Preferred Label : EGFR Mutant-selective Inhibitor BBT-176;
NCIt synonyms : Epidermal Growth Factor Receptor Mutant-selective Inhibitor BBT-176; Mutant-selective EGFR Inhibitor BBT-176;
NCIt definition : A fourth-generation, orally bioavailable, mutant-selective, epidermal growth factor
receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration,
EGFR mutant-selective inhibitor BBT-176 targets, binds to, and inhibits the activity
of EGFR with C797S triple mutations including Del19/T790M/C797S and L858R/T790M/C797S,
thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit
tumor growth in EGFR-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. BBT-176 inhibits EGFR with C797S mutations, which prevents
covalent bond formation with third-generation EGFR inhibitors leading to drug resistance.
BBT-176 may have enhanced anti-tumor effects in tumors with C797S-mediated resistance
when compared to other EGFR tyrosine kinase inhibitors.;
Molecule name : BBT 176; BBT-176;
NCI Metathesaurus CUI : CL1663071;
Origin ID : C180519;
UMLS CUI : C5556437;
Semantic type(s)
- concept_is_in_subset
- has_target
