EMD 1204831

EMD 1204831 is a potent and highly selective small molecule inhibitor of the mesenchymal–epithelial transition factor (c-Met) receptor tyrosine kinase, also known as the hepatocyte growth factor receptor (HGFR). It acts as a reversible, ATP-competitive inhibitor that selectively suppresses c-Met activity, thereby disrupting downstream signaling pathways involved in tumor cell migration, invasion, survival, and proliferation. Preclinical studies demonstrated that EMD 1204831 inhibits c-Met phosphorylation and downstream signaling in a dose-dependent manner and induces regression of human tumors in xenograft models. The drug was developed for use in advanced solid tumors but its clinical development was discontinued before reaching later-phase trials due to pharmacokinetic challenges related to autoinduction of metabolism. The developer was Merck Serono[5][7][8][10].