Platelet-derived growth factor(PDGF)and its receptors(PDGFR)play crucial role in devel- opment and progression of tumor,and are becoming hot targets for research of anti-cancer therapy.Blockade of PDGF/PDGFR signal transduction pathway can provide a potential and strategic approach to antitumor therapy. In this review,we give an overview about clinical development of pharmaceutical chemical compounds targeted PDGFR.