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Version: 17.06d (Release date: 2017-06-26)
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Afatinib (Code C66940)

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Terms & Properties

Preferred Name: Afatinib

Definition: An orally bioavailable anilino-quinazoline derivative and inhibitor of the receptor tyrosine kinase (RTK) epidermal growth factor receptor (ErbB; EGFR) family, with antineoplastic activity. Upon administration, afatinib selectively and irreversibly binds to and inhibits the epidermal growth factor receptors 1 (ErbB1; EGFR), 2 (ErbB2; HER2), and 4 (ErbB4; HER4), and certain EGFR mutants, including those caused by EGFR exon 19 deletion mutations or exon 21 (L858R) mutations. This may result in the inhibition of tumor growth and angiogenesis in tumor cells overexpressing these RTKs. Additionally, afatinib inhibits the EGFR T790M gatekeeper mutation which is resistant to treatment with first-generation EGFR inhibitors. EGFR, HER2 and HER4 are RTKs that belong to the EGFR superfamily; they play major roles in both tumor cell proliferation and tumor vascularization and are overexpressed in many cancer cell types.

Display Name: Afatinib

Label: Afatinib

NCI Thesaurus Code: C66940 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C2987648  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
(2e)-N-(4-(3-Chloro-4-Fluoroanilino)-7-(((3s)-Oxolan-3-yl)Oxy)Quinoxazolin-6-yl)-4-(Dimethylamino)But-2-Enamide
Afatinib
AFATINIB
BIBW 2992

External Source Codes: 
CAS Registry Number 850140-72-6 (see NLM ChemIDplus info)
FDA UNII Code 41UD74L59M
ChEBI ID CHEBI:61390 (see ChEBI info)
UMLS CUI C2987648

Other Properties:
     Name Value (qualifiers indented underneath)
Chemical_Formula C24H25ClFN5O3
code C66940
Contributing_Source CTRP
Contributing_Source FDA
Legacy_Concept_Name BIBW_2992
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=C66940

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