Abstract
Merestinib (LY-2801653) is a small-molecule inhibitor of the epithelial cell surface tyrosine kinase receptor, mesenchymal-epithelial transition factor receptor (MET). This promising anticancer agent is currently undergoing clinical development. In this article, we describe MET signaling pathways and interactions, genetic mutations of MET, the significance of MET inhibition in cancer treatment, and possible biomarkers for prediction of patient response to MET inhibitor therapy. The evolution of MET inhibitor research from bench to bedside is discussed, highlighting important aspects of agents that have passed, or are passing through the drug development pipeline, ending with the latest agent of interest, merestinib.