Nintedanib’s mechanism of action

Nintedanib is a small molecule that inhibits multiple receptor tyrosine kinases (RTKs) and non-receptor tyrosine kinases (nRTKs). Nintedanib inhibits the following RTKs: platelet-derived growth factor receptor (PDGFR) alpha and beta, fibroblast growth factor receptor (FGFR) 1-3, vascular endothelial growth factor receptor (VEGFR) 1-3, colony-stimulating factor 1 receptor (CSF1R), and Fms-like tyrosine kinase-3 (FLT-3). With the exception of FLT-3, these kinases have been implicated in the pathogenesis of interstitial lung disease (ILD). Nintedanib competitively binds to the adenosine triphosphate (ATP) binding pocket of these kinases and blocks intracellular signaling cascades, which has been shown to be involved in the pathogenesis of fibrotic tissue remodeling in ILD.