Preferred Label : Tuxobertinib;
NCIt synonyms : ErbB Mutant-specific Inhibitor BDTX-189; EGFR/HER2 Inhibitor BDTX-189; Allosteric ErbB Inhibitor BDTX-189;
NCIt definition : An orally bioavailable, irreversible, selective, small-molecule inhibitor of certain
oncogenic driver, allosteric mutations of the ErbB receptor tyrosine kinases epidermal
growth factor receptor (EGFR/ErbB1) and human epidermal growth factor receptor 2 (HER2/neu
or ErbB2), including extracellular domain allosteric mutations of HER2, and EGFR and
HER2 exon 20 insertion mutations, with potential antineoplastic activity. Upon oral
administration, tuxobertinib selectively binds to and inhibits these allosteric ErbB
mutants while sparing wild-type EGFR, which may result in the selective inhibition
of cellular proliferation and angiogenesis in tumor cells and tumors expressing these
allosteric ErbB mutations. EGFR and HER2, ErbB receptor tyrosine kinases mutated or
overexpressed in many tumor cell types, play a key role in tumor cell proliferation
and tumor vascularization.;
UNII : 6CE2107J4T;
CAS number : 2414572-47-5;
Molecule name : BDTX-189; BDTX 189;
NCI Metathesaurus CUI : CL1405430;
Origin ID : C171059;
UMLS CUI : C5667203;
Semantic type(s)
- concept_is_in_subset
- has_target
