cholesterol.Experimental
Cholic AcidThe serum concentration of Nintedanib can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Nintedanib can be increased when it is combined with Cilazapril.Approved
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
CitalopramThe serum concentration of Nintedanib can be increased when it is combined with Citalopram.Approved
Citric AcidThe risk or severity of adverse effects can be increased when Citric Acid is combined with Nintedanib.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
ClomipramineThe serum concentration of Nintedanib can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe serum concentration of Nintedanib can be decreased 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
ColforsinThe serum concentration of Nintedanib can be increased when it is combined with Colforsin.Experimental
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
Dabigatran etexilateThe risk or severity of adverse effects can be increased when Dabigatran etexilate is combined with Nintedanib.Approved
DaclatasvirThe serum concentration of Nintedanib can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Nintedanib can be increased when it is combined with Dactinomycin.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
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
DesloratadineThe serum concentration of Nintedanib can be increased when it is combined with Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Nintedanib can be decreased 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
DextromethorphanThe serum concentration of Nintedanib can be increased when it is combined with Dextromethorphan.Approved
DiclofenacThe serum concentration of Nintedanib can be increased when it is combined with Diclofenac.Approved, Vet 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
DigoxinDigoxin 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
DipyridamoleThe serum concentration of Nintedanib can be increased when it is combined with Dipyridamole.Approved
DocetaxelThe risk or severity of adverse effects can be increased when Docetaxel is combined with Nintedanib.Approved, Investigational
DoxazosinThe serum concentration of Nintedanib can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Nintedanib can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Nintedanib can be increased when it is combined with Doxorubicin.Approved, Investigational
DronabinolThe serum concentration of Nintedanib can be increased when it is combined with Dronabinol.Approved, Illicit
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
ElbasvirThe serum concentration of Nintedanib can be increased when it is combined with Elbasvir.Approved
EnalaprilThe serum concentration of Nintedanib can be increased when it is combined with Enalapril.Approved, Vet Approved
EnoxaparinThe risk or severity of adverse effects can be increased when Enoxaparin is combined with Nintedanib.Approved
EnzalutamideThe serum concentration of Nintedanib can be increased when it is combined with Enzalutamide.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
EstramustineThe serum concentration of Nintedanib can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Nintedanib can be decreased when it is combined with Estriol.Approved, Vet Approved
EstroneThe serum concentration of Nintedanib can be decreased when it is combined with Estrone.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
EtravirineThe serum concentration of Nintedanib can be increased when it is combined with Etravirine.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
FexofenadineThe serum concentration of Nintedanib can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Nintedanib can be increased when it is combined with Fidaxomicin.Approved
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
FlupentixolThe serum concentration of Nintedanib can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Nintedanib can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Nintedanib can be increased when it is combined with Flurazepam.Approved, Illicit
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
GefitinibThe serum concentration of Nintedanib can be increased when it is combined with Gefitinib.Approved, Investigational
GenisteinThe serum concentration of Nintedanib can be increased when it is combined with Genistein.Investigational
GlyburideThe serum concentration of Nintedanib can be increased when it is combined with Glyburide.Approved
GlycerolThe serum concentration of Nintedanib can be increased when it is combined with Glycerol.Experimental
Gramicidin DThe serum concentration of Nintedanib can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Nintedanib can be increased when it is combined with Grepafloxacin.Withdrawn
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
HirulogThe risk or severity of adverse effects can be increased when Hirulog is combined with Nintedanib.Experimental
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
ImipramineThe serum concentration of Nintedanib can be increased when it is combined with Imipramine.Approved
IndinavirThe serum concentration of Nintedanib can be increased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Nintedanib can be increased when it is combined with Indomethacin.Approved, Investigational
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
IvermectinThe serum concentration of Nintedanib can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Nintedanib can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe serum concentration of Nintedanib can be increased when it is combined with Ketoconazole.Approved, Investigational
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
LevofloxacinThe serum concentration of Nintedanib can be increased when it is combined with Levofloxacin.Approved, Investigational
LevothyroxineThe serum concentration of Nintedanib can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Nintedanib can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Nintedanib can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Nintedanib can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Nintedanib can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Nintedanib can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Nintedanib can be increased when it is combined with Loperamide.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
MaprotilineThe serum concentration of Nintedanib can be increased when it is combined with Maprotiline.Approved
MebendazoleThe serum concentration of Nintedanib can be increased when it is combined with Mebendazole.Approved, Vet Approved
MefloquineThe serum concentration of Nintedanib can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Nintedanib can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Nintedanib can be increased when it is combined with Meprobamate.Approved, Illicit
MethadoneThe serum concentration of Nintedanib can be increased when it is combined with Methadone.Approved
MetoprololThe serum concentration of Nintedanib can be increased when it is combined with Metoprolol.Approved, Investigational
MibefradilThe serum concentration of Nintedanib can be increased when it is combined with Mibefradil.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 decreased when it is combined with Mifepristone.Approved, Investigational
MitomycinThe serum concentration of Nintedanib can be increased when it is combined with Mitomycin.Approved
MitoxantroneThe serum concentration of Nintedanib can be increased when it is combined with Mitoxantrone.Approved, Investigational
MorphineThe serum concentration of Nintedanib can be increased when it is combined with Morphine.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.Investigational
NaltrexoneThe serum concentration of Nintedanib can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Nintedanib can be increased when it is combined with Naringenin.Experimental
NefazodoneThe serum concentration of Nintedanib can be decreased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Nintedanib can be increased when it is combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Nintedanib can be increased when it is combined with Neostigmine.Approved, Vet Approved
NicardipineThe serum concentration of Nintedanib can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Nintedanib can be decreased 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
NitrazepamThe serum concentration of Nintedanib can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Nintedanib can be increased when it is combined with Nitrendipine.Approved
NorethisteroneThe serum concentration of Nintedanib can be decreased when it is combined with Norethisterone.Approved
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
P-NitrophenolThe serum concentration of Nintedanib can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe serum concentration of Nintedanib can be increased when it is combined with Paclitaxel.Approved, Vet Approved
Palmitic AcidThe serum concentration of Nintedanib can be increased when it is combined with Palmitic Acid.Experimental
PantoprazoleThe serum concentration of Nintedanib can be increased when it is combined with Pantoprazole.Approved
ParoxetineThe serum concentration of Nintedanib can be increased when it is combined with Paroxetine.Approved, Investigational
Pentosan PolysulfateThe risk or severity of adverse effects can be increased when Pentosan Polysulfate is combined with Nintedanib.Approved
PerindoprilThe serum concentration of Nintedanib can be increased when it is combined with Perindopril.Approved
PhenindioneThe risk or severity of adverse effects can be increased when Phenindione is combined with Nintedanib.Approved
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
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.Investigational
Platelet Activating FactorThe serum concentration of Nintedanib can be decreased when it is combined with Platelet Activating Factor.Experimental
PonatinibThe serum concentration of Nintedanib can be increased when it is combined with Ponatinib.Approved
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
PrazosinThe serum concentration of Nintedanib can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Nintedanib can be increased when it is combined with Prednisone.Approved, Vet Approved
ProbenecidThe serum concentration of Nintedanib can be increased when it is combined with Probenecid.Approved
ProgesteroneThe serum concentration of Nintedanib can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromethazineThe serum concentration of Nintedanib can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Nintedanib can be increased when it is combined with Propafenone.Approved
PropranololThe serum concentration of Nintedanib can be increased when it is combined with Propranolol.Approved, Investigational
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
ProtriptylineThe serum concentration of Nintedanib can be increased when it is combined with Protriptyline.Approved
QuercetinThe serum concentration of Nintedanib can be increased when it is combined with Quercetin.Experimental
QuinacrineThe serum concentration of Nintedanib can be increased when it is combined with Quinacrine.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
ReboxetineThe serum concentration of Nintedanib can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Nintedanib can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Nintedanib can be decreased when it is combined with Reserpine.Approved
ReviparinThe risk or severity of adverse effects can be increased when Reviparin is combined with Nintedanib.Approved
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 decreased 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
RolapitantThe serum concentration of Nintedanib can be increased when it is combined with Rolapitant.Approved
SaquinavirThe serum concentration of Nintedanib can be increased when it is combined with Saquinavir.Approved, Investigational
ScopolamineThe serum concentration of Nintedanib can be increased when it is combined with Scopolamine.Approved
SelegilineThe serum concentration of Nintedanib can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
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
SpironolactoneThe serum concentration of Nintedanib can be increased when it is combined with Spironolactone.Approved
St. John's WortThe serum concentration of Nintedanib can be decreased when it is combined with St. John's Wort.Nutraceutical
StaurosporineThe serum concentration of Nintedanib can be increased when it is combined with Staurosporine.Experimental
StreptozocinThe serum concentration of Nintedanib can be decreased when it is combined with Streptozocin.Approved
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
SumatriptanThe serum concentration of Nintedanib can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Nintedanib can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Nintedanib can be increased when it is combined with Tacrine.Withdrawn
TacrolimusThe serum concentration of Nintedanib can be increased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Nintedanib can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Nintedanib can be increased when it is combined with Taurocholic Acid.Experimental
TelmisartanThe serum concentration of Nintedanib can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Nintedanib can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Nintedanib can be increased when it is combined with Terazosin.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
TolvaptanThe serum concentration of Nintedanib can be increased when it is combined with Tolvaptan.Approved
TrastuzumabTrastuzumab may increase the cardiotoxic activities of Nintedanib.Approved, Investigational
TrazodoneThe serum concentration of Nintedanib can be decreased when it is combined with Trazodone.Approved, Investigational
TrifluoperazineThe serum concentration of Nintedanib can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Nintedanib can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrimethoprimThe serum concentration of Nintedanib can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Nintedanib can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Nintedanib can be increased when it is combined with Troleandomycin.Approved
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
Ym150The risk or severity of adverse effects can be increased when Ym150 is combined with Nintedanib.Investigational
ZimelidineThe serum concentration of Nintedanib can be increased when it is combined with Zimelidine.Withdrawn
Food InteractionsNot Available
References
Synthesis ReferenceNot Available
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
ATC CodesL01XE31
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (484 KB)
MSDSNot Available
ADMET
Predicted ADMET featuresNot Available
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
CapsuleOral100 mg
CapsuleOral100 mg/1
CapsuleOral150 mg/1
CapsuleOral150 mg
PricesNot Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6762180 No2000-12-102020-12-10Us
US7119093 No2004-02-212024-02-21Us
US7989474 No2004-04-062024-04-06Us
Properties
StateSolid
Experimental PropertiesNot 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 FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as indolecarboxylic acids. These are compounds containing a carboxylic acid group linked to an indole.
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassIndoles and derivatives
Sub ClassIndolecarboxylic acids and derivatives
Direct ParentIndolecarboxylic acids
Alternative Parents
Substituents
  • Indolecarboxylic acid
  • N-piperazineacetamide
  • Alpha-amino acid or derivatives
  • Dihydroindole
  • Benzylether
  • Substituted aniline
  • Benzoyl
  • N-alkylpiperazine
  • N-methylpiperazine
  • Aniline
  • Benzenoid
  • Piperazine
  • 1,4-diazinane
  • Monocyclic benzene moiety
  • Vinylogous amide
  • Methyl ester
  • Tertiary carboxylic acid amide
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Lactam
  • Carboxylic acid ester
  • Carboxamide group
  • Azacycle
  • Monocarboxylic acid or derivatives
  • Enamine
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Amine
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available

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 survival, cell migration, macrophage function, chemotaxis, and cancer cell invasion. May play an essential role as a negative regulator of embryonic angiogenesis by inhibiting excessive proliferation ...
Gene Name:
FLT1
Uniprot ID:
P17948
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 embryonic hematopoiesis. Promotes proliferation, survival, migration and differentiation of endothelial cells. Promotes reorganization of the actin cytoskeleton. Isoforms lacking a transmembrane domai...
Gene Name:
KDR
Uniprot ID:
P35968
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 cardiovascular system during embryonic development. Promotes proliferation, survival and migration of endothelial cells, and regulates angiogenic sprouting. Signaling by activated FLT4 leads to enhanced pr...
Gene Name:
FLT4
Uniprot ID:
P35916
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 and migration. Required for normal mesoderm patterning and correct axial organization during embryonic development, normal skeletogenesis and normal development of the gonadotropin-releasing hormone (...
Gene Name:
FGFR1
Uniprot ID:
P11362
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 apoptosis, and in the regulation of embryonic development. Required for normal embryonic patterning, trophoblast function, limb bud development, lung morphogenesis, osteogenesis and skin development. Plays an...
Gene Name:
FGFR2
Uniprot ID:
P21802
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 essential role in the regulation of chondrocyte differentiation, proliferation and apoptosis, and is required for normal skeleton development. Regulates both osteogenesis and postnatal bone mineraliz...
Gene Name:
FGFR3
Uniprot ID:
P22607
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. Promotes phosphorylation of SHC1 and AKT1, and activation of the downstream effector MTOR. Promotes activation of RAS signaling and phosphorylation of downstream kinases, including MAPK1/ERK2 and/or...
Gene Name:
FLT3
Uniprot ID:
P36888
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-cell antigen receptor (TCR)-linked signal transduction pathways. Constitutively associated with the cytoplasmic portions of the CD4 and CD8 surface receptors. Association of the TCR with a peptide antig...
Gene Name:
LCK
Uniprot ID:
P06239
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, responses to growth factors and cytokines, integrin signaling, but also responses to DNA damage and genotoxic agents. Functions primarily as negative regulator, but can also function as activator, depending ...
Gene Name:
LYN
Uniprot ID:
P07948
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 receptors, receptor protein tyrosine kinases, G protein-coupled receptors as well as cytokine receptors. Participates in signaling pathways that control a diverse spectrum of biological activities including...
Gene Name:
SRC
Uniprot ID:
P12931
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
Molecular Weight:
141477.255 Da
Comments
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Drug created on June 24, 2015 05:32 / Updated on December 07, 2016 02:40