Savolitinib

Savolitinib is an inhibitor of cMET tyrosine kinase or hepatocyte growth factor receptor (HGFR). It potently inhibits the tyrosine kinase activity of recombinant cMET in vitro with an IC₅₀ value of 4 nM. It inhibits proliferation of cell lines SNU‐5, SNU‐638, Hs746T, SNU‐620, GTL16 and IM95m with 50% effective inhibitory concentrations of 0.6 nM, 0.8 nM, 1.3 nM, 3.5 nM, 5.6 nM and 14.7 nM respectively. It shows dose‐responsive anti‐tumor efficacy in gastric cancer Hs746t xenograft model treated once‐daily (0.3 mg/kg, 1 mg/kg or 2.5 mg/kg) orally, for 16 days.