Definition

An orally bioavailable protein tyrosine kinase inhibitor of the mutated form of the tumor-associated antigen (TAA) mast/stem cell factor receptor c-Kit (SCFR), D816V, with potential antineoplastic activity. Upon oral administration, elenestinib binds to and inhibits the specific c-Kit mutant D816V. This may result in an inhibition of cell proliferation in mast cells that overexpress this c-Kit mutation. D816V, a mutation in which the amino acid asparagine aspartic acid at position 816 in the mast/stem cell growth factor receptor Kit protein is replaced by valine, may drive mastocytosis and other mast cell disorders.