Nintedanib

Nintedanib is an indolinone derivative and small molecule tyrosine-kinase inhibitor, inhibiting endothelial growth factor activity in enzymatic assays. It targets vascular endothelial growth factor receptor (VEGFR) 1-3, fibroblast growth factor receptor (FGFR), and platelet-derived growth factor receptor (PDGFR) α and β, which may result cell apoptosis, a reduction in tumor vasculature; and the inhibition of tumor cell proliferation and migration. This agent also inhibits some Src family of tyrosine kinases, including Src, Lck, Lyn, and FLT-3.

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Background

Nintedanib binds to the ATP-binding site in the cleft between the amino and carboxy terminal lobes of the kinase domain . Nintedanib binds to and blocks the activation of cell receptors involved in blood vessel formation (angiogenesis) and reshaping. It inhibits cell proliferation in 3 cell types: endothelial cells, pericytes, and smooth muscle cells, resulting in apoptosis. The compound blocks the intracellular signalling needed for the proliferation, migration and transformation of fibroblasts.