Tepotinib, a highly selective inhibitor of the MET receptor tyrosine kinase, was developed using a fully biomarker-driven and model-informed approach to dose selection in early development, with the recommended phase 2 dose of 500 mg/day selected to provide sustained maximal target inhibition in tumor tissue, based on integrated modeling of preclinical PK/PD relationships, clinical PK, and tumor PD data evaluating inhibition of tumor MET phosphorylation in the first-in-human study [14, 31]. This evidence concerns the gene NTRK1 and neoplasm.