- Guide to PHARMACOLOGY
Synonyms: BIBF-1120 | BIBF1120 | Ofev® | Vargatef®
nintedanib is an approved drug (FDA & EMA (2014))
Compound class: Synthetic organic
Comment: Nintedanib is a kinase inhibitor, targeting three arms of proangiogenic signalling via VEGFRs, PDGFR and FGFR . It was developed by Boehringer Ingelheim.
Marketed formulations contain nintedanib esylate (PubChem CID 135476717).
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: nintedanib
|No information available.|
|Summary of Clinical Use|
|Nintedanib was originally approved as a treatment for idiopathic pulmonary fibrosis. Subsequently it has been approved (by the FDA) to slow pulmonary fuction decline in patients with systemic sclerosis-associated interstitial lung diseases (ILD).
Click here to link to ClinicalTrials.gov current list of nintedanib studies.
In October 2019 the FDA granted Breakthrough Therapy Designation to nintedanib for the treatment of progressive chronic fibrosing ILD, based on preliminary results from the Phase 3 INBUILD trial (NCT02999178). This resulted in full approval for this indication in March 2020.
|Mechanism Of Action and Pharmacodynamic Effects|
|Nintedanib inhibits multiple angiogenic pathways, and appears to also inhibit pathways associated with the fibrotic scarring of the lung observed in idiopathic pulmonary fibrosis (IPF). In tumours inhibition of VEGF receptor (VEGFR), PDGFR and FGFR kinase activity reduces tumour angiogenesis/neo-vascularisation, thereby restricitng tumour expansion . The mechanism in IPF is less clear. See  and  for further information.|
|Clinical Trial ID||Title||Type||Source||Comment||References|
|NCT02999178||Efficacy and Safety of Nintedanib in Patients With Progressive Fibrosing Interstitial Lung Disease (PF-ILD)||Phase 3 Interventional||Boehringer Ingelheim|
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)
European Medicines Agency (EMA)