Preferred Label : Tigozertinib;
NCIt synonyms : EGFR Inhibitor BLU-945; EGFR Mutant-selective Inhibitor BLU-945;
NCIt definition : A fourth-generation, orally bioavailable, mutant-selective, epidermal growth factor
receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration,
tigozertinib targets, binds to and inhibits the activity of EGFR with C797S triple
mutations including ex19del/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.
BLU-945 inhibits mutated forms of EGFR with C797S mutation, which prevents covalent
bond formation with third-generation EGFR inhibitors leading to drug resistance. BLU-945
may have enhanced anti-tumor effects in tumors with C797S-mediated resistance when
compared to other EGFR tyrosine kinase inhibitors.;
UNII : PA4PTH5HL9;
CAS number : 2660250-10-0;
Molecule name : BLU 945; BLU-945;
NCI Metathesaurus CUI : CL1663390;
Origin ID : C180668;
UMLS CUI : C5908095;
Semantic type(s)
- concept_is_in_subset
- has_target
