NCIt definition : The succinate salt form of mobocertinib, an orally available inhibitor of human epidermal
growth factor receptor (EGFR) exon 20 insertion mutations, with antineoplastic activity.
Upon oral administration, mobocertinib, and its active metabolites, specifically and
irreversibly binds to and inhibits exon 20 insertion mutations of EGFR. This prevents
EGFR-mediated signaling and leads to cell death in tumor cells expressing exon 20
insertion mutations. In addition, mobocertinib may inhibit the activity of other EGFR
family members, such as human epidermal growth factor receptor 2 (HER2; ERBB2) and
HER4. EGFR, HER-2 and -4 are receptor tyrosine kinases often mutated in numerous tumor
cell types. They play key roles in tumor cell proliferation and tumor vascularization.;