Preferred Label : Zipalertinib;
NCIt synonyms : Mutation-specific EGFR TKI TAS6417; EGFR Mutant-specific Inhibitor CLN-081; Pan-mutation-selective EGFR Tyrosine Kinase Inhibitor CLN-081; Pan- EGFR Inhibitor CLN-081; Pan-mutation-selective EGFR Inhibitor CLN-081;
NCIt definition : An orally available selective inhibitor of a broad spectrum of epidermal growth factor
receptor (EGFR) mutations, including EGFR exon 20 insertion mutations (EGFR Ex20ins;
Ex20ins mutations), with potential antineoplastic activity. CLN-081 is also active
against other EGFR mutations including exon 19 deletions (exon19del), L858R, and T790M,
as well as the less common G719X, L861Q and S768I mutations. Upon administration,
zipalertinib specifically and covalently binds to and inhibits a variety of EGFR mutations,
with particularly high selectivity against EGFR Ex20ins, which prevents EGFR mutant-mediated
signaling and leads to cell death in EGFR mutant-expressing tumor cells. Compared
to some other EGFR inhibitors, CLN-081 may have therapeutic benefits in tumors with
EGFR Ex20ins, as most EGFR mutant-selective inhibitors are not active against EGFR
Ex20ins. 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 : T4YMU8TW9H;
CAS number : 1661854-97-2;
Molecule name : TAS-6417; TAS 6417; CLN 081; CLN-081;
NCI Metathesaurus CUI : CL978830;
Origin ID : C165567;
UMLS CUI : C5708923;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
