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Version: 17.06d (Release date: 2017-06-26)
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Osimertinib (Code C116377)

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Terms & Properties

Preferred Name: Osimertinib

Definition: A third-generation, orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Upon oral administration, osimertinib 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. AZD9291 preferentially inhibits mutated forms of EGFR including T790M, a secondarily-acquired resistance mutation, and may have enhanced anti-tumor effects 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 when compared to non-selective EGFR inhibitors which also inhibit wild-type EGFR.

Display Name: Osimertinib

Label: Osimertinib

NCI Thesaurus Code: C116377 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C3896906  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
2-Propenamide, N-(2-((2-(dimethylamino)ethyl)methylamino)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl)amino)phenyl)-

External Source Codes: 
CAS Registry Number 1421373-65-0 (see NLM ChemIDplus info)
PDQ Closed Trial Search ID 747632
PDQ Open Trial Search ID 747632 (check for NCI PDQ open clinical trial info)
UMLS CUI C3896906

Other Properties:
     Name Value (qualifiers indented underneath)
code C116377
Contributing_Source CTRP
Contributing_Source FDA
Semantic_Type Pharmacologic Substance

Additional Concept Data: 
Defined Fully by Roles: No  


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