Preferred Label : Rezivertinib;
NCIt synonyms : EGFR Mutant-specific Inhibitor BPI-7711;
NCIt definition : An orally available third-generation and selective inhibitor of certain epidermal
growth factor receptor (EGFR) activating mutations, including the resistance mutations
T790M and L858R, as well as exon 19 deletion, with potential antineoplastic activity.
Upon administration, rezivertinib specifically and covalently binds to and inhibits
selective EGFR mutations, with particularly high selectivity against the T790M mutation,
which prevents EGFR mutant-mediated signaling and leads to cell death in EGFR mutant-expressing
tumor cells. Compared to some other EGFR inhibitors, BPI-7711 may have therapeutic
benefits in tumors with T790M-mediated drug resistance. This agent shows minimal activity
against wild-type EGFR (wt EGFR), and does not cause dose-limiting toxicities that
occur during the use of non-selective EGFR inhibitors, which also inhibit wt EGFR.
EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role
in tumor cell proliferation and tumor vascularization.;
UNII : U65F5M6BD5;
InChIKey : BPMZUKYFIDPLEA-UHFFFAOYSA-N;
CAS number : 1835667-12-3;
Molecule name : BPI-7711; BPI 7711;
NCI Metathesaurus CUI : CL555283;
Origin ID : C154286;
UMLS CUI : C5418249;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
