Preferred Label : EGFR Mutant-selective Inhibitor TRX-221;
NCIt synonyms : EGFR Inhibitor TRX-221;
NCIt definition : An orally bioavailable, mutant-selective, fourth-generation epidermal growth factor
receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration,
EGFR mutant-selective inhibitor TRX-221 targets, binds to and inhibits the activity
of EGFR with selective mutations, including Del19/T790M/C797S, L858R/T790M/C797S,
Del19/C797S, L858R/C797S, Del19/T790M, L858R/T790M, Del19, and L858R, thereby preventing
EGFR mutant-mediated signaling. This may both induce cell death and inhibit tumor
growth in EGFR mutant-overexpressing tumor cells. EGFR, a receptor tyrosine kinase
mutated in many tumor cell types, plays a key role in tumor cell proliferation and
tumor vascularization. TRX-221 is able to cross the blood-brain barrier (BBB). By
sparing wild-type (WT) EGFR, TRX-221 may avoid EGFR-related toxicities.;
Molecule name : TRX-221; TRX 221;
NCI Metathesaurus CUI : CL1927626;
Origin ID : C205440;
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