Identification

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Name
Nintedanib
Accession Number
DB09079
Type
Small Molecule
Groups
Approved
Description

Nintedanib is a small molecule kinase inhibitor used in the treatment of pulmonary fibrosis, systemic sclerosis-associated interstitial lung disease, and non-small cell lung cancer (NSCLC).8,9 It was first approved for use in the United States in 2014.8 Within the spectrum of idiopathic pulmonary fibrosis treatment options, nintedanib is currently one of only two disease-modifying therapies available and indicated for the condition (the other being Pirfenidone) and as such is used as a first-line treatment following diagnosis to slow down the progressive loss of lung function.6 As a chemotherapeutic agent for NSCLC, nintedanib, in combination with Docetaxel, is reserved for patients who have tried and failed first-line chemotherapeutic options.9

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
  • Nintedanib
External IDs
BIBF 1120 / BIBF-1120 / BIBF1120
Product Ingredients
IngredientUNIICASInChI Key
Nintedanib esylate42F62RTZ4G656247-18-6MMMVNAGRWOJNMW-FJBFXRHMSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
OfevCapsule100 mg/1OralBoehringer Ingelheim Pharmaceuticals, Inc.2014-10-15Not applicableUs
OfevCapsule150 mg/1OralBoehringer Ingelheim Pharmaceuticals, Inc.2014-10-15Not applicableUs
OfevCapsule150 mgOralBoehringer Ingelheim (Canada) Ltd Ltee2015-06-29Not applicableCanada
OfevCapsule100 mgOralBoehringer Ingelheim (Canada) Ltd Ltee2015-06-29Not applicableCanada
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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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)-3-[({4-[N-methyl-2-(4-methylpiperazin-1-yl)acetamido]phenyl}amino)(phenyl)methylidene]-2-oxo-2,3-dihydro-1H-indole-6-carboxylate
SMILES
COC(=O)C1=CC=C2C(NC(=O)\C2=C(/NC2=CC=C(C=C2)N(C)C(=O)CN2CCN(C)CC2)C2=CC=CC=C2)=C1

Pharmacology

Indication

In the US, nintedanib is indicated for the treatment of idiopathic pulmonary fibrosis (IPF)8 and to slow declining pulmonary function in patients with systemic sclerosis-associated interstitial lung disease.10 In the EU, nintedanib is indicated in combination with docetaxel for the treatment of adult patients with metastatic, locally advanced, or locally recurrent non-small cell lung cancer of adenocarcinoma histology who have already tried first-line therapy.9

Associated Conditions
Pharmacodynamics

Nintedanib is a small molecule kinase inhibitor that inhibits upstream kinase activity to ultimately inhibit lung fibroblast proliferation and migration, as well as signalling pathways that promote the proliferation and survival of endothelial and perivascular cells in tumour tissues.8,9,5

Nintedanib poses a risk of drug-induced liver injury, especially within the first three months of therapy.8,9 Liver function tests should be conducted at baseline prior to beginning therapy, at regular intervals for the first three months of therapy, and as indicated thereafter in patients exhibiting symptoms of hepatic injury such as jaundice or right upper quadrant pain. It is not recommended to be used in patients with pre-existing moderate to severe hepatic impairment (Child Pugh class B or C).

Mechanism of action

Nintedanib is a small molecule, competitive, triple angiokinase inhibitor that targets multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs). Many of these RTKs are implicated in lung fibrosis and tumour angiogenesis, so nintedanib is therefore used in the treatment of proliferative diseases such as idiopathic pulmonary fibrosis, non-small cell lung cancer, and systemic sclerosis-associated interstitial lung disease.8,9 The specific RTKs that nintedanib inhibits are platelet-derived growth factor (PDGFR) α and β, fibroblast growth factor receptor (FGFR) 1-3, vascular endothelial growth factor receptor (VEGFR) 1-3, and Fns-Like tyrosine kinase-3 (FLT3).8,9,5 Nintedanib binds to the ATP-binding pocket of these receptors and inhibits their activity, thereby blocking signalling cascades that result in the proliferation and migration of lung fibroblasts. Nintedanib also inhibits kinase signalling pathways in various cells within tumour tissues, including endothelial cells, pericytes, smooth muscle cells, and cells contributing to angiogenesis, culminating in an inhibition of cell proliferation and apoptosis of affected tumour cells.5

In addition to RTK inhibition, nintedanib also prevents the actions of the nRTKs Lck, Lyn, and Src.8,9,5 The contribution of the inhibition of Lck and Lyn towards the therapeutic efficacy of nintedanib is unclear, but inhibition of the Src pathway by nintedanib has been shown to reduce lung fibrosis.5,7

TargetActionsOrganism
AVascular endothelial growth factor receptor 1
inhibitor
Humans
AVascular endothelial growth factor receptor 2
inhibitor
Humans
AVascular endothelial growth factor receptor 3
inhibitor
Humans
APlatelet-derived growth factor receptor alpha
inhibitor
Humans
APlatelet-derived growth factor receptor beta
inhibitor
Humans
AFibroblast growth factor receptor 1
inhibitor
Humans
AFibroblast growth factor receptor 2
inhibitor
Humans
AFibroblast growth factor receptor 3
inhibitor
Humans
UReceptor-type tyrosine-protein kinase FLT3
inhibitor
Humans
UTyrosine-protein kinase Lck
inhibitor
Humans
UTyrosine-protein kinase Lyn
inhibitor
Humans
UProto-oncogene tyrosine-protein kinase Src
inhibitor
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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Absorption

The absolute bioavailability of nintedanib is low at approximately 4.7%, likely owing to substantial first-pass metabolism and the effects of p-glycoprotein (P-gp) transporters.8,9,5 Tmax following oral administration is reached after approximately 2 hours in fasted patients and approximately 4 hours in fed patients, regardless of the food consumed.8,9 Administration of nintedanib following a high-fat, high-calorie meal resulted in an increase in Cmax by approximately 15% and an increase in AUC by approximately 20%.5 Age, body weight, and smoking status have been found to alter exposure to nintedanib, but these effects are not significant enough to warrant dose alterations.8,5

Volume of distribution

Nintedanib appears to follow biphasic disposition kinetics - the observed volume of distribution following intravenous administration is 1050 L8,9, indicating extensive distribution into peripheral tissues. In rats, nintedanib was shown to rapidly and homogeneously distribute into peripheral tissues with the exception of the CNS, suggestive of an inability of nintedanib to cross the blood-brain barrier.5

Protein binding

Plasma protein binding of nintedanib is high, with a bound fraction of 97.8%. Albumin is thought to be the major binding protein.8,9,5

Metabolism

Nintedanib is predominantly metabolized via hydrolytic cleavage by esterases to its principle metabolite, BIBF 1202, which then undergoes glucuronidation via UGT enzymes in the intestines and liver (specifically UGT 1A1, UGT 1A7, UGT 1A8, and UGT 1A10) to form BIBF 1202 glucuronide.8,9,5 The CYP450 enzyme system plays a minor role in nintedanib metabolism, with CYP3A4 believed to be the main contributor - the major CYP-dependent metabolite of nintedanib, a demethylated metabolite termed BIBF 1053, could not be detected in plasma during pharmacokinetic studies and was found only in small quantities in the feces (approximately 4% of total dose).5 CYP-dependent metabolism of nintedanib accounts for roughly 5% of total drug metabolism, as opposed to 25% for esterase cleavage.8,9 Other minor metabolites, M7 and M8, are found in very small quantities in the urine (0.03% and 0.01%, respectively), though their origin and relevance is currently unclear.5

Route of elimination

Nintedanib is eliminated primarily via fecal and biliary excretion, with 93.4% of radio labelled nintedanib found in feces within 120 hours following administration.8,9,5 Renal clearance accounts for a small portion of nintedanib's elimination, approximately 0.65% of the total dose, and excretion of unchanged nintedanib 48 hours after oral and intravenous doses was 0.05% and 1.4%, respectively.8,9,5

Half life

The terminal elimination half-life of nintedanib is approximately 10-15 hours.9,5 In patients with idiopathic pulmonary fibrosis, the effective half-life of nintedanib has been estimated to be approximately 9.5 hours.8,5

Clearance

Nintedanib is has a high total plasma clearance of approximately 1390 mL/min and a renal clearance of 20 mL/min.8

Toxicity

Experience with nintedanib overdose is limited, but patients who inadvertently received higher-than-intended doses during initial trials experienced adverse effects consistent with the known safety profile of nintedanib, for example elevated liver enzymes and significant gastrointestinal effects.8,9

There are no specific guidelines for the treatment of nintedanib overdose - in this case, therapy should be interrupted and general supportive measures employed as indicated.8,9

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
(R)-warfarinThe risk or severity of bleeding can be increased when (R)-warfarin is combined with Nintedanib.
(S)-WarfarinThe risk or severity of bleeding can be increased when (S)-Warfarin is combined with Nintedanib.
3,5-diiodothyropropionic acidThe therapeutic efficacy of 3,5-diiodothyropropionic acid can be decreased when used in combination with Nintedanib.
3,5-DiiodotyrosineThe therapeutic efficacy of 3,5-Diiodotyrosine can be decreased when used in combination with Nintedanib.
4-hydroxycoumarinThe risk or severity of bleeding can be increased when 4-hydroxycoumarin is combined with Nintedanib.
6-Deoxyerythronolide BThe metabolism of Nintedanib can be decreased when combined with 6-Deoxyerythronolide B.
7-ethyl-10-hydroxycamptothecinThe metabolism of Nintedanib can be decreased when combined with 7-ethyl-10-hydroxycamptothecin.
9-aminocamptothecinThe metabolism of 9-aminocamptothecin can be decreased when combined with Nintedanib.
AbaloparatideThe therapeutic efficacy of Abaloparatide can be decreased when used in combination with Nintedanib.
AbataceptThe metabolism of Nintedanib can be increased when combined with Abatacept.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
Not Available

References

Synthesis Reference

Gerald J. Roth, Armin Heckel, Florian Colbatzky, Sandra Handschuh, Jörg Kley, Thorsten Lehmann-Lintz, Ralf Lotz, Ulrike Tontsch-Grunt, Rainer Walter, and Frank Hilberg Journal of Medicinal Chemistry 2009 52 (14), 4466-4480 DOI: 10.1021/jm900431g

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]
  5. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  6. Richeldi L, Collard HR, Jones MG: Idiopathic pulmonary fibrosis. Lancet. 2017 May 13;389(10082):1941-1952. doi: 10.1016/S0140-6736(17)30866-8. Epub 2017 Mar 30. [PubMed:28365056]
  7. Li LF, Kao KC, Liu YY, Lin CW, Chen NH, Lee CS, Wang CW, Yang CT: Nintedanib reduces ventilation-augmented bleomycin-induced epithelial-mesenchymal transition and lung fibrosis through suppression of the Src pathway. J Cell Mol Med. 2017 Nov;21(11):2937-2949. doi: 10.1111/jcmm.13206. Epub 2017 Jun 9. [PubMed:28598023]
  8. FDA Approved Drugs: Nintedanib [Link]
  9. EMA Approved Drugs: Nintedanib [Link]
  10. FDA New Indication Approval: Nintedanib [Link]
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 / 5maf / 5te0 / 6nec

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1Active Not RecruitingTreatmentCervical Carcinoma / Colorectal Adenocarcinoma / Non-Squamous Non-Small Cell Lung Cancer / Platinum-refractory Ovarian Carcinoma / Renal Cell Adenocarcinoma1
1Active Not RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1Active Not RecruitingTreatmentLung Cancers / Stage IB Non-Small Cell Lung Carcinoma AJCC v7 / Stage II Non-Small Cell Lung Cancer AJCC v7 / Stage IIA Non-Small Cell Lung Carcinoma AJCC v7 / Stage IIB Non-Small Cell Lung Carcinoma AJCC v7 / Stage IIIA Non-Small Cell Lung Cancer AJCC v71
1CompletedNot AvailableMalignant Solid Tumours1
1CompletedTreatmentAbdominal wall neoplasm / Neoplasms, Ovarian1
1CompletedTreatmentBreast Cancer1
1CompletedTreatmentGenital Neoplasms, Female1
1CompletedTreatmentHealthy Volunteers8
1CompletedTreatmentHeathy Volunteer1
1CompletedTreatmentHepatic Insufficiency1
1CompletedTreatmentHepatocellular,Carcinoma1
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)7
1CompletedTreatmentMultiple Myeloma (MM)1
1CompletedTreatmentNeoplasms4
1CompletedTreatmentProstatic Neoplasms1
1CompletedTreatmentScleroderma, Systemic1
1CompletedTreatmentTumors2
1CompletedTreatmentTumors, Solid1
1RecruitingTreatmentAcute Myeloid Leukemia With t(9;11)(p22.3;q23.3); MLLT3-KMT2A / Fibroblast Growth Factor Basic Form Measurement / FLT3 Internal Tandem Duplication / Recurrent Adult Acute Myeloid Leukemia / Refractory Acute Myeloid Leukemia1
1SuspendedTreatmentPatients With Any Advanced Solid Tumors1
1TerminatedOtherLung Cancer Non-Small Cell Cancer (NSCLC)1
1TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1TerminatedTreatmentNeoplasms, Ovarian1
1TerminatedTreatmentOvarian Cancer1
1, 2Active Not RecruitingTreatmentCutaneous Malignant Melanoma1
1, 2CompletedTreatmentBreast Cancer1
1, 2Not Yet RecruitingTreatmentAdenocarcinoma of the Lung / NSCLC, Recurrent1
1, 2RecruitingTreatmentCancer of Pancreas1
1, 2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC) / Non Small Cell Lung Cancer Metastatic1
1, 2RecruitingTreatmentRelapsed/Refractory Acute Myeloid Leukemia1
1, 2TerminatedTreatmentGlioblastoma Multiforme (GBM)1
1, 2Unknown StatusTreatmentLeukemia Acute Myeloid Leukemia (AML)1
2Active Not RecruitingTreatmentCarcinoid Tumors / Metastatic Carcinoid Tumors / Neuroendocrine Neoplasms1
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
2Active Not RecruitingTreatmentDifferentiated Thyroid Cancer (DTC) / Medullary Thyroid Cancer (MTC)1
2Active Not RecruitingTreatmentEsophagogastric Adenocarcinoma1
2Active Not RecruitingTreatmentNeoplasms, Lung1
2Active Not RecruitingTreatmentNon-Small Cell Lung Cancer Recurrent / Squamous Cell Carcinoma of Lung / Stage III Non-Small Cell Lung Cancer / Stage IV Non-Small Cell Lung Cancer1
2Active Not RecruitingTreatmentRecurrent Pleural Malignant Mesothelioma / Stage IV Pleural Mesothelioma1
2Active Not RecruitingTreatmentRecurrent or Metastatic Salivary Gland Cancer of the Head and Neck1
2Active Not RecruitingTreatmentRenal Cell Adenocarcinoma1
2Active Not RecruitingTreatmentTransitional Cell Carcinoma1
2Active Not RecruitingTreatmentUterine Cervical Neoplasms1
2CompletedNot AvailableIdiopathic Pulmonary Fibrosis (IPF)1
2CompletedPreventionNeoplasms, Ovarian1
2CompletedSupportive CareLung Non-Squamous Non-Small Cell Carcinoma / Radiation-Induced Pneumonitis / Stage II Lung Non-Small Cell Cancer AJCC v7 / Stage IIA Lung Non-Small Cell Carcinoma AJCC v7 / Stage IIA Non-Small Cell Lung Carcinoma / Stage IIB Lung Non-Small Cell Carcinoma AJCC v7 / Stage IIB Non-Small Cell Lung Carcinoma / Stage III Lung Non-Small Cell Cancer AJCC v7 / Stage IIIA Lung Non-Small Cell Cancer AJCC v7 / Stage IIIA Non-Small Cell Lung Cancer / Stage IIIB Lung Non-Small Cell Cancer AJCC v7 / Stage IIIb Non-small Cell Lung Cancer / Stage IV Lung Non-Small Cell Cancer AJCC v7 / Stage IV Non-Small Cell Lung Cancer1
2CompletedTreatmentAnaplastic Astrocytoma (AA) / Anaplastic Oligoastrocytoma / Anaplastic Oligodendroglioma (AO) / Glioblastomas / Gliosarcoma1
2CompletedTreatmentBreast Cancer1
2CompletedTreatmentColorectal Cancers1
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
2CompletedTreatmentFallopian Tube Cancer / Malignant Peritoneal Neoplasm / Ovarian Cancer1
2CompletedTreatmentFallopian Tube Cancer / Ovarian Cancer1
2CompletedTreatmentHepatocellular,Carcinoma2
2CompletedTreatmentIdiopathic Pulmonary Fibrosis (IPF)1
2CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2CompletedTreatmentLung Cancer Small Cell Lung Cancer (SCLC) / Refractory Small cell lung cancer1
2CompletedTreatmentNeoplasms, Colorectal2
2CompletedTreatmentOvarian Cancer1
2CompletedTreatmentProstatic Neoplasms2
2CompletedTreatmentPulmonary Fibrosis3
2CompletedTreatmentRecurrent Glioblastoma1
2Not Yet RecruitingTreatmentHemorrhagic Hereditary Telangiectasia (HHT)1
2RecruitingPreventionHNSCC / Neoplasms, Head and Neck1
2RecruitingTreatmentAppendix Cancer1
2RecruitingTreatmentBronchiolitis Obliterans (BO) / Bronchiolitis Obliterans Syndrome (BOS)1
2RecruitingTreatmentEndometrial Clear Cell Carcinoma / Ovarian Clear Cell Carcinoma1
2RecruitingTreatmentIdiopathic Pulmonary Fibrosis (IPF) / Lung Transplant; Complications1
2RecruitingTreatmentAdvanced thymic carcinoma / Lung Cancer Metastatic / Lung Cancer Non-Small Cell Cancer (NSCLC) / Lung Cancer Small Cell Lung Cancer (SCLC) / Lung Cancers / Pleural Mesotheliomas1
2RecruitingTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
2RecruitingTreatmentLymphangioleiomyomatosis1
2RecruitingTreatmentMalignant Pleural Mesothelioma (MPM)1
2RecruitingTreatmentSoft Tissue Sarcoma (STS)1
2TerminatedTreatmentBreast Cancer1
2TerminatedTreatmentNeoplasms, Colorectal1
2WithdrawnTreatmentEsophagogastric Adenocarcinoma / Metastatic Disease / No Previous Chemotherapy for Metastatic Esophagogastric Cancer1
2WithdrawnTreatmentLung Cancer Small Cell Lung Cancer (SCLC) / Platinum-sensitive1
2, 3TerminatedTreatmentMesothelioma1
3Active Not RecruitingTreatmentIdiopathic Pulmonary Fibrosis (IPF)1
3Active Not RecruitingTreatmentLung Diseases, Interstitial1
3CompletedTreatmentAbdominal wall neoplasm / Neoplasms, Ovarian1
3CompletedTreatmentIdiopathic Pulmonary Fibrosis (IPF)2
3CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)2
3CompletedTreatmentLung Diseases, Interstitial1
3CompletedTreatmentNeoplasms, Colorectal1
3CompletedTreatmentPulmonary Fibrosis2
3CompletedTreatmentScleroderma, Systemic1
3Not Yet RecruitingTreatmentLung Diseases, Interstitial1
3RecruitingTreatmentLung Diseases, Interstitial1
3RecruitingTreatmentLung-transplant Recipients1
3TerminatedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
4CompletedTreatmentIdiopathic Pulmonary Fibrosis (IPF)4
4Not Yet RecruitingTreatmentProgressive Idiopathic Pulmonary Fibrosis1
4RecruitingTreatmentIdiopathic Pulmonary Fibrosis (IPF)1
Not AvailableActive Not RecruitingNot AvailableIdiopathic Pulmonary Fibrosis (IPF)1
Not AvailableActive Not RecruitingNot AvailablePulmonary Fibrosis1
Not AvailableCompletedNot AvailableIdiopathic Pulmonary Fibrosis (IPF)2
Not AvailableNo Longer AvailableNot AvailableIdiopathic Pulmonary Fibrosis (IPF)2
Not AvailableRecruitingNot AvailableIdiopathic Pulmonary Fibrosis (IPF)1

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)
US7989474No2011-08-022024-04-06Us
US7119093No2006-10-102024-02-21Us
US6762180No2004-07-132020-12-10Us
US9907756No2018-03-062029-06-07Us
US10105323No2018-10-232029-06-04Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)305CRoth, et. al. 2015
water solubility>20mg/mLRoth, et. al. 2015
logP3.0Roth, et. al. 2015
Predicted Properties
PropertyValueSource
Water Solubility0.0309 mg/mLALOGPS
logP3.7ALOGPS
logP2.79ChemAxon
logS-4.2ALOGPS
pKa (Strongest Acidic)10.86ChemAxon
pKa (Strongest Basic)7.23ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area94.22 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity159.1 m3·mol-1ChemAxon
Polarizability58.79 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
Humans
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]
  2. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  3. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
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]
  2. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  3. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
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]
  2. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  3. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
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 PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chem...
Gene Name
PDGFRA
Uniprot ID
P16234
Uniprot Name
Platelet-derived growth factor receptor alpha
Molecular Weight
122668.46 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]
  2. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  3. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Vascular endothelial growth factor binding
Specific Function
Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic...
Gene Name
PDGFRB
Uniprot ID
P09619
Uniprot Name
Platelet-derived growth factor receptor beta
Molecular Weight
123966.895 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]
  2. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  3. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
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]
  2. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  3. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
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]
  2. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  3. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
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]
  2. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  3. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
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]
  2. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  3. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
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]
  2. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  3. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
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]
  2. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  3. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
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]
  2. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  3. FDA Approved Drugs: Nintedanib [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da
References
  1. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  2. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A7
Uniprot ID
Q9HAW7
Uniprot Name
UDP-glucuronosyltransferase 1-7
Molecular Weight
59818.315 Da
References
  1. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  2. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A8
Uniprot ID
Q9HAW9
Uniprot Name
UDP-glucuronosyltransferase 1-8
Molecular Weight
59741.035 Da
References
  1. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  2. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Protein kinase c binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. Isoform 2 lacks transferase activity but acts as a negative reg...
Gene Name
UGT1A10
Uniprot ID
Q9HAW8
Uniprot Name
UDP-glucuronosyltransferase 1-10
Molecular Weight
59809.075 Da
References
  1. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  2. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  2. FDA Approved Drugs: Nintedanib [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
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
References
  1. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
  2. FDA Approved Drugs: Nintedanib [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Secondary active organic cation transmembrane transporter activity
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Wind S, Schmid U, Freiwald M, Marzin K, Lotz R, Ebner T, Stopfer P, Dallinger C: Clinical Pharmacokinetics and Pharmacodynamics of Nintedanib. Clin Pharmacokinet. 2019 Sep;58(9):1131-1147. doi: 10.1007/s40262-019-00766-0. [PubMed:31016670]

Drug created on June 24, 2015 05:32 / Updated on November 22, 2019 04:21