Preferred Label : Mavelertinib;
NCIt synonyms : 2-Propenamide, N-((3R,4R)-4-fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)-3-pyrrolidinyl)-;
NCIt definition : An orally available inhibitor of the epidermal growth factor receptor (EGFR) mutant
form T790M, with potential antineoplastic activity. Mavelertinib specifically binds
to and inhibits EGFR T790M, a secondary acquired resistance mutation, which prevents
EGFR-mediated signaling and leads to cell death in EGFR/T790M-expressing tumor cells.
Compared to some other EGFR inhibitors, PF-06747775 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 can 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 : YXX2180047;
InChIKey : JYIUNVOCEFIUIU-GHMZBOCLSA-N;
CAS number : 1776112-90-3;
Molecule name : PF-06747775;
Origin ID : C120307;
UMLS CUI : C4682405;
Semantic type(s)
- concept_is_in_subset
- has_target
