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Version: 17.06d (Release date: 2017-06-26)
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EGFR Inhibitor EGF816 (Code C115109)

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Terms & Properties

Preferred Name: EGFR Inhibitor EGF816

Definition: An orally available, irreversible, third-generation, mutant-selective epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, EGF816 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. EGF816 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.

Label: EGFR Inhibitor EGF816

NCI Thesaurus Code: C115109 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: CL472640  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
EGF816
EGFR Inhibitor EGF816

External Source Codes: 
PDQ Closed Trial Search ID 760001
PDQ Open Trial Search ID 760001 (check for NCI PDQ open clinical trial info)
NCI META CUI CL472640

Other Properties:
     Name Value (qualifiers indented underneath)
code C115109
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  

URL: https://ncit.nci.nih.gov/ncitbrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C115109

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