Vascular endothelial growth factor receptor 1, 2, and 3; fibroblast growth factor receptor 1, 2, and 3; and platelet-derived growth factor receptor alpha and beta (VEGFR1-3 / FGFR1-3 / PDGFRα/β)

The target VEGFR1-3 / FGFR1-3 / PDGFRα/β represents a cluster of three major families of receptor tyrosine kinases (RTKs) that collectively regulate angiogenesis, lymphangiogenesis, and fibrogenesis. These receptors—Vascular Endothelial Growth Factor Receptors (VEGFR1, 2, 3), Fibroblast Growth Factor Receptors (FGFR1, 2, 3), and Platelet-Derived Growth Factor Receptors (PDGFRα, β)—are critical for the proliferation and migration of endothelial cells, fibroblasts, and pericytes. In oncology, simultaneous inhibition of these pathways is used to overcome resistance to VEGF-only therapies, as FGF and PDGF signaling often provide compensatory escape mechanisms for tumor vascularization. Beyond cancer, this multi-target profile is central to the treatment of fibrotic diseases like idiopathic pulmonary fibrosis (IPF), where it blocks the activation of fibroblasts and the deposition of extracellular matrix. Drugs targeting this cluster, such as nintedanib and dovitinib, act as small-molecule inhibitors that bind to the intracellular ATP-binding pocket of the receptors, thereby halting downstream oncogenic and pro-fibrotic signaling cascades.

Other names

Triple angiokinase targetVEGFR/FGFR/PDGFR clusterMulti-kinase receptor tyrosine kinase clusterAngiogenic and fibrogenic receptor group

Competitive inhibition of the ATP-binding site of the intracellular tyrosine kinase domain, blocking receptor autophosphorylation and downstream signaling pathways such as MAPK/ERK and PI3K/AKT.