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Version: 17.06d (Release date: 2017-06-26)
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Afatinib Dimaleate (Code C97273)

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Terms & Properties

Preferred Name: Afatinib Dimaleate

Definition: The dimaleate salt form of afatinib, 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 Dimaleate

Label: Afatinib Dimaleate

NCI Thesaurus Code: C97273 (Search for linked caDSR metadata)  (search value sets)

NCI Metathesaurus Link: C1879772  (see NCI Metathesaurus info)

Synonyms & Abbreviations: (see Synonym Details)
(2E)-N-(4-((3-Chloro-4-fluorophenyl)amino)-7-(((3S)-tetrahydrofuran-3-yl)oxy)quinazolin- 6-yl)-4-(dimethylamino)but-2-enamide bis(hydrogen (2Z)-but-2-enedioate)
2-Butenamide, N-[4-[(3-chloro-4-fluorophenyl)amino]7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-,(2E)-, (2Z)-2-Butenedioate (1:2)
Afatinib Dimaleate
AFATINIB DIMALEATE
BIBW2992 MA2
BIBW 2992MA2
Gilotrif

External Source Codes: 
CAS Registry Number 850140-73-7 (see NLM ChemIDplus info)
FDA UNII Code V1T5K7RZ0B
PDQ Closed Trial Search ID 537572
PDQ Open Trial Search ID 537572 (check for NCI PDQ open clinical trial info)
UMLS CUI C1879772

Other Properties:
     Name Value (qualifiers indented underneath)
code C97273
Contributing_Source CTRP
Contributing_Source FDA
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=C97273

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