Multi-kinase target profile (KIT, FGFR1-3, PDGFRα, SRC, LCK) (KIT/FGFR/PDGFR/SRC/LCK)

This target profile represents a cluster of tyrosine kinases including the Mast/stem cell growth factor receptor (KIT), Fibroblast Growth Factor Receptors 1-3 (FGFR1-3), Platelet-Derived Growth Factor Receptor alpha (PDGFRα), and the non-receptor kinases Src and Lck. These proteins are integral to various cellular processes such as proliferation, differentiation, and angiogenesis. KIT, FGFR, and PDGFR are transmembrane receptors that trigger intracellular signaling cascades upon ligand binding, while Src and Lck are cytoplasmic kinases involved in immune cell signaling and oncogenic transformation. In many cancers and fibrotic diseases, these kinases are overexpressed or mutated, leading to uncontrolled cell growth and tissue remodeling. Drugs targeting this specific combination, most notably nintedanib, act as multi-kinase inhibitors to disrupt the signaling pathways driving tumor vascularization and myofibroblast activation. This broad-spectrum inhibition is particularly effective in treating idiopathic pulmonary fibrosis and certain solid tumors where multiple redundant pathways contribute to disease progression.

Other names

Triple angiokinase inhibitor targetsNintedanib target profileReceptor tyrosine kinase and Src family kinase group

Competitive inhibition of the ATP-binding pocket of multiple receptor tyrosine kinases (VEGFR, FGFR, PDGFR) and non-receptor tyrosine kinases (Src, Lck), blocking downstream signaling pathways such as PI3K/Akt, MAPK/ERK, and STAT.