Tyrosine kinases inhibited by Lenvatinib (TKI2-inhibited kinases)

The target refers to a specific set of receptor tyrosine kinases (RTKs) inhibited by Lenvatinib, which is designated as 'Tyrosine Kinase Inhibitor Two' in certain clinical trial protocols, such as the MYCHELANGELO I trial (NCT05497453) for OTX-2002. These kinases include the vascular endothelial growth factor receptors (VEGFR1, VEGFR2, and VEGFR3), fibroblast growth factor receptors (FGFR1, FGFR2, FGFR3, and FGFR4), platelet-derived growth factor receptor alpha (PDGFRα), KIT, and RET. These proteins play critical roles in tumor angiogenesis, lymphangiogenesis, and oncogenic signaling pathways that drive cell proliferation and survival. In the context of hepatocellular carcinoma (HCC), inhibiting these kinases disrupts the blood supply to the tumor and directly inhibits the growth of malignant cells. Drugs targeting these kinases are often used as standard-of-care systemic therapies for advanced or unresectable solid tumors, particularly in the liver and thyroid.

Other names

Lenvatinib targetsVEGFR1-3FGFR1-4PDGFRαKITRETTKI2 targets

ATP-competitive inhibition of receptor tyrosine kinases