NCIt definition : A small-molecule receptor tyrosine kinase (RTK) inhibitor of proto-oncogene receptor
tyrosine kinase (KIT), colony-stimulating factor-1 receptor (CSF1R) and FMS-like tyrosine
kinase 3 (FLT3), with antineoplastic activity. Upon oral administration, pexidartinib
targets, binds to and inhibits phosphorylation of KIT, CSF1R and FLT3 harboring an
internal tandem duplication (ITD) mutation. This results in the inhibition of tumor
cell proliferation. FLT3, CSF1R and FLT3 are overexpressed or mutated in many cancer
cell types and play major roles in tumor cell proliferation and metastasis.;