Foretinib

Foretinib is an oral multikinase inhibitor targeting Met, RON, Axl, and vascular endothelial growth factor receptor. Foretinib (XL880, GSK1363089) inhibits HGF receptor family tyrosine kinases with an IC50 of 3 nM for Ron. Foretinib (XL880, GSK1363089) also inhibits KDR, Flt-1, and Flt-4 with IC50 of 0.9, 6.8 and 2.8 nM, respectively. In addition, EXEL-2880 inhibits members of the platelet-derived growth factor receptor family and the angiopoietin-1 receptor Tie-2. Foretinib (XL880, GSK1363089) is the 1st orally available small molecule inhibitor of Met to enter the clinic and appears to be generally well tolerated.