Preferred Label : Naquotinib Mesylate;
NCIt definition : The mesylate salt form of naquotinib, an orally available, irreversible, third-generation,
mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential
antineoplastic activity. Upon oral administration, naquotinib covalently binds to
and inhibits the activity of mutant forms of EGFR, including the T790M EGFR mutant,
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. Naquotinib preferentially inhibits mutated forms of EGFR including
T790M, a secondarily acquired resistance mutation, and may have therapeutic benefits
in tumors with T790M-mediated resistance when compared to other EGFR tyrosine kinase
inhibitors. As this agent is selective towards mutant forms of EGFR, its toxicity
profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit
wild-type EGFR.;
UNII : 12T09LV21O;
InChIKey : ALDUQYYVQWGTMR-GJFSDDNBSA-N;
CAS number : 1448237-05-5;
NCI Metathesaurus CUI : CL971703;
Origin ID : C166454;
UMLS CUI : C5237985;
Semantic type(s)
- concept_is_in_subset
- has_free_acid_or_base_form
- is_salt_form_of
